Record Information
Version 1.0
Creation Date 2009-03-06 11:58:07 -0700
Update Date 2014-08-11 10:01:43 -0600
Accession Number T3D0127
Identification
Common Name Chlorpyrifos
Description Chlorpyrifos is an organophosphate insecticide. In the home, it is used to control cockroaches, fleas, and termites; it is also used in some pet flea and tick collars. On the farm, it is used to control ticks on cattle and as a spray to control crop pests. (L268)
Compound Type
  • Organic Compound
  • Organochloride
  • Aromatic Hydrocarbon
  • Organophosphate
  • Insecticide
Chemical Structure
Thumb
Synonyms
  1. Bonidel
  2. Brodan
  3. Chloropyrifos
  4. Chloropyriphos
  5. Chlorpyrifos (ban)
  6. Chlorpyrifos (dursban)
  7. Chlorpyrifos [ban]
  8. Chlorpyrifos ethyl
  9. Chlorpyrifos-ethyl
  10. Chlorpyriphos
  11. Chlorpyriphos [iso-french]
  12. Chlorpyriphos-ethyl
  13. Chlorpyritos
  14. Chlorpyrofos
  15. Chlorpyrophos
  16. Clorpyrifos
  17. Coroban
  18. Crossfire
  19. Danusban
  20. Detmol u.a
  21. Detmol u.a.
  22. Dhanusban
  23. Diethyl O-(3,5,6-trichloro-2-pyridyl) phosphorothioate
  24. Durmet
  25. Dursban
  26. Empire
  27. Equity
  28. Eradex
  29. Ethion, DRY
  30. Ethyl chlorpyriphos
  31. Geodinfos
  32. Grofo
  33. Killmaster
  34. Lentrek
  35. Lock-on
  36. Lorsban
  37. Lorsban 50SL
  38. Loxiran
  39. M-chlorpyrifos
  40. O,O-Diaethyl-O-3,5,6-trichlor-2-pyridylmonothiophosphat
  41. O,O-Diethyl O-(3,5,6-Trichloro-2-pyridyl) phosphorothioate
  42. O,O-Diethyl O-(3,5,6-trichloro-2-pyridinyl)phosphorothioate
  43. O,O-Diethyl O-(3,5,6-trichloro-2-pyridyl) phsophorothioate
  44. O,O-Diethyl O-3,5,6-trichloro-2-pyridyl phosphorothioate
  45. O,O-Diethyl-o-(3,5,6-trichloro-2-pyridyl)phosphorothiolate
  46. O,O-diethyl O-(3,5,6-trichloropyridin-2-yl) thiophosphate
  47. Pageant
  48. Piridane
  49. Pyrinex
  50. Radar
  51. Radar (fungicide)
  52. Silrifos
  53. Spannit
  54. Stipend
  55. Suscon
  56. Suscon blue
  57. Suscon green
  58. Tafaban
  59. Talon
  60. Terial
  61. Trichlorpyrphos
  62. Zidil
  63. o,o-Diethyl o-(3,5,6-trichloro-2-pyridinyl) thiophosphate
  64. o,o-Diethyl-o-(3,5,6-trichloro-2-pyridyl)phosphorothioate
  65. Chlorpyrifos
  66. Phosphorothioic acid, O,O-diethyl O-(3,5,6-trichloro-2-pyridinyl) ester
Chemical Formula C9H11Cl3NO3PS
Average Molecular Weight 350.586
Monoisotopic Molecular Weight 348.926283546
IUPAC Name
ethyl 3,5,6-trichloropyridin-2-yl ethoxy(sulfanylidene)phosphonite
Traditional IUPAC Name
chlorpyrifos
CAS Registry Number 2921-88-2
SMILES
CCOP(=S)(OCC)OC1=NC(Cl)=C(Cl)C=C1Cl
InChI Identifier
InChI=1S/C9H11Cl3NO3PS/c1-3-14-17(18,15-4-2)16-9-7(11)5-6(10)8(12)13-9/h5H,3-4H2,1-2H3
InChI Key InChIKey=SBPBAQFWLVIOKP-UHFFFAOYSA-N
Chemical Taxonomy
Kingdom Organic Compounds
Super Class Heterocyclic Compounds
Class Pyridines and Derivatives
Sub Class Hydropyridines
Direct Parent Pyridinones
Alternative Parents
  • Aryl Chlorides
  • Organic Phosphoric Acids
  • Organic Thiophosphoric Acid Esters
  • Organic Thiophosphonic Acid Derivatives
