| Version |
2.5 |
| Creation Date |
2005-06-13 13:24:05 |
| Update Date |
2009-06-23 18:06:53 |
| Primary Accession Number |
DB00371 |
| Secondary Accession Number |
|
| Name |
Meprobamate |
| Drug Type |
- Approved
- Illicit
- Small Molecule
|
| Description |
A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of anxiety disorders, and also for the short-term management of insomnia but has largely been superseded by the benzodiazepines. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) Meprobamate is a controlled substance in the U.S. |
| Synonyms |
- DEA No. 2820
- Meprobamat [German]
- Meprobamato [INN-Spanish]
- Meprobamato [Italian]
- Meprobamatum [INN-Latin]
- Meprobamic acid
- Procarbamide
|
| Brand Names |
- 3P bamate
- Amepromat
- Amosene
- Anastress
- Anathylmon
- Anatimon
- Andaksin
- Andaxin
- Aneural
- Aneurol
- Aneusral
- Aneuxal
- Aneuxral
- Ansiatan
- Ansietan
- Ansil
- Ansiowas
- Anural
- Anxietil
- Anzil
- Apascil
- Apasil
- Apo-Meprobamate
- Appetrol
- Appetrol-Sr
- Arcoban
- Arpon
- Artolon
- Ataraxine
- Atraxin
- Auxietil
- Ayeramate
- Ayermate
- Bamate
- Bamd 400
- Bamo 400
- Biobamat
- Biobamate
- Brobamate
- Calmadin
- Calmax
- Calmiren
- Canquil 400
- Canquil-400
- Carbaxin
- Cirpon
- Cirponyl
- Coprobate
- Crestanil
- Cypron
- Cyrpon
- Dapaz
- Deprol
- Despasmol
- Dicandiol
- Diron
- Diurnal
- Diveron
- Dormabrol
- Ecuanil
- Edenal
- Enorden
- Epicur
- Epikur
- Equagesic
- Equanil
- Equatrate
- Equazine-M
- Equilium
- Equinil
- Equitar
- Erina
- Estasil
- Fas-Cile
- Fas-Cile 200
- Gadexyl
- Gagexyl
- Harmonin
- Hartol
- Holbamate
- Ipsotian
- Kesso-Bamate
- Kessobamate
- Klort
- Larten
- Lepenil
- Lepetown
- Letyl
- Libiolan
- Madiol
- Mar-Bate
- Margonil
- Mendel
- Mepamtin
- Mepantin
- Mepavlon
- Mepiosine
- Meposed
- Mepranil
- Mepriam
- Meprin
- Meprindon
- Mepro-Aspirin
- Mepro-analgesic
- Meprobam
- Meprobamat
- Meproban
- Meprocompren
- Meprocon
- Meprocon CMC
- Meprodil
- Meprodiol
- Meprol
- Meproleaf
- Mepron
- Mepronil
- Meprosa
- Meprosan
- Meprosin
- Meprospan
- Meprotabs
- Meprotan
- Meprotanum
- Meproten
- Meprotil
- Meprovan
- Meprozine
- Meptran
- Mesmar
- Metractyl
- Metranquil
- Micrainin
- Milpath
- Milprem
- Miltamato
- Miltann
- Miltaun
- Miltown
- Miltrate
- Miltuan
- Miltwon
- Misedant
- Morbam
- Multaun
- My-trans
- Neo-Tran
- Nephentine
- Nervonus
- Neuramate
- Oasil
- Optarket
- Orlevol
- Orolevol
- Pan-tranquil
- Pancalma
- Panediol
- Pankalma
- Pathibamate
- Paxin
- Pensive
- Perequietil
- Perequil
- Perquietil
- Pertranquil
- Pimal
- Placidon
- Placitate
- Prequil
- Probamato
- Probamyl
- Probate
- Procalmadiol
- Procalmadol
- Procalmidol
- Promate
- Promato
- Proquanil
- Protran
- Q-Gesic
- Quaname
- Quanane
- Quanil
- Quietidon
- Quivet
- Rastenil
- Reostral
- Restenil
- Restenyl
- Restinal
- Restinil
- Restran
- Robamate
- SK-Bamate
- Sadanyl
- Scolazil
- Sedabamate
- Sedanil
- Sedanyl
- Sedazil
- Sedoquil
- Sedoselecta
- Selene
- Seril
- Setran
- Shalvaton
- Solevione anastress
- Sowell
- Spantran
- Stensolo
- Tamate
- Tensol
- Tensonal
- Trancot
- Trankvilan
- Tranlisant
- Tranmep
- Tranquil
- Tranquilan
- Tranquilate
- Tranquilax
- Tranquiline
- Tranquillin
- Tranquilsan
- Tranquinol
- Tranquisan
- Trelmar
- Urbil
- Urbilat
- Vio-Bamate
- Vistabamate
- Wardamate
- Wyseals
- Zirpon
|
| Brand Mixtures |
- 282 Mep (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate + Meprobamate)
- 282 Mep Tab (Acetylsalicylic Acid + Caffeine Citrate + Codeine Phosphate + Meprobamate)
- Equagesic Tablets (Acetylsalicylic Acid + Ethoheptazine Citrate + Meprobamate)
|
| Chemical IUPAC Name |
[2-(carbamoyloxymethyl)-2-methylpentyl] carbamate |
