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Showing toxin card for Midazolam (T3D2859)

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Version 1.0
Creation Date 2009-07-21 20:27:24
Update Date 2010-05-18 21:00:26
Accession Number T3D2859
Name Midazolam
Compound Type
  • Adjuvant, Anesthesia
  • Anesthetic, Intravenous
  • Anti-Anxiety Agent
  • Drug
  • GABA Modulator
  • Hypnotic and Sedative
Description A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH. [PubChem] Midazolam is a schedule IV drug in the United States.
Synonyms
  1. Midazolam Base
  2. Midazolam Hcl
  3. Midazolamum [INN-Latin]
Chemical IUPAC Name 12-chloro-9-(2-fluorophenyl)-3-methyl-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(14),3,5,8,10,12-hexaene
Chemical Formula C18H13ClFN3
Chemical Structure Structure
CAS Registry Number 59467-70-8
InChI Identifier InChI=1S/C18H13ClFN3/c1-11-21-9-13-10-22-18(14-4-2-3-5-16(14)20)15-8-12(19)6-7-17(15)23(11)13/h2-9H,10H2,1H3
InChI Key InChIKey=DDLIGBOFAVUZHB-UHFFFAOYSA-N
PubChem Compound ID 4192 Link Image
KEGG ID C07524 Link Image
UniProt ID Not Available
OMIM ID Not Available
ChEBI ID Not Available
BioCyc ID Not Available
SuperToxic ID Not Available
CTD ID Not Available
Stitch ID Midazolam Link Image
DrugBank ID DB00683 Link Image
PDB ID Not Available
ACToR ID Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Midazolam Link Image
Monoisotopic Mass 325.078203
MOL File Show
PDB File Show
SDF File Show
SMILES CC1=NC=C2CN=C(C3=CC=CC=C3F)C3=CC(Cl)=CC=C3N12
Appearance Not Available
Melting Point 159 oC
Solubility 0.024 mg/mL [Thorsteinn Loftsson and Dagn?? Hreinsd??ttir, 2006]
Predicted LogP 3.1348
Route of Exposure Intravenous
Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Metabolism Midazolam is primarily metabolized in the liver and gut by human cytochrome P450 IIIA4 (CYP3A4) to its pharmacologic active metabolite, (alpha)-hydroxymidazolam, and 4-hydroxymidazolam.
Toxicity Values LD50: 825 mg/kg (Oral, Rat)
Lethal Dose Not Available
Carcinogenicity (IARC Classification) Not Available
Uses/Sources Intravenous midazolam is indicated for procedural sedation (often in combination with an opioid, such as fentanyl), for pre-op sedation, for the induction of general anesthesia, and for sedation of ventilated patients in critical care units. Oral midazolam is indicated for the short term treatment of moderately severe insomnia in patients who did not adequately react to other hypnotics, and who have persistent trouble in falling asleep. [Wikipedia]
Minimum Risk Level Not Available
Health Effects They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive.
Symptoms Not Available
Treatment Treatment of midazolam overdosage is the same as that followed for overdosage with other benzodiazepines. Respiration, pulse rate and blood pressure should be monitored and general supportive measures should be employed. Attention should be given to the maintenance of a patent airway and support of ventilation, including administration of oxygen. Should hypotension develop, treatment may include intravenous fluid therapy, repositioning, judicious use of vasopressors appropriate to the clinical situation, if indicated, and other appropriate counter-measures. Gastrointestinal decontamination with lavage and/or activated charcoal once the patient's airway is secure is also recommended. Flumazenil, a specific benzodiazepine-receptor antagonist, is indicated for the complete or partial reversal of the sedative effects of midazolam and may be used in situations when an overdose with a benzodiazepine is known or suspected. (V650)
General References
  • T838 - Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. [PubMed Link Image]
  • U177 - Vermeeren A: Residual effects of hypnotics: epidemiology and clinical implications. CNS Drugs. 2004;18(5):297-328. [PubMed Link Image]
  • T785 - Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8. [PubMed Link Image]
  • U174 - Drugs.com