  • Organonitrogen Compounds
  • Organosulfur Compounds
Molecular Framework Aromatic Heteromonocyclic Compounds
Substituents
  • aryl chloride
  • organic halide
  • organochloride
  • organonitrogen compound
  • organic thiophosphoric acid ester
  • thiophosphonic-acid-derivative
  • organosulfur compound
  • organic phosphate
External Descriptors
  • a small molecule(Cyc)
  • organochlorine insecticide(ChEBI)
  • organic thiophosphate(ChEBI)
  • organothiophosphate insecticide(ChEBI)
  • Organophosphorus insecticides(KEGG)
  • organochlorine acaricide(ChEBI)
Biological Properties
Status Unknown/Not Detected
Origin Not Available
Cellular Locations Not Available
Biofluid Locations Not Available
Tissue Locations Not Available
Pathways Not Available
Physical Properties
State Not Available
Appearance White crystals.
Experimental Properties
Property Value
Melting Point 42 C
Boiling Point Not Available
Solubility 0.00112 mg/mL at 24 °C [YALKOWSKY,SH & DANNENFELSER,RM (1992)]
LogP Not Available
Predicted Properties
PropertyValueSource
water solubility1.45e-03 g/lALOGPS
logP5.15ALOGPS
logP4.78ChemAxon
logS-5.4ALOGPS
pKa (strongest basic)-4.2ChemAxon
physiological charge0ChemAxon
hydrogen acceptor count1ChemAxon
hydrogen donor count0ChemAxon
polar surface area40.58ChemAxon
rotatable bond count6ChemAxon
refractivity79ChemAxon
polarizability30.42ChemAxon
Spectra
Spectra Not Available
Toxicity Profile
Route of Exposure Oral (L268) ; inhalation (L268) ; dermal (L268)
Mechanism of Toxicity Chlorpyrifos and its bioactivation product, chlorpyrifos oxon, inhibit neural acetylcholinesterase by forming a stable covalent bond at the active site. The result of this acetylcholinesterase inhibition is cholinergic overstimulation of the central nervous system. Chlorpyrifos oxon also binds to muscarinic receptors, altering the signal transduction, which affects cellular signalling and disrupts neurological function. It also inhibits an endogenous signaling modulator, fatty acid amide hydrolase, producing secondary neurotoxicity. Chlorpyrifos alters cytochrome P-450 levels, controlling the metabolism of itself and other xenobiotics, and inhibits neuropathy target esterase, producing ataxia. (L268, A163, A165, A167, A217))
Metabolism Chlorpyrifos is absorbed mainly via ingestion and inhalation, but may also be absorbed to a lesser extent through the skin. Chlorpyrifos rapidly distributes to all the major organs and is bioactivated to chlorpyrifos oxon in the liver via cytochrome P-450-dependent desulfuration. The oxon is hydrolyzed by A-esterase to diethylphosphate and 3,5,6-trichloro-2-pyridinol (TCP), the major metabolite. Chlorpyrifos is primarily excreted in the urine in the form of TCP conjugates. (L268)
Toxicity Values LD50: 102 mg/kg (Oral, Rat) (T42) LD50: 1233 mg/kg (Dermal, Rabbit) (T42) LD50: 192 mg/kg (Intraperitoneal, Mouse) (T14) LC50: 560 mg/m3 over 4 hours (Inhalation, Rat) (T42)
Lethal Dose 300 mg/kg for an adult human. (T26)
Carcinogenicity (IARC Classification) Not Available