| Chemical Formula |
C9H18N2O4 |
| Chemical Structure |
 |
| CAS Registry Number |
57-53-4 |
| InChI Identifier |
InChI=1/C9H18N2O4/c1-3-4-9(2,5-14-7(10)12)6-15-8(11)13/h3-6H2,1-2H3,(H2,10,12)(H2,11,13)/f/h10-11H2 |
| InChI Key |
NPPQSCRMBWNHMW-OUBFLUSYCR |
| KEGG Drug |
D00376  |
| KEGG Compound |
Not Available |
| PubChem Compound |
4064  |
| PubChem Substance |
7847442  |
| ChEBI ID |
Not Available |
| PharmGKB ID |
PA450377  |
| HET ID |
Not Available |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
02238646  |
| RxList Link |
http://www.rxlist.com/cgi/generic2/meprobamate.htm  |
| PDRhealth Link |
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/mil1268.shtml  |
| Wikipedia Link |
http://en.wikipedia.org/wiki/Meprobamate  |
| FDA Label |
Not Available |
| Material Safety Data Sheet (MSDS) |
|
| Synthesis Reference |
Not Available |
| Average Molecular Weight |
218.2502 |
| Monoisotopic Molecular Weight |
218.1267 |
| State |
Solid |
| Melting Point |
105 oC |
| Experimental Water Solubility |
4700 mg/L
Source: PhysProp
|
| Predicted Water Solubility |
2.47e+00 mg/mL
Calculated using ALOGPS
|
| Experimental LogP/Hydrophobicity |
0.7
Source: PhysProp
|
| Predicted LogP |
1.06
Calculated using ALOGPS
|
| Experimental LogS |
-1.67 [ADME Research, USCD] |
| Predicted LogS |
-1.95
Calculated using ALOGPS
|
| Experimental Caco2 Permeability |
Not Available |
| pKa/Isoelectric Point |
Not Available |
| Mass Spectrum |
Not Available
|
| MOL File |
Show | Download  |
| SDF File |
Show | Download  |
| PDB File |
Show | Download  |
| 2D Structure |
|
| 3D Structure |
|
| Experimental PDB ID |
Not Available |
| Isomeric SMILES |
CCCC(C)(COC(N)=O)COC(N)=O |
| Canonical SMILES |
CCCC(C)(COC(N)=O)COC(N)=O |
| Drug Category |
- Anti-anxiety Agents
- Anticonvulsants
- Hypnotics and Sedatives
- Muscle Relaxants, Central
|
| ATC Codes |
|
| AHFS Codes |
Not Available |
| Indication |
For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. |
| Pharmacology |
Meprobamate is an anxiolytic drug. It was the best selling minor tranquilizer for a time but has largely been replaced by benzodiazepines. Meprobamate has most of the pharmacological effects and dangers of the barbiturates (though it was marketed as being safer). However, it is less sedating at effective doses. It is reported to have some anticonvulsant properties against absence seizures, but can exacerbate generalized tonic-clonic seizures. It has also been used as a hypnotic (sleeping pill). However, its is currently only licensed as an anxiolytic and it is a third or fourth-order choice. |
| Mechanism of Action |
Meprobamate's mechanism of action is not known. It has been shown in animal studies to have effects at multiple sites in the central nervous system, including the thalamus and limbic system. Meprobamate binds to GABAA receptors which interrupt neuronal communication in the reticular formation and spinal cord, causing sedation and altered perception of pain. |
| Absorption |
Well absorbed from the gastrointestinal tract. |
| Toxicity |
Symptoms of overdose include coma, drowsiness, loss of muscle control, severely impaired breathing, shock, sluggishness, and unresponsiveness. Death has been reported with ingestion of as little as 12 g meprobamate and survival with as much as 40 g. |
| Protein Binding |
Not Available |
| Biotransformation |
Hepatic. |
| Half Life |
Plasma half-life is about 10 hours. |
| Dosage Forms |
|
| Patient Information |
Not Available |
| Contraindications |
Show  |
| Interactions |
Show  |
| Drug Interactions |
Not Available
|
| Food Interactions |
- Take without regard to meals. Avoid alcohol.