  • U176 - Garratt JC, Gent JP, Feely M, Haigh JR: Can benzodiazepines be classified by characterising their anticonvulsant tolerance-inducing potential? Eur J Pharmacol. 1988 Jan 5;145(1):75-80. [PubMed Link Image]
  • U175 - Isojarvi JI, Tokola RA: Benzodiazepines in the treatment of epilepsy in people with intellectual disability. J Intellect Disabil Res. 1998 Dec;42 Suppl 1:80-92. [PubMed Link Image]
Targets
  1. Gamma-aminobutyric acid receptor subunit alpha-1
  2. Gamma-aminobutyric acid receptor subunit beta-1
  3. Gamma-aminobutyric acid receptor subunit beta-3
  4. Gamma-aminobutyric acid receptor subunit alpha-5
  5. Gamma-aminobutyric acid receptor subunit alpha-3
  6. Gamma-aminobutyric acid receptor subunit alpha-2
  7. Gamma-aminobutyric acid receptor subunit beta-2
  8. Gamma-aminobutyric acid receptor subunit alpha-4
  9. Gamma-aminobutyric acid receptor subunit alpha-6
Target 1 [top]
Target 1 ID 36
Target 1 Name Gamma-aminobutyric acid receptor subunit alpha-1
Target 1 Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Target 1 Description 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
Target 1 Synonyms
  1. GABA(A) receptor subunit alpha-1
Target 1 Gene Name GABRA1
Target 1 Protein Sequence >Gamma-aminobutyric acid receptor subunit alpha-1 
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
Target 1 Number of Residues 456
Target 1 Molecular Weight 51801.4
Target 1 Theoretical pI 9.61
Target 1 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
gamma-aminobutyric acid signaling pathway
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in chloride channel activity
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Signals
  • 1-27
Target 1 Transmembrane Regions
  • 252-273
  • 279-300
  • 313-334
  • 422-443
Target 1 Essentiality Non Essential
Target 1 Domain Function PF02931:Neur_chan_LBD PF02932:Neur_chan_memb
Target 1 GenBank ID Protein Not Available
Target 1 UniProtKB ID P14867 Link Image
Target 1 Cellular Location Cell junction, synapse, postsynaptic cell membrane
Target 1 Gene Sequence Not Available
Target 1 GenBank Gene ID Not Available
Target 1 GeneCard ID GABRA1 Link Image
Target 1 GenAtlas ID GABRA1 Link Image
Target 1 HGNC ID HGNC:4075 Link Image
Target 1 Chromosome Location Not Available
Target 1 Locus 5q34-q35
Target 1 SNPs SNPJam Report Link Image
Target 1 Toxin References
  • S912 - Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 1 General References 2465923; 15489334; 2847710; 11992121; 16718694
Target 2 [top]
Target 2 ID 224
Target 2 Name Gamma-aminobutyric acid receptor subunit beta-1
Target 2 Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Target 2 Description 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
Target 2 Synonyms
  1. GABA(A) receptor subunit beta-1
Target 2 Gene Name GABRB1
Target 2 Protein Sequence >Gamma-aminobutyric acid receptor subunit beta-1 
MWTVQNRESLGLLSFPVMITMVCCAHSTNEPSNMSYVKETVDRLLKGYDIRLRPDFGGPP
VDVGMRIDVASIDMVSEVNMDYTLTMYFQQSWKDKRLSYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWNGGEGAVTGVNKIELPQFSIVDYKMVSKKVEFTTGAYPRLSLSFRLK
RNIGYFILQTYMPSTLITILSWVSFWINYDASAARVALGITTVLTMTTISTHLRETLPKI
PYVKAIDIYLMGCFVFVFLALLEYAFVNYIFFGKGPQKKGASKQDQSANEKNKLEMNKVQ
VDAHGNILLSTLEIRNETSGSEVLTSVSDPKATMYSYDSASIQYRKPLSSREAYGRALDR
HGVPSKGRIRRRASQLKVKIPDLTDVNSIDKWSRMFFPITFSLFNVVYWLYYVH
Target 2 Number of Residues 474
Target 2 Molecular Weight 54234.1
Target 2 Theoretical pI 9.01
Target 2 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in chloride channel activity
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Signals
  • 1-25
Target 2 Transmembrane Regions
  • 246-267
  • 271-293
  • 305-327
  • 452-473
Target 2 Essentiality Non Essential
Target 2 Domain Function PF02931:Neur_chan_LBD PF02932:Neur_chan_memb
Target 2 GenBank ID Protein Not Available
Target 2 UniProtKB ID P18505 Link Image
Target 2 Cellular Location Cell junction, synapse, postsynaptic cell membrane
Target 2 Gene Sequence >1425 bp 
ATGTGGACAGTACAAAATCGAGAGAGTCTGGGGCTTCTCTCTTTCCCTGTGATGATTACC