Uses/Sources Chlorpyrifos is used as a pesticide. In the home, it is used to control cockroaches, fleas, and termites; it is also used in some pet flea and tick collars. On the farm, it is used to control ticks on cattle and as a spray to control crop pests. (L268)
Minimum Risk Level Acute Oral: 0.003 mg/kg/day (L134) Intermediate Oral: 0.003 mg/kg/day (L134) Chronic Oral: 0.001 mg/kg/day (L134)
Health Effects Chlorpyrifos damages the nervous system. High levels may result in severe sweating, loss of bowel control, severe muscle tremors, seizures, loss of consciousness, coma, or death. (L268)
Symptoms Chlorpyrifos exposure may produce a variety of effects on the nervous system including headaches, blurred vision, lacrimation, excessive salivation, runny nose, dizziness, confusion, muscle weakness or tremors, nausea, diarrhea, and sudden changes in heart rate. High levels may result in severe sweating, loss of bowel control, severe muscle tremors, seizures, loss of consciousness, coma, or death. (L268)
Treatment The effects of chlorpyrifos can be reversed by administration of the cholinergic blocking agent, atropine. (L268)
Normal Concentrations
Not Available
DrugBank ID Not Available
HMDB ID Not Available
PubChem Compound ID 2730
ChEMBL ID Not Available
ChemSpider ID Not Available
KEGG ID C14322
UniProt ID Not Available
OMIM ID Not Available
ChEBI ID 34631
BioCyc ID Not Available
CTD ID D004390
Stitch ID Chlorpyrifos
PDB ID Not Available
ACToR ID 465
Wikipedia Link Chlorpyrifos
References
General References
  • A163 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35. [7513360 ]
  • A165 — Das PC, Cao Y, Rose RL, Cherrington N, Hodgson E: Enzyme induction and cytotoxicity in human hepatocytes by chlorpyrifos and N,N-diethyl-m-toluamide (DEET). Drug Metabol Drug Interact. 2008;23(3-4):237-60. [19326769 ]
  • A167 — Richardson RJ, Moore TB, Kayyali US, Fowke JH, Randall JC: Inhibition of hen brain acetylcholinesterase and neurotoxic esterase by chlorpyrifos in vivo and kinetics of inhibition by chlorpyrifos oxon in vitro: application to assessment of neuropathic risk. Fundam Appl Toxicol. 1993 Apr;20(3):273-9. [7684990 ]
  • A217 — Quistad GB, Sparks SE, Casida JE: Fatty acid amide hydrolase inhibition by neurotoxic organophosphorus pesticides. Toxicol Appl Pharmacol. 2001 May 15;173(1):48-55. [11350214 ]
  • T14 — Lewis RJ (1996). Sax's Dangerous Properties of Industrial Materials. 9th ed. Volumes 1-3. New York, NY: Van Nostrand Reinhold.
  • T26 — National Institute for Occupational Safety and Health (2002). RTECS: Registry of Toxic Effects of Chemical Substances.
  • T42 — FAO/WHO (1999). Pesticide Residues in Food, Toxicological Evaluations, Chlorpyrifos.
  • L134 — ATSDR - Agency for Toxic Substances and Disease Registry (2001). Minimal Risk Levels (MRLs) for Hazardous Substances. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
  • L268 — ATSDR - Agency for Toxic Substances and Disease Registry (1997). Toxicological profile for chlorpyrifos. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]