|
| Pathways |
Not Available
|
| General References |
- Wikipedia

- RxList

- PDRhealth

|
| Organisms Affected |
|
| Targets |
- Gamma-aminobutyric-acid receptor subunit alpha-2
- Gamma-aminobutyric-acid receptor subunit alpha-5
- Gamma-aminobutyric-acid receptor subunit alpha-4
- Gamma-aminobutyric-acid receptor subunit alpha-3
- Gamma-aminobutyric-acid receptor subunit alpha-6
- Gamma-aminobutyric-acid receptor subunit alpha-1
|
|
Drug Target 1
[top]
|
| Target 1 ID |
423 |
| Target 1 Name |
Gamma-aminobutyric-acid receptor subunit alpha-2 |
| Target 1 Synonyms |
- GABA(A) receptor subunit alpha-2
- Gamma-aminobutyric-acid receptor subunit alpha-2 precursor
|
| Target 1 Gene Name |
GABRA2 |
| Target 1 Protein Sequence |
>Gamma-aminobutyric-acid receptor subunit alpha-2 precursor
MKTKLNIYNIEFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPG
LGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSC
PLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVM
TAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWTWDGKSVVNDKKKEKASV
MIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRM
SRIVFPVLFGTFNLVYWATYLNREPVLGVSP
|
| Target 1 Number of Residues |
458 |
| Target 1 Molecular Weight |
51340 |
| Target 1 Theoretical pI |
9.41 |
| 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 GABA-A receptor activity |
| Target 1 Specific Function |
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 Pathways |
Not Available
|
| Target 1 Reactions |
Not Available |
| Target 1 Pfam Domain Function |
|
| Target 1 Signals |
|
| Target 1 Transmembrane Regions |
- 252-273
- 279-300
- 313-334
- 420-441
|
| Target 1 Essentiality |
Non-Essential |
| Target 1 GenBank ID Protein |
386422  |
| Target 1 UniProtKB/Swiss-Prot ID |
P47869  |
| Target 1 UniProtKB/Swiss-Prot Entry Name |
GBRA2_HUMAN  |
| Target 1 PDB ID |
Not Available |
| Target 1 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 1 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 1 GenBank Gene ID |
|
| Target 1 GeneCard ID |
GABRA2  |
| Target 1 GenAtlas ID |
GABRA2  |
| Target 1 HGNC ID |
HGNC:4076  |
| Target 1 Chromosome Location |
4 |
| Target 1 Locus |
4p12 |
| Target 1 SNPs |
SNPJam Report  |
| Target 1 General References |
- Hadingham KL, Wingrove P, Le Bourdelles B, Palmer KJ, Ragan CI, Whiting PJ: Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma-aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. Mol Pharmacol. 1993 Jun;43(6):970-5. [PubMed
]
|
| Target 1 Drug References |
- Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed
]
|
|
Drug Target 2
[top]
|
| Target 2 ID |
523 |
| Target 2 Name |
Gamma-aminobutyric-acid receptor subunit alpha-5 |
| Target 2 Synonyms |
- Gamma-aminobutyric-acid receptor subunit alpha-5 precursor
|
| Target 2 Gene Name |
GABRA5 |
| Target 2 Protein Sequence |
>Gamma-aminobutyric-acid receptor subunit alpha-5 precursor
MDNGMFSGFIMIKNLLLFCISMNLSSHFGFSQMPTSSVKDETNDNITIFTRILDGLLDGY
DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL
NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF
PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS
TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM
TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA
KIKKKREVILNKSTNAFTTGKMSHPPNIPKEQTPAGTSNTTSVSVKPSEEKTSESKKTYN
SISKIDKMSRIVFPVLFGTFNLVYWATYLNREPVIKGAASPK
|
| Target 2 Number of Residues |
469 |
| Target 2 Molecular Weight |
52147 |
| Target 2 Theoretical pI |
9.56 |
| 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 GABA-A receptor activity |
| Target 2 Specific Function |
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 Pathways |
Not Available
|
| Target 2 Reactions |
Not Available |
| Target 2 Pfam Domain Function |
|
| Target 2 Signals |
|
| Target 2 Transmembrane Regions |
- 260-281
- 286-307
- 319-341
- 428-449
|
| Target 2 Essentiality |
Non-Essential |
| Target 2 GenBank ID Protein |
182916  |
| Target 2 UniProtKB/Swiss-Prot ID |
P31644  |
| Target 2 UniProtKB/Swiss-Prot Entry Name |
GBRA5_HUMAN  |
| Target 2 PDB ID |
Not Available |
| Target 2 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 2 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 2 GenBank Gene ID |
|
| Target 2 GeneCard ID |
GABRA5  |
| Target 2 GenAtlas ID |
GABRA5  |
| Target 2 HGNC ID |
HGNC:4079  |
| Target 2 Chromosome Location |
15 |
| Target 2 Locus |
15q11.2-q12 |
| Target 2 SNPs |
SNPJam Report  |
| Target 2 General References |
- Wingrove P, Hadingham K, Wafford K, Kemp JA, Ragan CI, Whiting P: Cloning and expression of a cDNA encoding the human GABA-A receptor alpha 5 subunit. Biochem Soc Trans. 1992 Feb;20(1):18S. [PubMed
]
- Knoll JH, Sinnett D, Wagstaff J, Glatt K, Wilcox AS, Whiting PM, Wingrove P, Sikela JM, Lalande M: FISH ordering of reference markers and of the gene for the alpha 5 subunit of the gamma-aminobutyric acid receptor (GABRA5) within the Angelman and Prader-Willi syndrome chromosomal regions. Hum Mol Genet. 1993 Feb;2(2):183-9. [PubMed
]
- Kim Y, Glatt H, Xie W, Sinnett D, Lalande M: Human gamma-aminobutyric acid-type A receptor alpha5 subunit gene (GABRA5): characterization and structural organization of the 5' flanking region. Genomics. 1997 Jun 15;42(3):378-87. [PubMed
]
|
| Target 2 Drug References |
- Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed
]
|
|
Drug Target 3
[top]
|
| Target 3 ID |
530 |
| Target 3 Name |
Gamma-aminobutyric-acid receptor subunit alpha-4 |
| Target 3 Synonyms |
- Gamma-aminobutyric-acid receptor subunit alpha-4 precursor
|
| Target 3 Gene Name |
GABRA4 |
| Target 3 Protein Sequence |
>Gamma-aminobutyric-acid receptor subunit alpha-4 precursor
MVSAKKVPAIALSAGVSFALLRFLCLAVCLNESPGQNQKEEKLCTENFTRILDSLLDGYD
NRLRPGFGGPVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWIDKRLKYDGPIEILRLN
NMMVTKVWTPDTFFRNGKKSVSHNMTAPNKLFRIMRNGTILYTMRLTISAECPMRLVDFP
MDGHACPLKFGSYAYPKSEMIYTWTKGPEKSVEVPKESSSLVQYDLIGQTVSSETIKSIT
GEYIVMTVYFHLRRKMGYFMIQTYIPCIMTVILSQVSFWINKESVPARTVFGITTVLTMT
TLSISARHSLPKVSYLTAMDWFIAVCFAFVFSALIEFAAVNYFTNIQMEKAKRKTSKPPQ
EVPAAPVQREKHPEAPLQDTNANLNMRKRTNALVHSESDVGNRTEVGNHSSKSSTVVQES
SKGTPRSYLASSPNPFSRANAAETISAARALPSASPTSIRTGHMPRKASVGSASTRHVFG
SRLQRIKTTVNTIGATGKLSATPPPSAPPPSGSGTSKIDKYARILFPVTFGAFNMVYWVV