ATGGTCTGTTGTGCACACAGCACCAATGAACCCAGCAACATGCCATACGTGAAAGAGACA
GTGGACAGATTGCTCAAAGGATATGACATTCGCTTGCGGCCGGACTTCGGAGGGCCCCCC
GTCGACGTTGGGATGCGGATCGATGTCGCCAGCATAGACATGGTCTCCGAAGTGAATATG
GATTATACACTCACCATGTATTTCCAGCAGTCTTGGAAAGACAAAAGGCTTTCTTATTCT
GGAATCCCACTGAACCTCACCCTAGACAATAGGGTAGCTGACCAACTCTGGGTACCAGAC
ACCTACTTTCTGAATGACAAGAAATCATTTGTGCATGGGGTCACAGTGAAAAATCGAATG
ATTCGACTGCATCCTGATGGAACAGTTCTCTATGGACTCCGAATCACAACCACAGCTGCA
TGTATGATGGATCTTCGAAGATATCCACTGGATGAGCAGAACTGCACCCTGGAGATCGAA
AGTTATGGCTATACCACTGATGACATTGAATTTTACTGGAATGGAGGAGAAGGGGCAGTC
ACTGGTGTTAATAAAATCGAACTTCCTCAATTTTCAATTGTTGACTACAAGATGGTGTCT
AAGAAGGTGGAGTTCACAACAGGAGCGTATCCACGACTGTCACTAAGTTTTCGTCTAAAG
AGAAACATTGGTTACTTCATTTTGCAAACCTACATGCCTTCTACACTGATTACAATTCTG
TCCTGGGTGTCTTTTTGGATCAACTATGATGCATCTGCAGCCAGAGTCGCACTAGGAATC
ACGACGGTGCTTACAATGACAACCATCAGCACCCACCTCAGGGAGACCCTGCCAAAGATC
CCTTATGTCAAAGCGATTGATATTTATCTGATGGGTTGCTTTGTGTTTGTGTTCCTGGCT
CTGCTGGAGTATGCCTTTGTAAATTACATCTTCTTTGGGAAAGGCCCTCAGAAAAAGGGA
GCTAGCAAACAAGACCAGAGTGCCAATGAGAAGAATAAACTGGAGATGAATAAAGTCCAG
GTCGACGCCCACGGTAACATTCTCCTCAGCACCCTGGAAATCCGGAATGAGACGAGTGGC
TCGGAAGTGCTCACGAGCGTGAGCGACCCCAAGGCCACCATGTACTCCTATGACAGCGCC
AGCATCCAGTACCGCAAGCCCCTGAGCAGCCGCGAGGCCTACGGGCGCGCCCTGGACCGG
CACGGGGTACCCAGCAAGGGGCGCATCCGCAGGCGTGCCTCCCAGCTCAAAGTCAAGATC
CCCGACTTGACTGATGTGAATTCCATAGACAAGTGGTCCCGAATGTTTTTCCCCATCACC
TTTTCTCTTTTTAATGTCGTCTATTGGCTTTACTATGTACACTGA
Target 2 GenBank Gene ID Not Available
Target 2 GeneCard ID GABRB1 Link Image
Target 2 GenAtlas ID GABRB1 Link Image
Target 2 HGNC ID HGNC:4081 Link Image
Target 2 Chromosome Location Not Available
Target 2 Locus 4p12
Target 2 SNPs SNPJam Report Link Image
Target 2 Toxin References
  • S912 - Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 2 General References 2465923; 1655634; 14702039; 15489334; 2160058; 8178835; 17924679
Target 3 [top]
Target 3 ID 193
Target 3 Name Gamma-aminobutyric acid receptor subunit beta-3
Target 3 Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Target 3 Description 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
Target 3 Synonyms
  1. GABA(A) receptor subunit beta-3
Target 3 Gene Name GABRB3
Target 3 Protein Sequence >Gamma-aminobutyric acid receptor subunit beta-3 
MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNR
VDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRS
LPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
Target 3 Number of Residues 473
Target 3 Molecular Weight 54115.0
Target 3 Theoretical pI 9.41
Target 3 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 3 General Function Involved in chloride channel activity
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Signals
  • 1-25
Target 3 Transmembrane Regions
  • 246-267
  • 271-293
  • 305-327
  • 451-472
Target 3 Essentiality Non Essential
Target 3 Domain Function PF02931:Neur_chan_LBD PF02932:Neur_chan_memb
Target 3 GenBank ID Protein Not Available
Target 3 UniProtKB ID P28472 Link Image
Target 3 Cellular Location Cell junction, synapse, postsynaptic cell membrane
Target 3 Gene Sequence >1422 bp 
ATGTGGGGCCTTGCGGGAGGAAGGCTTTTCGGCATCTTCTCGGCCCCGGTGCTGGTGGCT
GTGGTGTGCTGCGCCCAGAGTGTGAACGATCCCGGGAACATGTCCTTTGTGAAGGAGACG
GTGGACAAGCTGTTGAAAGGCTACGACATTCGCCTAAGACCCGACTTCGGGGGTCCCCCG
GTCTGCGTGGGGATGAACATCGACATCGCCAGCATCGACATGGTTTCCGAAGTCAACATG
GATTATACCTTAACCATGTATTTTCAACAATATTGGAGAGATAAAAGGCTCGCCTATTCT
GGGATCCCTCTCAACCTCACGCTTGACAATCGAGTGGCTGACCAGCTATGGGTGCCCGAC
ACATATTTCTTAAATGACAAAAAGTCATTTGTGCATGGAGTGACAGTGAAAAACCGCATG
ATCCGTCTTCACCCTGATGGGACAGTGCTGTATGGGCTCAGAATCACCACGACAGCAGCA
TGCATGATGGACCTCAGGAGATACCCCCTGGACGAGCAGAACTGCACTCTGGAAATTGAA
AGCTATGGCTACACCACGGATGACATTGAGTTTTACTGGCGAGGCGGGGACAAGGCTGTT
ACCGGAGTGGAAAGGATTGAGCTCCCGCAGTTCTCCATCGTGGAGCACCGTCTGGTCTCG
AGGAATGTTGTCTTCGCCACAGGTGCCTATCCTCGACTGTCACTGAGCTTTCGGTTGAAG
AGGAACATTGGATACTTCATTCTTCAGACTTATATGCCCTCTATACTGATAACGATTCTG
TCGTGGGTGTCCTTCTGGATCAATTATGATGCATCTGCTGCTAGAGTTGCCCTCGGGATC
ACAACTGTGCTGACAATGACAACCATCAACACCCACCTTCGGGAGACCTTGCCCAAAATC
CCCTATGTCAAAGCCATTGACATGTACCTTATGGGCTGCTTCGTCTTTGTGTTCCTGGCC