Targets

1. Acetylcholinesterase

Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.

Chlorpyrifos and its bioactivation product, chlorpyrifos oxon, and inhibit neural acetylcholinesterase by forming a stable covalent bond at the active site. The result of this acetylcholinesterase inhibition is cholinergic overstimulation of the central nervous system. (L268)
UniProt ID: P22303
Gene: ACHE
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • L268 — ATSDR - Agency for Toxic Substances and Disease Registry (1997). Toxicological profile for chlorpyrifos. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]

2. Muscarinic acetylcholine receptor M1

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.

Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (A163)
UniProt ID: P11229
Gene: CHRM1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A163 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35. [7513360 ]

3. Muscarinic acetylcholine receptor M2

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition.

Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (A163)
UniProt ID: P08172
Gene: CHRM2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A163 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35. [7513360 ]

4. Muscarinic acetylcholine receptor M3

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.

Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (A163)
UniProt ID: P20309
Gene: CHRM3
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A163 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35. [7513360 ]

5. Muscarinic acetylcholine receptor M4

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.

Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (A163)
UniProt ID: P08173
Gene: CHRM4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A163 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35. [7513360 ]

6. Muscarinic acetylcholine receptor M5

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.

Chlorpyrifos oxon binds to muscarinic receptors, altering the receptors signal transduction, which affects cellular signalling and disrupts neurological function. (A163)
UniProt ID: P08912
Gene: CHRM5
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A163 — Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35. [7513360 ]

7. Serum albumin

Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.

Chlorpyrifos oxon binds albumin and may generate an antibody response. (A164)
UniProt ID: P02768
Gene: ALB
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A164 — Li B, Schopfer LM, Hinrichs SH, Masson P, Lockridge O: Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry assay for organophosphorus toxicants bound to human albumin at Tyr411. Anal Biochem. 2007 Feb 15;361(2):263-72. Epub 2006 Dec 4. [17188226 ]

8. Cytochrome P450 3A4

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,8-cineole 2-exo-monooxygenase. The enzyme also hydroxylates etoposide.

Chlorpyrifos is an irreversible non-competitive inhibitor of cytochrome P-450 3A4. (A166)
UniProt ID: P08684
Gene: CYP3A4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A166 — Usmani KA, Hodgson E, Rose RL: In vitro metabolism of carbofuran by human, mouse, and rat cytochrome P450 and interactions with chlorpyrifos, testosterone, and estradiol. Chem Biol Interact. 2004 Dec 7;150(3):221-32. [15560889 ]

9. Neuropathy target esterase

Phospholipase B that deacylates intracellular phosphatidylcholine (PtdCho), generating glycerophosphocholine (GroPtdCho). This deacylation occurs at both sn-2 and sn-1 positions of PtdCho. Its specific chemical modification by certain organophosphorus (OP) compounds leads to distal axonopathy.

Chlorpyrifos inhibits neuropathy target esterase, producing ataxia. (A167)
UniProt ID: Q8IY17
Gene: PNPLA6
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A167 — Richardson RJ, Moore TB, Kayyali US, Fowke JH, Randall JC: Inhibition of hen brain acetylcholinesterase and neurotoxic esterase by chlorpyrifos in vivo and kinetics of inhibition by chlorpyrifos oxon in vitro: application to assessment of neuropathic risk. Fundam Appl Toxicol. 1993 Apr;20(3):273-9. [7684990 ]

10. Cannabinoid receptor 1

Involved in cannabinoid-induced CNS effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. Inhibits L-type Ca(2+) channel current. Isoform 2 and isoform 3 have altered ligand binding.

Chlorpyrifos oxon inhibits cannabinoid receptor 1. (A168)
UniProt ID: P21554
Gene: CNR1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A168 — Quistad GB, Nomura DK, Sparks SE, Segall Y, Casida JE: Cannabinoid CB1 receptor as a target for chlorpyrifos oxon and other organophosphorus pesticides. Toxicol Lett. 2002 Sep 5;135(1-2):89-93. [12243867 ]

11. Fatty-acid amide hydrolase 1

Degrades bioactive fatty acid amides like oleamide, the endogenous cannabinoid, anandamide and myristic amide to their corresponding acids, thereby serving to terminate the signaling functions of these molecules. Hydrolyzes polyunsaturated substrate anandamide preferentially as compared to monounsaturated substrates.

Chlorpyrifos inhibits an endogenous signaling modulator, fatty acid amide hydrolase, producing secondary neurotoxicity. (A217)
UniProt ID: O00519
Gene: FAAH
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A217 — Quistad GB, Sparks SE, Casida JE: Fatty acid amide hydrolase inhibition by neurotoxic organophosphorus pesticides. Toxicol Appl Pharmacol. 2001 May 15;173(1):48-55. [11350214 ]

12. Fatty-acid amide hydrolase 2

Degrades bioactive fatty acid amides like oleamide, the endogenous cannabinoid, anandamide and myristic amide to their corresponding acids, thereby serving to terminate the signaling functions of these molecules. Hydrolyzes monounsaturated substrate anandamide preferentially as compared to polyunsaturated substrates.

