| Version |
1.0 |
| Creation Date |
2009-07-21 20:27:45 |
| Update Date |
2010-05-18 21:00:46 |
| Accession Number |
T3D2903 |
| Name |
Diazepam |
| Compound Type |
- Adjuvant, Anesthesia
- Anesthetic, Intravenous
- Anti-Anxiety Agent
- Anticonvulsant
- Antiemetic
- Drug
- GABA Modulator
- Hypnotic and Sedative
- Muscle Relaxant, Central
|
| Description |
A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of gamma-aminobutyric acid activity. It is used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome. (From Martindale, The Extra Pharmacopoeia, 30th ed, p589) |
| Synonyms |
- DAP
- Methyldiazepinone
|
| Chemical IUPAC Name |
7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one |
| Chemical Formula |
C16H13ClN2O |
| Chemical Structure |
 |
| CAS Registry Number |
439-14-5 |
| InChI Identifier |
InChI=1S/C16H13ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3 |
| InChI Key |
InChIKey=AAOVKJBEBIDNHE-UHFFFAOYSA-N |
| PubChem Compound ID |
3016  |
| KEGG ID |
C06948  |
| UniProt ID |
Not Available |
| OMIM ID |
Not Available |
| ChEBI ID |
4494  |
| BioCyc ID |
Not Available |
| SuperToxic ID |
Not Available |
| CTD ID |
Not Available |
| Stitch ID |
Diazepam  |
| DrugBank ID |
DB00829  |
| PDB ID |
Not Available |
| ACToR ID |
Not Available |
| Wikipedia Link |
http://en.wikipedia.org/wiki/Diazepam  |
| Monoisotopic Mass |
284.071641 |
| MOL File |
Show |
| PDB File |
Show |
| SDF File |
Show |
| SMILES |
CN1C2=CC=C(Cl)C=C2C(=NCC1=O)C1=CC=CC=C1 |
| Appearance |
Not Available |
| Melting Point |
125-126oC |
| Solubility |
Slightly soluble (50 mg/L) |
| Predicted LogP |
3.0761 |
| Route of Exposure |
Parenteral (intramuscular); oral; enteral(rectal). |
| Mechanism of Action |
Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. |
| Metabolism |
Hepatic via the Cytochrome P450 enzyme system. The main active metabolite is desmethyldiazepam, in addition to minor active metabolites including temazepam and oxazepam. |
| Toxicity Values |
LD50: 1200 mg/kg (oral, rat) (W553)
LD50: 1000 mg/kg (oral, dog) (W553)
LD50: 700 mg/kg (oral, mice) (W553) |
| Lethal Dose |
Not Available |
| Carcinogenicity (IARC Classification) |
Not Available |
| Uses/Sources |
Diazepam is used to treat a wide range of conditions and has been one of the most frequently prescribed medications in the world for the past 40 years. [Wikipedia] |
| Minimum Risk Level |
Not Available |
| Health Effects |
They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive. May cause a potentially dangerous rash that may develop into Stevens Johnson syndrome, an extremely rare but potentially fatal skin disease. |
| Symptoms |
Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored. |
| Treatment |
General supportive measures should be employed, along with intravenous fluids, and an adequate airway maintained. Hypotension may be combated by the use of norepinephrine or metaraminol. Dialysis is of limited value. Flumazenil, a specific benzodiazepine receptor antagonist, is indicated for the complete or partial reversal of the sedative effects of benzodiazepines and may be used in situations when an overdose with a benzodiazepine is known or suspected. (V650) |
| General References |
- W553 - IPCS Inchem monograph for Diazepam []
- T350 - Mant A, Whicker SD, McManus P, Birkett DJ, Edmonds D, Dumbrell D: Benzodiazepine utilisation in Australia: report from a new pharmacoepidemiological database. Aust J Public Health. 1993 Dec;17(4):345-9. [PubMed
]
- U448 - McLean MJ, Macdonald RL: Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture. J Pharmacol Exp Ther. 1988 Feb;244(2):789-95. [PubMed
]
- T839 - Oishi R, Nishibori M, Itoh Y, Saeki K: Diazepam-induced decrease in histamine turnover in mouse brain. Eur J Pharmacol. 1986 May 27;124(3):337-42. [PubMed
]
- U447 - Usami N, Yamamoto T, Shintani S, Ishikura S, Higaki Y, Katagiri Y, Hara A: Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol Pharm Bull. 2002 Apr;25(4):441-5. [PubMed
]
- U446 - Drugs.com
- T840 - Earley JV, Fryer RI, Ning RY: Quinazolines and 1,4-benzodiazepines. LXXXIX: Haptens useful in benzodiazepine immunoassay development. J Pharm Sci. 1979 Jul;68(7):845-50. [PubMed
]
|
| Targets |
- Translocator protein
- Gamma-aminobutyric acid receptor subunit alpha-1
- Gamma-aminobutyric acid receptor subunit alpha-2