CTTCTGGAGTATGCCTTTGTCAACTACATTTTCTTTGGAAGAGGCCCTCAAAGGCAGAAG
AAGCTTGCAGAAAAGACAGCCAAGGCAAAGAATGACCGTTCAAAGAGCGAAAGCAACCGG
GTGGATGCTCATGGAAATATTCTGTTGACATCGCTGGAAGTTCACAATGAAATGAATGAG
GTCTCAGGCGGCATTGGCGATACCAGGAATTCAGCAATATCCTTTGACAACTCAGGAATC
CAGTACAGGAAACAGAGCATGCCTCGAGAAGGGCATGGGCGATTCCTGGGGGACAGAAGC
CTCCCGCACAAGAAGACCCATCTACGGAGGAGGTCTTCACAGCTCAAAATTAAAATACCT
GATCTAACCGATGTGAATGCCATAGACAGATGGTCCAGGATCGTGTTTCCATTCACTTTT
TCTCTTTTCAACTTAGTTTACTGGCTGTACTATGTTAACTGA
Target 3 GenBank Gene ID Not Available
Target 3 GeneCard ID GABRB3 Link Image
Target 3 GenAtlas ID GABRB3 Link Image
Target 3 HGNC ID HGNC:4083 Link Image
Target 3 Chromosome Location Chromosome:15
Target 3 Locus 15q11.2-q12
Target 3 SNPs SNPJam Report Link Image
Target 3 Toxin References
  • S912 - Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 3 General References 1664410; 15489334; 8382702; 1714232; 12189488; 18514161
Target 4 [top]
Target 4 ID 133
Target 4 Name Gamma-aminobutyric acid receptor subunit alpha-5
Target 4 Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Target 4 Description 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
Target 4 Synonyms
  1. GABA(A) receptor subunit alpha-5
Target 4 Gene Name GABRA5
Target 4 Protein Sequence >Gamma-aminobutyric acid receptor subunit alpha-5 
MDNGMFSGFIMIKNLLLFCISMNLSSHFGFSQMPTSSVKDETNDNITIFTRILDGLLDGY
DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL
NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF
PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS
TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM
TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA
KIKKKREVILNKSTNAFTTGKMSHPPNIPKEQTPAGTSNTTSVSVKPSEEKTSESKKTYN
SISKIDKMSRIVFPVLFGTFNLVYWATYLNREPVIKGAASPK
Target 4 Number of Residues 462
Target 4 Molecular Weight 52145.6
Target 4 Theoretical pI 9.56
Target 4 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
gamma-aminobutyric acid signaling pathway
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 4 General Function Involved in chloride channel activity
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Signals
  • 1-31
Target 4 Transmembrane Regions
  • 260-281
  • 286-307
  • 319-341
  • 428-449
Target 4 Essentiality Non Essential
Target 4 Domain Function PF02931:Neur_chan_LBD PF02932:Neur_chan_memb
Target 4 GenBank ID Protein Not Available
Target 4 UniProtKB ID P31644 Link Image
Target 4 Cellular Location Cell junction, synapse, postsynaptic cell membrane
Target 4 Gene Sequence >1389 bp 
ATGGACAATGGAATGTTCTCTGGTTTTATCATGATCAAAAACCTCCTTCTCTTTTGTATT
TCCATGAACTTATCCAGTCACTTTGGCTTTTCACAGATGCCAACCAGTTCAGTGAAAGAT
GAGACCAATGACAACATCACGATATTTACCAGGATCTTGGATGGGCTCTTGGATGGCTAC
GACAACAGACTTCGGCCCGGGCTGGGAGAGCGCATCACTCAGGTGAGGACCGACATCTAC
GTCACCAGCTTCGGCCCGGTGTCCGACACGGAAATGGAGTACACCATAGACGTGTTTTTC
CGACAAAGCTGGAAAGATGAAAGGCTTCGGTTTAAGGGGCCCATGCAGCGCCTCCCTCTC
AACAACCTCCTTGCCAGCAAGATCTGGACCCCAGACACGTTCTTCCACAACGGGAAGAAG
TCCATCGCTCACAACATGACCACGCCCAACAAGCTGCTGCGGCTGGAGGACGACGGCACC
CTGCTCTACACCATGCGCTTGACCATCTCTGCAGAGTGCCCCATGCAGCTTGAGGACTTC
CCGATGGATGCGCACGCTTGCCCTCTGAAATTTGGCAGCTATGCGTACCCTAATTCTGAA
GTCGTTTACGTCTGGACCAACGGCTCCACCAAGTCGGTGGTGGTGGCGGAAGATGGCTCC
AGACTGAACCAGTACCACCTGATGGGGCAGACGGTGGGCACTGAGAACATCAGCACCAGC
ACAGGCGAATACACAATCATGACAGCTCACTTCCACCTGAAAAGGAAGATTGGCTACTTT
GTCATCCAGACCTACCTTCCCTGCATAATGACCGTGATCTTATCACAGGTGTCCTTTTGG
CTGAACCGGGAATCAGTCCCAGCCAGGACAGTTTTTGGGGTCACCACGGTGCTGACCATG
ACGACCCTCAGCATCAGCGCCAGGAACTCTCTGCCCAAAGTGGCCTACGCCACCGCCATG
GACTGGTTCATAGCTGTGTGCTATGCCTTCGTCTTCTCGGCGCTGATAGAGTTTGCCACG
GTCAATTACTTTACCAAGAGAGGCTGGGCCTGGGATGGCAAAAAAGCCTTGGAAGCAGCC
AAGATCAAGAAAAAGCGTGAAGTCATACTAAATAAGTCAACAAACGCTTTTACAACTGGG
AAGATGTCTCACCCCCCAAACATTCCGAAGGAACAGACCCCAGCAGGGACGTCGAATACA
ACCTCAGTCTCAGTAAAACCCTCTGAAGAGAAGACTTCTGAAAGCAAAAAGACTTACAAC
AGTATCAGCAAAATTGACAAAATGTCCCGAATCGTATTCCCAGTCTTGTTCGGCACTTTC
AACTTAGTTTACTGGGCAACGTATTTGAATAGGGAGCCGGTGATAAAAGGAGCCGCCTCT
CCAAAATAA
Target 4 GenBank Gene ID Not Available
Target 4 GeneCard ID GABRA5 Link Image
Target 4 GenAtlas ID GABRA5 Link Image