Chlorpyrifos inhibits an endogenous signaling modulator, fatty acid amide hydrolase, producing secondary neurotoxicity. (A217)
UniProt ID: Q6GMR7
Gene: FAAH2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • A217 — Quistad GB, Sparks SE, Casida JE: Fatty acid amide hydrolase inhibition by neurotoxic organophosphorus pesticides. Toxicol Appl Pharmacol. 2001 May 15;173(1):48-55. [11350214 ]

13. Calcium-transporting ATPase type 2C member 1

This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of the calcium.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P98194
Gene: ATP2C1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

14. Calcium-transporting ATPase type 2C member 2

This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium (By similarity).

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: O75185
Gene: ATP2C2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

15. Gamma-aminobutyric acid receptor subunit alpha-1

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P14867
Gene: GABRA1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

16. Gamma-aminobutyric acid receptor subunit alpha-2

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P47869
Gene: GABRA2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

17. Gamma-aminobutyric acid receptor subunit alpha-3

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P34903
Gene: GABRA3
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

18. Gamma-aminobutyric acid receptor subunit alpha-4

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P48169
Gene: GABRA4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

19. Gamma-aminobutyric acid receptor subunit alpha-5

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P31644
Gene: GABRA5
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

20. Gamma-aminobutyric acid receptor subunit alpha-6

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: Q16445
Gene: GABRA6
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

21. Gamma-aminobutyric acid receptor subunit beta-1

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P18505
Gene: GABRB1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

22. Gamma-aminobutyric acid receptor subunit beta-2

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P47870
Gene: GABRB2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

23. Gamma-aminobutyric acid receptor subunit beta-3

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P28472
Gene: GABRB3
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

24. Gamma-aminobutyric acid receptor subunit delta

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: O14764
Gene: GABRD
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

25. Gamma-aminobutyric acid receptor subunit epsilon

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P78334
Gene: GABRE
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

26. Gamma-aminobutyric acid receptor subunit gamma-1

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: Q8N1C3
Gene: GABRG1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

27. Gamma-aminobutyric acid receptor subunit gamma-2

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P18507
Gene: GABRG2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

28. Gamma-aminobutyric acid receptor subunit gamma-3

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: Q99928
Gene: GABRG3
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

29. Gamma-aminobutyric acid receptor subunit pi

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to modulatory agents such as pregnanolone.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: O00591
Gene: GABRP
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

30. Gamma-aminobutyric acid receptor subunit rho-1

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA receptor could play a role in retinal neurotransmission.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P24046
Gene: GABRR1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

31. Gamma-aminobutyric acid receptor subunit rho-2

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-2 GABA receptor could play a role in retinal neurotransmission.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: P28476
Gene: GABRR2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

32. Gamma-aminobutyric acid receptor subunit rho-3

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel (By similarity).

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: A8MPY1
Gene: GABRR3
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

33. Gamma-aminobutyric acid receptor subunit theta

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.

This organochloride antagonizes the action of the neurotransmitter gamma-aminobutyric acid (GABA) acting at the GABA-A receptors, effectively blocking the GABA-induced uptake of chloride ions and causing hyperexcitability of the central nervous system. (T10)
UniProt ID: Q9UN88
Gene: GABRQ
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

34. Plasma membrane calcium-transporting ATPase 1

This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium out of the cell.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P20020
Gene: ATP2B1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

35. Plasma membrane calcium-transporting ATPase 2

This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium out of the cell.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: Q01814
Gene: ATP2B2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

36. Plasma membrane calcium-transporting ATPase 3

This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium out of the cell.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: Q16720
Gene: ATP2B3
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