- Gamma-aminobutyric acid receptor subunit alpha-3
|
|
Target 1
[top]
|
| Target 1 ID |
1151 |
| Target 1 Name |
Translocator protein |
| Target 1 Mechanism of Action |
Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. |
| Target 1 Description |
Responsible for the manifestation of peripheral-type benzodiazepine recognition sites and is most likely to comprise binding domains for benzodiazepines and isoquinoline carboxamides. May play a role in the transport of porphyrins and heme. Plays a role in the transport of cholesterol across mitochondrial membranes in steroidogenic cells (By similarity) |
| Target 1 Synonyms |
- Peripheral-type benzodiazepine receptor; PBR; PKBS; Mitochondrial benzodiazepine receptor
|
| Target 1 Gene Name |
TSPO |
| Target 1 Protein Sequence |
>Translocator protein
MAPPWVPAMGFTLAPSLGCFVGSRFVHGEGLRWYAGLQKPSWHPPHWVLGPVWGTLYSAM
GYGSYLVWKELGGFTEKAVVPLGLYTGQLALNWAWPPIFFGARQMGWALVDLLLVSGAAA
ATTVAWYQVSPLAARLLYPYLAWLAFATTLNYCVWRDNHGWHGGRRLPE
|
| Target 1 Number of Residues |
169 |
| Target 1 Molecular Weight |
18778.7 |
| Target 1 Theoretical pI |
9.33 |
| Target 1 GO Classification |
|
Function
|
| Not Available |
|
Process
|
| Not Available |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 1 General Function |
Signal transduction mechanisms |
| Target 1 Pathways |
Not Available |
| Target 1 Reactions |
Not Available |
| Target 1 Signals |
|
| Target 1 Transmembrane Regions |
- 6-26
- 47-67
- 80-100
- 106-126
- 135-155
|
| Target 1 Essentiality |
Non Essential |
| Target 1 Domain Function |
PF03073:TspO_MBR |
| Target 1 GenBank ID Protein |
Not Available |
| Target 1 UniProtKB ID |
P30536  |
| Target 1 Cellular Location |
Mitochondrion membrane |
| Target 1 Gene Sequence |
>510 bp
CCCCTGAACAGCAGCTGCAGCAGCCATGGCCCCGCCCTGGGTGCCCGCCATGGGCTTCAC
GCTGGCGCCCAGCCTGGGGTGCTTCGTGGGCTCCCGCTTTGTCCACGGCGAGGGTCTCCG
CTGGTACGCCGGCCTGCAGAAGCCCTCGTGGCACCCGCCCCACTGGGTGCTGGGCCCTGT
CTGGGGCACGCTCTACTCAGCCATGGGGTACGGCTCCTACCTGGTCTGGAAAGAGCTGGG
AGGCTTCACAGAGAAGGCTGTGGTTCCCCTGGGCCTCTACACTGGGCAGCTGGCCCTGAA
CTGGGCATGGCCCCCCATCTTCTTTGGTGCCCGACAAATGGGCTGGGCCTTGGTGGATCT
CCTGCTGGTCAGTGGGGCGGCGGCNGCCACTACCGTGGCCTGGTACCAGGTGAGCCCGCT
GGCCGCCCGCCTGCTCTACCCCTACCTGGCCTGGCTGGCCTTCGCGACCACACTCAACTA
CTGCGTATGGCGGGACAACCATGGCTGGCA
|
| Target 1 GenBank Gene ID |
Not Available |
| Target 1 GeneCard ID |
TSPO  |
| Target 1 GenAtlas ID |
TSPO  |
| Target 1 HGNC ID |
HGNC:1158  |
| Target 1 Chromosome Location |
Chromosome:22 |
| Target 1 Locus |
22q13.31 |
| Target 1 SNPs |
SNPJam Report  |
| Target 1 Toxin References |
- S918 - Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
- U451 - Chen Z, Kong X: Study of Candida albicans vaginitis model in Kunming mice. J Huazhong Univ Sci Technolog Med Sci. 2007 Jun;27(3):307-10. [PubMed
]
- U449 - Falchi AM, Battetta B, Sanna F, Piludu M, Sogos V, Serra M, Melis M, Putzolu M, Diaz G: Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands. Neuropharmacology. 2007 Aug;53(2):318-29. Epub 2007 Jun 2. [PubMed
]
- U450 - Han WQ, Wang LJ, Sun XY, Li JS: Treatment of bactericide wastewater by combined process chemical coagulation, electrochemical oxidation and membrane bioreactor. J Hazard Mater. 2007 Jun 7;. [PubMed
]
|
| Target 1 General References |
1847678; 7721091; 16189298; 15461802; 10591208; 15489334; 9915832; 16822554 |
|
Target 2
[top]
|
| Target 2 ID |
36 |
| Target 2 Name |
Gamma-aminobutyric acid receptor subunit alpha-1 |
| Target 2 Mechanism of Action |
Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. |
| 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 |
- GABA(A) receptor subunit alpha-1
|
| Target 2 Gene Name |
GABRA1 |
| Target 2 Protein Sequence |
>Gamma-aminobutyric acid receptor subunit alpha-1
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
|
| Target 2 Number of Residues |
456 |
| Target 2 Molecular Weight |
51801.4 |
| Target 2 Theoretical pI |
9.61 |
| 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
|
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 2 General Function |
Involved in chloride channel activity |
| Target 2 Pathways |
Not Available |
| Target 2 Reactions |
Not Available |
| Target 2 Signals |
|
| Target 2 Transmembrane Regions |
- 252-273
- 279-300
- 313-334
- 422-443
|
| 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 |