Target 4 HGNC ID HGNC:4079 Link Image
Target 4 Chromosome Location Chromosome:15
Target 4 Locus 15q11.2-q12
Target 4 SNPs SNPJam Report Link Image
Target 4 Toxin References
  • S912 - Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 4 General References 8388764; 1321750; 14702039; 15489334; 9205108; 17370265
Target 5 [top]
Target 5 ID 153
Target 5 Name Gamma-aminobutyric acid receptor subunit alpha-3
Target 5 Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Target 5 Description 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
Target 5 Synonyms
  1. GABA(A) receptor subunit alpha-3
Target 5 Gene Name GABRA3
Target 5 Protein Sequence >Gamma-aminobutyric acid receptor subunit alpha-3 
MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDS
TDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQ
TWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLL
YTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRL
NQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLN
RESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVN
YFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGA
APSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVN
RESAIKGMIRKQ
Target 5 Number of Residues 492
Target 5 Molecular Weight 55164.1
Target 5 Theoretical pI 8.93
Target 5 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
gamma-aminobutyric acid signaling pathway
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 5 General Function Involved in benzodiazepine receptor activity
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Signals
  • 1-28
Target 5 Transmembrane Regions
  • 277-298
  • 304-325
  • 338-359
  • 458-479
Target 5 Essentiality Non Essential
Target 5 Domain Function PF02931:Neur_chan_LBD PF02932:Neur_chan_memb
Target 5 GenBank ID Protein Not Available
Target 5 UniProtKB ID P34903 Link Image
Target 5 Cellular Location Cell junction, synapse, postsynaptic cell membrane
Target 5 Gene Sequence >1479 bp 
ATGATAATCACACAAACAAGTCACTGTTACATGACCAGCCTTGGGATTCTTTTCCTGATT
AATATTCTCCCTGGAACCACTGGTCAAGGGGAATCAAGACGACAAGAACCCGGGGACTTT
GTGAAGCAGGACATTGGCGGGCTGTCTCCTAAGCATGCCCCAGATATTCCTGATGACAGC
ACTGACAACATCACTATCTTCACCAGAATCTTGGATCGTCTTCTGGACGGCTATGACAAC
CGGCTGCGACCTGGGCTTGGAGATGCAGTGACTGAAGTGAAGACTGACATCTACGTGACC
AGTTTTGGCCCTGTGTCAGACACTGACATGGAGTACACTATTGATGTATTTTTTCGGCAG
ACATGGCATGATGAAAGACTGAAATTTGATGGCCCCATGAAGATCCTTCCACTGAACAAT
CTCCTGGCTAGTAAGATCTGGACACCGGACACCTTCTTCCACAATGGCAAGAAATCAGTG
GCTCATAACATGACCACGCCCAACAAGCTGCTCAGATTGGTGGACAACGGAACCCTCCTC
TATACAATGAGGTTAACAATTCATGCTGAGTGTCCCATGCATTTGGAAGATTTTCCCATG
GATGTGCATGCCTGCCCACTGAAGTTTGGAAGCTATGCCTATACAACAGCTGAAGTGGTT
TATTCTTGGACTCTCGGAAAGAACAAATCCGTGGAAGTGGCACAGGATGGTTCTCGCTTG
AACCAGTATGACCTTTTGGGCCATGTTGTTGGGACAGAGATAATCCGGTCTAGTACAGGA
GAATATGTCGTCATGACAACCCACTTCCATCTCAAGCGAAAAATTGGCTACTTTGTGATC
CAGACCTACTTGCCATGTATCATGACTGTCATTCTGTCACAAGTGTCGTTCTGGCTCAAC
AGAGAGTCTGTTCCTGCCCGTACAGTCTTTGGTGTCACCACTGTGCTTACCATGACCACC
TTGAGTATCAGTGCCAGAAATTCCTTACCTAAAGTGGCATATGCGACGGCCATGGACTGG
TTCATAGCCGTCTGTTATGCCTTTGTATTTTCTGCACTGATTGAATTTGCCACTGTCAAC
TATTTCACCAAGCGGAGTTGGGCTTGGGAAGGCAAGAAGGTGCCAGAGGCCCTGGAGATG
AAGAAGAAAACACCAGCAGCCCCAGCAAAGAAAACCAGCACTACCTTCAACATCGTGGGG
ACCACCTATCCCATCAACCTGGCCAAGGACACTGAATTTTCCACCATCTCCAAGGGCGCT
GCTCCCAGTGCCTCCTCAACCCCAACAATCATTGCTTCACCCAAGGCCACCTACGTGCAG
GACAGCCCGACTGAGACCAAGACCTACAACAGTGTCAGCAAGGTTGACAAAATTTCCCGC
ATCATCTTTCCTGTGCTCTTTGCCATATTCAATCTGGTCTATTGGGCCACATATGTCAAC
CGGGAGTCAGCTATCAAGGGCATGATCCGCAAACAGTAG
Target 5 GenBank Gene ID Not Available
Target 5 GeneCard ID GABRA3 Link Image
Target 5 GenAtlas ID GABRA3 Link Image
Target 5 HGNC ID HGNC:4077 Link Image
Target 5 Chromosome Location Not Available
Target 5 Locus Xq28
Target 5 SNPs SNPJam Report Link Image
Target 5 Toxin References
  • S912 - Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 5 General References 8391122; 10602120; 15489334
Target 6 [top]
Target 6 ID 115
Target 6 Name Gamma-aminobutyric acid receptor subunit alpha-2