YLSKDTMEKSESLM
|
| Target 3 Number of Residues |
563 |
| Target 3 Molecular Weight |
61641 |
| Target 3 Theoretical pI |
10.00 |
| 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 GABA-A receptor activity |
| Target 3 Specific Function |
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 Pathways |
Not Available
|
| Target 3 Reactions |
Not Available |
| Target 3 Pfam Domain Function |
|
| Target 3 Signals |
|
| Target 3 Transmembrane Regions |
- 259-280
- 285-306
- 318-340
- 524-543
|
| Target 3 Essentiality |
Non-Essential |
| Target 3 GenBank ID Protein |
905393  |
| Target 3 UniProtKB/Swiss-Prot ID |
P48169  |
| Target 3 UniProtKB/Swiss-Prot Entry Name |
GBRA4_HUMAN  |
| Target 3 PDB ID |
Not Available |
| Target 3 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 3 Gene Sequence |
>1665 bp
ATGGTTTCTGCCAAGAAGGTACCCGCGATCGCTCTGTCCGCCGGGGTCAGTTTCGCCCTC
CTGCGCTTCCTGTGCCTGGCGGTTTGTTTAAACGAATCCCCAGGACAGAACCAAAAGGAG
GAGAAATTGTGCACAGAAAATTTCACCCGCATCCTGGACAGTTTGCTCGATGGTTATGAC
AACAGGCTGCGTCCTGGATTTGGGGGTCCTGTTACAGAAGTGAAAACTGACATATATGTC
ACCAGCTTTGGACCTGTTTCTGATGTTGAAATGGAATACACAATGGATGTGTTCTTCAGG
CAGACATGGATTGACAAAAGATTAAAATATGACGGCCCCATTGAAATTTTGAGATTGAAC
AATATGATGGTAACGAAAGTGTGGACCCCTGATACTTTCTTCAGGAATGGAAAGAAATCT
GTCTCACATAATATGACAGCTCCAAATAAGCTTTTTAGAATTATGAGAAATGGTACTATT
TTATACACAATGAGACTCACCATAAGTGCGGAGTGTCCCATGAGATTGGTGGATTTTCCC
ATGGATGGTCATGCATGCCCTTTGAAATTCGGGAGTTATGCCTATCCAAAGAGTGAGATG
ATCTATACCTGGACAAAAGGTCCTGAGAAATCAGTTGAAGTTCCGAAGGAGTCTTCCAGC
TTAGTTCAATATGATTTGATTGGGCAAACCGTATCAAGTGAAACCATCAAATCAATTACG
GGCGAATATATTGTTATGACGGTTTACTTCCACCTCAGACGGAAGATGGGTTATTTTATG
ATTCAGACCTATATTCCGTGCATTATGACAGTGATTCTTTCTCAAGTTTCATTTTGGATA
AATAAAGAATCAGTTCCCGCTAGGACTGTATTTGGAATAACAACTGTCCTCACCATGACC
ACACTAAGCATCAGTGCACGACATTCTTTGCCCAAAGTGTCCTACTTGACCGCCATGGAC
TGGTTCATAGCTGTCTGCTTTGCTTTTGTATTTTCGGCCCTTATCGAGTTTGCTGCTGTC
AACTATTTCACCAATATTCAAATGGAAAAAGCCAAAAGAAAGACATCAAAGCCCCCTCAG
GAAGTTCCCGCTGCTCCAGTGCAGAGAGAGAAGCATCCTGAAGCCCCTCTGCAGGATACA
AATGCCAATTTGAACATGAGAAAAAGAACAAATGCTTTGGTTCACTCTGAATCTGATGTT
GGCAACAGAACTGAGGTGGGAAACCATTCAAGCAAATCTTCCACAGTTGTTCAAGAATCT
TCTAAAGGCACACCTCGGTCTTACTTAGCTTCCAGTCCAAACCCATTCAGCCGTGCAAAT
GCAGCTGAAACCATATCTGCAGCAAGAGCACTTCCATCTGCTTCTCCTACTTCTATCCGA
ACTGGACATATGCCTCGAAAGGCTTCAGTTGGATCTGCTTCTACTCGTCACGTGTTTGGA
TCAAGACTGCAGAGGATAAAGACCACAGTTAATACCATAGGGGCTACTGGGAAGTTGTCA
GCTACTCCTCCTCCATCGGCTCCACCACCTTCTGGATCTGGCACAAGTAAAATAGACAAA
TATGCCCGTATTCTCTTTCCAGTCACATTTGGGGCATTTAACATGGTTTATTGGGTTGTT
TATTTATCTAAGGACACTATGGAGAAATCAGAAAGTCTAATGTAA
|
| Target 3 GenBank Gene ID |
|
| Target 3 GeneCard ID |
GABRA4  |
| Target 3 GenAtlas ID |
GABRA4  |
| Target 3 HGNC ID |
HGNC:4078  |
| Target 3 Chromosome Location |
4 |
| Target 3 Locus |
4p12 |
| Target 3 SNPs |
SNPJam Report  |
| Target 3 General References |
- McLean PJ, Farb DH, Russek SJ: Mapping of the alpha 4 subunit gene (GABRA4) to human chromosome 4 defines an alpha 2-alpha 4-beta 1-gamma 1 gene cluster: further evidence that modern GABAA receptor gene clusters are derived from an ancestral cluster. Genomics. 1995 Apr 10;26(3):580-6. [PubMed