37. Plasma membrane calcium-transporting ATPase 4

This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium out of the cell.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P23634
Gene: ATP2B4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

38. Sarcoplasmic/endoplasmic reticulum calcium ATPase 1

This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the translocation of calcium from the cytosol to the sarcoplasmic reticulum lumen. Contributes to calcium sequestration involved in muscular excitation/contraction.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: O14983
Gene: ATP2A1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

39. Sarcoplasmic/endoplasmic reticulum calcium ATPase 2

This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the translocation of calcium from the cytosol to the sarcoplasmic reticulum lumen. Isoform 2 is involved in the regulation of the contraction/relaxation cycle.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P16615
Gene: ATP2A2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

40. Sarcoplasmic/endoplasmic reticulum calcium ATPase 3

This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of calcium. Transports calcium ions from the cytosol into the sarcoplasmic/endoplasmic reticulum lumen. Contributes to calcium sequestration involved in muscular excitation/contraction.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: Q93084
Gene: ATP2A3
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

41. Sodium/potassium-transporting ATPase subunit gamma

May be involved in forming the receptor site for cardiac glycoside binding or may modulate the transport function of the sodium ATPase.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P54710
Gene: FXYD2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

42. Sodium/potassium-transporting ATPase subunit alpha-1

This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions, providing the energy for active transport of various nutrients.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P05023
Gene: ATP1A1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

43. Sodium/potassium-transporting ATPase subunit alpha-2

This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium, providing the energy for active transport of various nutrients.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P50993
Gene: ATP1A2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

44. Sodium/potassium-transporting ATPase subunit alpha-3

This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions, providing the energy for active transport of various nutrients.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P13637
Gene: ATP1A3
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

45. Sodium/potassium-transporting ATPase subunit alpha-4

This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions, providing the energy for active transport of various nutrients. Plays a role in sperm motility.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: Q13733
Gene: ATP1A4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

46. Sodium/potassium-transporting ATPase subunit beta-1

This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The beta subunit regulates, through assembly of alpha/beta heterodimers, the number of sodium pumps transported to the plasma membrane.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P05026
Gene: ATP1B1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

47. Sodium/potassium-transporting ATPase subunit beta-2

This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The exact function of the beta-2 subunit is not known.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P14415
Gene: ATP1B2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

48. Sodium/potassium-transporting ATPase subunit beta-3

This is the non-catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of Na(+) and K(+) ions across the plasma membrane. The exact function of the beta-3 subunit is not known.

This organochloride inhibits Na+/K+ ATPase and Ca2+ and Mg2+ ATPase, which are essential for the transport of calcium across membranes. This results in the accumulation of intracellular free calcium ions, which promotes release of neurotransmitters from storage vesicles, the subsequent depolarization of adjacent neurons, and the propagation of stimuli throughout the central nervous system. (T10)
UniProt ID: P54709
Gene: ATP1B3
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T10 — Casarett LJ, Klaassen CD, and Watkins JB (2003). Casarett and Doull's essentials of toxicology. New York: McGraw-Hill/Medical Pub. Div.

49. Estrogen receptor

Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full length receptor. Isoform 3 can bind to ERE and inhibit isoform 1.

Causes endocrine disruption in humans by binding to and inhibiting the estrogen receptor. (T152)
UniProt ID: P03372
Gene: ESR1
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T152 — Luft S, Milki E, Glustrom E, Ampiah-Bonney R, O'Hara P. Binding of Organochloride and Pyrethroid Pesticides To Estrogen Receptors α and β: A Fluorescence Polarization Assay. Biophysical Journal 2009;96(3):444a.

50. Estrogen receptor beta

Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.

Causes endocrine disruption in humans by binding to and inhibiting the estrogen receptor. (T152)
UniProt ID: Q92731
Gene: ESR2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
References:
  • T152 — Luft S, Milki E, Glustrom E, Ampiah-Bonney R, O'Hara P. Binding of Organochloride and Pyrethroid Pesticides To Estrogen Receptors α and β: A Fluorescence Polarization Assay. Biophysical Journal 2009;96(3):444a.