Target 6 Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Target 6 Description 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
Target 6 Synonyms
  1. GABA(A) receptor subunit alpha-2
Target 6 Gene Name GABRA2
Target 6 Protein Sequence >Gamma-aminobutyric acid receptor subunit alpha-2 
MKTKLNIYNMQFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPG
LGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSC
PLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVM
TAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKASV
MIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRM
SRIVFPVLFGTFNLVYWATYLNREPVLGVSP
Target 6 Number of Residues 451
Target 6 Molecular Weight 51325.9
Target 6 Theoretical pI 9.50
Target 6 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
gamma-aminobutyric acid signaling pathway
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 6 General Function Involved in benzodiazepine receptor activity
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Signals
  • 1-28
Target 6 Transmembrane Regions
  • 252-273
  • 279-300
  • 313-334
  • 420-441
Target 6 Essentiality Non Essential
Target 6 Domain Function PF02931:Neur_chan_LBD PF02932:Neur_chan_memb
Target 6 GenBank ID Protein Not Available
Target 6 UniProtKB ID P47869 Link Image
Target 6 Cellular Location Cell junction, synapse, postsynaptic cell membrane
Target 6 Gene Sequence >1356 bp 
ATGAAGACAAAATTGAACATCTACAACATCGAGTTCCTGCTTTTTGTTTTCTTGGTGTGG
GACCCTGCCAGGTTGGTGCTGGCTAACATCCAAGAAGATGAGGCTAAAAATAACATTACC
ATCTTTACGAGAATTCTTGACAGACTTCTGGATGGTTACGATAATCGGCTTAGACCAGGA
CTGGGAGACAGTATTACTGAAGTCTTCACTAACATCTACGTGACCAGTTTTGGCCCTGTC
TCAGATACAGATATGGAATATACAATTGATGTTTTCTTTCGACAAAAATGGAAAGATGAA
CGTTTAAAATTTAAAGGTCCTATGAATATCCTTCGACTAAACAATTTAATGGCTAGCAAA
ATCTGGACTCCAGATACCTTTTTTCACAATGGGAAGAAATCAGTAGCTCATAATATGACA
ATGCCAAATAAGTTGCTTCGAATTCAGGATGATGGGACTCTGCTGTATACCATGAGGCTT
ACAGTTCAAGCTGAATGCCCAATGCACTTGGAGGATTTCCCAATGGATGCTCATTCATGT
CCTCTGAAATTTGGCAGCTATGCATATACAACTTCAGAGGTCACTTATATTTGGACTTAC
AATGCATCTGATTCAGTACAGGTTGCTCCTGATGGCTCTAGGTTAAATCAATATGACCTG
CTGGGCCAATCAATCGGAAAGGAGACAATTAAATCCAGTACAGGTGAATATACTGTAATG
ACAGCTCATTTCCACCTGAAAAGAAAAATTGGGTATTTTGTGATTCAAACCTATCTGCCT
TGCATCATGACTGTCATTCTCTCCCAAGTTTCATTCTGGCTTAACAGAGAATCTGTGCCT
GCAAGAACTGTGTTTGGAGTAACAACTGTCCTAACAATGACAACTCTAAGCATCAGTGCT
CGGAATTCTCTCCCCAAAGTGGCTTATGCAACTGCCATGGACTGGTTTATTGCTGTTTGT
TATGCATTTGTGTTCTCTGCCCTAATTGAATTTGCAACTGTTAATTACTTCACCAAAAGA
GGATGGACTTGGGATGGGAAGAGTGTAGTAAATGACAAGAAAAAAGAAAAGGCTTCCGTT
ATGATACAGAACAACGCTTATGCAGTGGCTGTTGCCAATTATGCCCCGAATCTTTCAAAA
GATCCAGTTCTCTCCACCATCTCCAAGAGTGCAACCACGCCAGAACCCAACAAGAAGCCA
GAAAACAAGCCAGCTGAAGCAAAGAAAACTTTCAACAGTGTTAGCAAAATTGACAGAATG
TCCAGAATAGTTTTTCCAGTTTTGTTTGGTACCTTTAATTTAGTTTACTGGGCTACATAT
TTAAACAGAGAACCTGTATTAGGGGTCAGTCCTTGA
Target 6 GenBank Gene ID Not Available
Target 6 GeneCard ID GABRA2 Link Image
Target 6 GenAtlas ID GABRA2 Link Image
Target 6 HGNC ID HGNC:4076 Link Image
Target 6 Chromosome Location Not Available
Target 6 Locus 4p12
Target 6 SNPs SNPJam Report Link Image
Target 6 Toxin References
  • S912 - Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 6 General References 8391122; 15024690
Target 7 [top]
Target 7 ID 111
Target 7 Name Gamma-aminobutyric acid receptor subunit beta-2
Target 7 Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Target 7 Description 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
Target 7 Synonyms
  1. GABA(A) receptor subunit beta-2
Target 7 Gene Name GABRB2
Target 7 Protein Sequence >Gamma-aminobutyric acid receptor subunit beta-2 
MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKM
DPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALER
HVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
Target 7 Number of Residues 474
Target 7 Molecular Weight 54605.9
Target 7 Theoretical pI 9.66
Target 7 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 7 General Function Involved in chloride channel activity
Target 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Signals
  • 1-25
Target 7 Transmembrane Regions