P14867  |
| Target 2 Cellular Location |
Cell junction, synapse, postsynaptic cell membrane |
| Target 2 Gene Sequence |
Not Available |
| Target 2 GenBank Gene ID |
Not Available |
| Target 2 GeneCard ID |
GABRA1  |
| Target 2 GenAtlas ID |
GABRA1  |
| Target 2 HGNC ID |
HGNC:4075  |
| Target 2 Chromosome Location |
Not Available |
| Target 2 Locus |
5q34-q35 |
| Target 2 SNPs |
SNPJam Report  |
| 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
]
- 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
]
|
| Target 2 General References |
2465923; 15489334; 2847710; 11992121; 16718694 |
|
Target 3
[top]
|
| Target 3 ID |
115 |
| Target 3 Name |
Gamma-aminobutyric acid receptor subunit alpha-2 |
| Target 3 Mechanism of Action |
Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. |
| 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 |
- GABA(A) receptor subunit alpha-2
|
| Target 3 Gene Name |
GABRA2 |
| Target 3 Protein Sequence |
>Gamma-aminobutyric acid receptor subunit alpha-2
MKTKLNIYNMQFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPG
LGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSC
PLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVM
TAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKASV
MIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRM
SRIVFPVLFGTFNLVYWATYLNREPVLGVSP
|
| Target 3 Number of Residues |
451 |
| Target 3 Molecular Weight |
51325.9 |
| Target 3 Theoretical pI |
9.50 |
| 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
|
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 3 General Function |
Involved in benzodiazepine receptor activity |
| Target 3 Pathways |
Not Available |
| Target 3 Reactions |
Not Available |
| Target 3 Signals |
|
| Target 3 Transmembrane Regions |
- 252-273
- 279-300
- 313-334
- 420-441
|
| 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 |
P47869  |
| Target 3 Cellular Location |
Cell junction, synapse, postsynaptic cell membrane |
| Target 3 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 3 GenBank Gene ID |
Not Available |
| Target 3 GeneCard ID |
GABRA2  |
| Target 3 GenAtlas ID |
GABRA2  |
| Target 3 HGNC ID |
HGNC:4076  |
| Target 3 Chromosome Location |
Not Available |
| Target 3 Locus |
4p12 |
| Target 3 SNPs |
SNPJam Report  |
| Target 3 Toxin References |
- S918 - Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
|
| Target 3 General References |
8391122; 15024690 |
|
Target 4
[top]
|
| Target 4 ID |
153 |
| Target 4 Name |
Gamma-aminobutyric acid receptor subunit alpha-3 |
| Target 4 Mechanism of Action |
Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. |
| 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 |
- GABA(A) receptor subunit alpha-3
|
| Target 4 Gene Name |
GABRA3 |
| Target 4 Protein Sequence |
>Gamma-aminobutyric acid receptor subunit alpha-3
MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDS
TDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQ
TWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLL
YTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRL
NQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLN
RESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVN
YFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGA
APSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVN
RESAIKGMIRKQ
|
| Target 4 Number of Residues |
492 |
| Target 4 Molecular Weight |
55164.1 |
| Target 4 Theoretical pI |
8.93 |
| 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 benzodiazepine receptor activity |
| Target 4 Pathways |
Not Available |
| Target 4 Reactions |
Not Available |
| Target 4 Signals |
|
| Target 4 Transmembrane Regions |
- 277-298
- 304-325
- 338-359
- 458-479
|
| 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 |
P34903  |
| Target 4 Cellular Location |
Cell junction, synapse, postsynaptic cell membrane |
| Target 4 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 4 GenBank Gene ID |
Not Available |
| Target 4 GeneCard ID |
GABRA3  |
| Target 4 GenAtlas ID |
GABRA3  |
| Target 4 HGNC ID |
HGNC:4077  |
| Target 4 Chromosome Location |
Not Available |
| Target 4 Locus |
Xq28 |
| Target 4 SNPs |
SNPJam Report  |
| Target 4 Toxin References |
- S918 - Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
|
| Target 4 General References |
8391122; 10602120; 15489334 |