  • 245-266
  • 270-292
  • 304-326
  • 452-473
Target 7 Essentiality Non Essential
Target 7 Domain Function PF02931:Neur_chan_LBD PF02932:Neur_chan_memb
Target 7 GenBank ID Protein Not Available
Target 7 UniProtKB ID P47870 Link Image
Target 7 Cellular Location Cell junction, synapse, postsynaptic cell membrane
Target 7 Gene Sequence >1425 bp 
ATGTGGAGAGTGCGGAAAAGGGGCTACTTTGGGATTTGGTCCTTCCCCTTAATAATCGCC
GCTGTCTGTGCGCAGAGTGTCAATGACCCTAGTAATATGTCGCTGGTTAAAGAGACGGTG
GATAGACTCCTGAAAGGCTATGACATTCGTCTGAGACCAGATTTTGGAGGTCCCCCCGTG
GCTGTGGGGATGAACATTGACATTGCCAGCATCGATATGGTTTCTGAAGTCAATATGGAT
TATACCTTGACAATGTACTTTCAACAAGCCTGGAGAGATAAGAGGCTGTCCTATAATGTA
ATACCTTTAAACTTGACTCTGGACAACAGAGTGGCAGACCAGCTCTGGGTGCCTGATACC
TATTTCCTGAACGATAAGAAGTCATTTGTGCACGGAGTGACTGTTAAGAACCGCATGATT
CGCCTGCATCCTGATGGCACCGTCCTTTATGGACTCAGAATCACAACCACAGCTGCCTGC
ATGATGGACCTAAGGAGGTACCCACTGGATGAACAAAACTGCACCTTGGAAATTGAGAGC
TATGGATACACAACTGATGACATTGAGTTTTACTGGCGTGGCGATGATAATGCAGTAACA
GGAGTAACGAAAATTGAACTTCCACAGTTCTCTATTGTAGATTACAAACTTATCACCAAG
AAGGTTGTTTTTTCCACAGGTTCCTATCCCAGGTTATCCCTCAGCTTTAAGCTTAAGAGA
AACATTGGCTACTTTATCCTGCAAACATACATGCCTTCCATCCTGATTACCATCCTCTCC
TGGGTCTCCTTCTGGATTAATTACGATGCTTCAGCTGCAAGGGTGGCATTAGGAATCACA
ACTGTCCTCACAATGACCACAATCAACACCCACCTCCGGGAAACTCTCCCTAAAATCCCC
TATGTGAAGGCCATTGACATGTACCTGATGGGGTGCTTTGTCTTCGTTTTCATGGCCCTT
CTGGAATATGCCCTAGTCAACTACATCTTCTTTGGGAGGGGGCCCCAACGCCAAAAGAAA
GCAGCTGAGAAGGCTGCCAGTGCCAACAATGAGAAGATGCGCCTGGATGTCAACAAGATG
GACCCCCATGAGAACATCTTACTGAGCACTCTCGAGATAAAAAATGAAATGGCCACATCT
GAGGCTGTGATGGGACTTGGAGACCCCAGAAGCACAATGCTAGCCTATGATGCCTCCAGC
ATCCAGTATCGGAAAGCTGGGTTGCCCAGGCATAGTTTTGGCCGAAATGCTCTGGAACGA
CATGTGGCGCAAAAGAAAAGTCGCCTGAGGAGACGCGCCTCCCAACTGAAAATCACCATC
CCTGACTTGACTGATGTGAATGCCATAGATCGGTGGTCCCGCATATTCTTCCCAGTGGTT
TTTTCCTTCTTCAACATCGTCTATTGGCTTTATTATGTGAACTAA
Target 7 GenBank Gene ID Not Available
Target 7 GeneCard ID GABRB2 Link Image
Target 7 GenAtlas ID GABRB2 Link Image
Target 7 HGNC ID HGNC:4082 Link Image
Target 7 Chromosome Location Not Available
Target 7 Locus 5q34
Target 7 SNPs SNPJam Report Link Image
Target 7 Toxin References
  • S912 - Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 7 General References 8264558; 7707873; 15489334; 17370265
Target 8 [top]
Target 8 ID 246
Target 8 Name Gamma-aminobutyric acid receptor subunit alpha-4
Target 8 Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Target 8 Description 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
Target 8 Synonyms
  1. GABA(A) receptor subunit alpha-4
Target 8 Gene Name GABRA4
Target 8 Protein Sequence >Gamma-aminobutyric acid receptor subunit alpha-4 
MVSAKKVPAIALSAGVSFALLRFLCLAVCLNESPGQNQKEEKLCTENFTRILDSLLDGYD
NRLRPGFGGPVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWIDKRLKYDGPIEILRLN
NMMVTKVWTPDTFFRNGKKSVSHNMTAPNKLFRIMRNGTILYTMRLTISAECPMRLVDFP
MDGHACPLKFGSYAYPKSEMIYTWTKGPEKSVEVPKESSSLVQYDLIGQTVSSETIKSIT
GEYIVMTVYFHLRRKMGYFMIQTYIPCIMTVILSQVSFWINKESVPARTVFGITTVLTMT
TLSISARHSLPKVSYATAMDWFIAVCFAFVFSALIEFAAVNYFTNIQMEKAKRKTSKPPQ
EVPAAPVQREKHPEAPLQNTNANLNMRKRTNALVHSESDVGNRTEVGNHSSKSSTVVQES
SKGTPRSYLASSPNPFSRANAAETISAARALPSASPTSIRTGYMPRKASVGSASTRHVFG
SRLQRIKTTVNTIGATGKLSATPPPSAPPPSGSGTSKIDKYARILFPVTFGAFNMVYWVV
YLSKDTMEKSESLM
Target 8 Number of Residues 554
Target 8 Molecular Weight 61622.6
Target 8 Theoretical pI 10.02
Target 8 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
gamma-aminobutyric acid signaling pathway
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 8 General Function Involved in benzodiazepine receptor activity
Target 8 Pathways Not Available
Target 8 Reactions Not Available
Target 8 Signals
  • 1-35
Target 8 Transmembrane Regions
  • 259-280
  • 285-306
  • 318-340
  • 524-543
Target 8 Essentiality Non Essential
Target 8 Domain Function PF02931:Neur_chan_LBD PF02932:Neur_chan_memb
Target 8 GenBank ID Protein Not Available
Target 8 UniProtKB ID P48169 Link Image
Target 8 Cellular Location Cell junction, synapse, postsynaptic cell membrane
Target 8 Gene Sequence Not Available
Target 8 GenBank Gene ID Not Available
Target 8 GeneCard ID GABRA4 Link Image
Target 8 GenAtlas ID GABRA4 Link Image
Target 8 HGNC ID HGNC:4078 Link Image
Target 8 Chromosome Location Not Available
Target 8 Locus 4p12
Target 8 SNPs SNPJam Report Link Image
Target 8 Toxin References
  • S912 - Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 8 General References 8719416; 14702039; 15815621; 15489334; 7607683; 17693683; 16959974
Target 9 [top]
Target 9 ID 257
Target 9 Name Gamma-aminobutyric acid receptor subunit alpha-6
Target 9 Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Target 9 Description 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
Target 9 Synonyms
  1. GABA(A) receptor subunit alpha-6
Target 9 Gene Name GABRA6
Target 9 Protein Sequence >Gamma-aminobutyric acid receptor subunit alpha-6 
MASSLPWLCIILWLENALGKLEVEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKT
DIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFGGPTEILSLNNLMVSKIWTPDTFFRN
GKKSIAHNMTTPNKLFRIMQNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYP
KSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKM
GYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYA
TAMDWFIAVCFAFVFSALIEFAAVNYFTNLQTQKAKRKAQFAAPPTVTISKATEPLEAEI
VLHPDSKYHLKKRITSLSLPIVSSSEANKVLTRAPILQSTPVTPPPLSPAFGGTSKIDQY
SRILFPVAFAGFNLVYWVVYLSKDTMEVSSSVE
Target 9 Number of Residues 453
Target 9 Molecular Weight 51023.7
Target 9 Theoretical pI 8.40
Target 9 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
gamma-aminobutyric acid signaling pathway
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 9 General Function Involved in benzodiazepine receptor activity
Target 9 Pathways Not Available
Target 9 Reactions Not Available
Target 9 Signals
  • 1-19
Target 9 Transmembrane Regions
  • 243-264
  • 269-290
  • 301-324
  • 420-441
Target 9 Essentiality Non Essential
Target 9 Domain Function PF02931:Neur_chan_LBD PF02932:Neur_chan_memb
Target 9 GenBank ID Protein Not Available
Target 9 UniProtKB ID Q16445 Link Image
Target 9 Cellular Location Cell junction, synapse, postsynaptic cell membrane
Target 9 Gene Sequence >1362 bp 
ATGGCGTCATCTCTGCCCTGGCTGTGCATTATTCTGTGGCTAGAAAATGCCCTAGGGAAA
CTCGAAGTTGAAGGCAACTTCTACTCAGAAAACGTCAGTCGGATCCTGGACAACTTGCTT
GAAGGCTATGACAATCGGCTGCGGCCGGGATTTGGAGGTGCTGTCACTGAAGTCAAAACA
GACATTTATGTGACCAGTTTTGGGCCCGTGTCAGATGTGGAGATGGAGTATACGATGGAT
GTTTTTTTTCGCCAGACCTGGACTGATGAGAGGTTGAAGTTTGGGGGGCCAACTGAGATT
CTGAGTCTGAATAATTTGATGGTCAGTAAAATCTGGACGCCTGACACCTTTTTCAGAAAT
GGTAAAAAGTCCATTGCTCACAACATGACAACTCCTAATAAACTCTTCAGAATAATGCAG
AATGGAACCATTTTATACACCATGAGGCTTACCATCAATGCTGACTGTCCCATGAGGCTG
GTTAACTTTCCTATGGATGGGCATGCTTGTCCACTCAAGTTTGGGAGCTATGCTTATCCC
AAAAGTGAAATCATATATACGTGGAAAAAAGGACCACTTTACTCAGTAGAAGTCCCAGAA
GAATCTTCAAGCCTTCTCCAGTATGATCTGATTGGACAAACAGTATCTAGTGAGACAATT
AAATCTAACACAGGTGAATACGTTATAATGACAGTTTACTTCCACTTGCAAAGGAAGATG
GGCTACTTCATGATACAGATATACACTCCTTGCATTATGACAGTCATTCTTTCCCAGGTG
TCTTTCTGGATTAATAAGGAGTCCGTCCCAGCAAGAACTGTTTTTGGGATCACCACTGTT
TTAACTATGACCACTTTGAGCATCAGTGCCCGGCACTCTTTGCCAAAAGTGTCATATGCC
ACTGCCATGGATTGGTTCATAGCTGTTTGCTTTGCATTCGTCTTCTCTGCTCTTATCGAG
TTCGCAGCTGTCAACTACTTTACCAATCTTCAGACACAGAAGGCGAAAAGGAAGGCACAG
TTTGCAGCCCCACCCACAGTGACAATATCAAAAGCTACTGAACCTTTGGAAGCTGAGATT
GTTTTGCATCCTGACTCCAAATATCATCTGAAGAAAAGGATCACTTCTCTGTCTTTGCCA
ATAGTTTCATCTTCCGAGGCCAATAAAGTGCTCACGAGAGCGCCCATCTTACAATCAACA
CCTGTCACACCCCCACCACTCCCGCCAGCCTTTGGAGGCACCAGTAAAATAGACCAGTAT
TCTCGAATTCTCTTCCCAGTTGCATTTGCAGGATTCAACCTTGTGTACTGGGTAGTTTAT
CTTTCCAAAGATACAATGGAAGTGAGTAGCAGTGTTGAATAG
Target 9 GenBank Gene ID Not Available
Target 9 GeneCard ID GABRA6 Link Image
Target 9 GenAtlas ID GABRA6 Link Image
Target 9 HGNC ID HGNC:4080 Link Image
Target 9 Chromosome Location Not Available
Target 9 Locus 5q34
Target 9 SNPs SNPJam Report Link Image
Target 9 Toxin References
  • S912 - Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  • S911 - Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Target 9 General References 8632757; 15489334; 16959974

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government.