]
- Yang W, Drewe JA, Lan NC: Cloning and characterization of the human GABAA receptor alpha 4 subunit: identification of a unique diazepam-insensitive binding site. Eur J Pharmacol. 1995 Nov 30;291(3):319-25. [PubMed
]
|
| Target 3 Drug References |
- Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed
]
|
|
Drug Target 4
[top]
|
| Target 4 ID |
580 |
| Target 4 Name |
Gamma-aminobutyric-acid receptor subunit alpha-3 |
| Target 4 Synonyms |
- Gamma-aminobutyric-acid receptor subunit alpha-3 precursor
|
| Target 4 Gene Name |
GABRA3 |
| Target 4 Protein Sequence |
>Gamma-aminobutyric-acid receptor subunit alpha-3 precursor
MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDS
TDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQ
TWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLL
YTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRL
NQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLN
RESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVN
YFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGA
APSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVN
RESAIKGMIRKQ
|
| Target 4 Number of Residues |
500 |
| Target 4 Molecular Weight |
55165 |
| 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 GABA-A receptor activity |
| Target 4 Specific Function |
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 Pathways |
Not Available
|
| Target 4 Reactions |
Not Available |
| Target 4 Pfam Domain Function |
|
| Target 4 Signals |
|
| Target 4 Transmembrane Regions |
- 277-298
- 304-325
- 338-359
- 458-479
|
| Target 4 Essentiality |
Non-Essential |
| Target 4 GenBank ID Protein |
386424  |
| Target 4 UniProtKB/Swiss-Prot ID |
P34903  |
| Target 4 UniProtKB/Swiss-Prot Entry Name |
GBRA3_HUMAN  |
| Target 4 PDB ID |
Not Available |
| Target 4 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| 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 |
|
| Target 4 GeneCard ID |
GABRA3  |
| Target 4 GenAtlas ID |
GABRA3  |
| Target 4 HGNC ID |
HGNC:4077  |
| Target 4 Chromosome Location |
X |
| Target 4 Locus |
Xq28 |
| Target 4 SNPs |
SNPJam Report  |
| Target 4 General References |
- Amir R, Dahle EJ, Toriolo D, Zoghbi HY: Candidate gene analysis in Rett syndrome and the identification of 21 SNPs in Xq. Am J Med Genet. 2000 Jan 3;90(1):69-71. [PubMed
]
- Hadingham KL, Wingrove P, Le Bourdelles B, Palmer KJ, Ragan CI, Whiting PJ: Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma-aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. Mol Pharmacol. 1993 Jun;43(6):970-5. [PubMed
]
|
| Target 4 Drug References |
- Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed
]
|
|
Drug Target 5
[top]
|
| Target 5 ID |
841 |
| Target 5 Name |
Gamma-aminobutyric-acid receptor subunit alpha-6 |
| Target 5 Synonyms |
- Gamma-aminobutyric-acid receptor subunit alpha-6 precursor
|
| Target 5 Gene Name |
GABRA6 |
| Target 5 Protein Sequence |
>Gamma-aminobutyric-acid receptor subunit alpha-6 precursor
MASSLPWLCIILWLENALGKLEVEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKT
DIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFGGPTEILSLNNLMVSKIWTPDTFFRN
GKKSIAHNMTTPNKLFRIMQNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYP
KSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKM
GYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYA
TAMDWFIAVCFAFVFSALIEFAAVNYFTNLQTQKAKRKAQFAAPPTVTISKATEPLEAEI
VLHPDSKYHLKKRITSLSLPIVSSSEANKVLTRAPILQSTPVTPPPLPPAFGGTSKIDQY
SRILFPVAFAGFNLVYWVVYLSKDTMEVSSSVE
|
| Target 5 Number of Residues |
460 |
| Target 5 Molecular Weight |
51035 |
| Target 5 Theoretical pI |
8.40 |
| 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 GABA-A receptor activity |
| Target 5 Specific Function |
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 Pathways |
Not Available
|
| Target 5 Reactions |
Not Available |
| Target 5 Pfam Domain Function |
|
| Target 5 Signals |
|
| Target 5 Transmembrane Regions |
- 243-264
- 269-290
- 301-324
- 420-441
|
| Target 5 Essentiality |
Non-Essential |
| Target 5 GenBank ID Protein |
1470364  |
| Target 5 UniProtKB/Swiss-Prot ID |
Q16445  |
| Target 5 UniProtKB/Swiss-Prot Entry Name |
GBRA6_HUMAN  |
| Target 5 PDB ID |
Not Available |
| Target 5 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 5 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 5 GenBank Gene ID |
|
| Target 5 GeneCard ID |
GABRA6  |
| Target 5 GenAtlas ID |
GABRA6  |
| Target 5 HGNC ID |
HGNC:4080  |
| Target 5 Chromosome Location |
5 |
| Target 5 Locus |
5q34 |
| Target 5 SNPs |
SNPJam Report  |
| Target 5 General References |
- Hadingham KL, Garrett EM, Wafford KA, Bain C, Heavens RP, Sirinathsinghji DJ, Whiting PJ: Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol Pharmacol. 1996 Feb;49(2):253-9. [PubMed
]
|
| Target 5 Drug References |
- Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed
]
|
|
Drug Target 6
[top]
|
| Target 6 ID |
872 |
| Target 6 Name |
Gamma-aminobutyric-acid receptor subunit alpha-1 |
| Target 6 Synonyms |
- Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
|
| Target 6 Gene Name |
GABRA1 |
| Target 6 Protein Sequence |
>Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
|
| Target 6 Number of Residues |
463 |
| Target 6 Molecular Weight |
51802 |
| Target 6 Theoretical pI |
9.61 |
| 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 GABA-A receptor activity |
| Target 6 Specific Function |
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 Pathways |
Not Available
|
| Target 6 Reactions |
Not Available |
| Target 6 Pfam Domain Function |
|
| Target 6 Signals |
|
| Target 6 Transmembrane Regions |
- 252-273
- 279-300
- 313-334
- 422-443
|
| Target 6 Essentiality |
Non-Essential |
| Target 6 GenBank ID Protein |
31631  |
| Target 6 UniProtKB/Swiss-Prot ID |
P14867  |
| Target 6 UniProtKB/Swiss-Prot Entry Name |
GBRA1_HUMAN  |
| Target 6 PDB ID |
Not Available |
| Target 6 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 6 Gene Sequence |
>1371 bp
ATGAGGAAAAGTCCAGGTCTGTCTGACTGTCTTTGGGCCTGGATCCTCCTTCTGAGCACA
CTGACTGGAAGAAGCTATGGACAGCCGTCATTACAAGATGAACTTAAAGACAATACCACT
GTCTTCACCAGGATTTTGGACAGACTCCTAGATGGTTATGACAATCGCCTGAGACCAGGA
TTGGGAGAGCGTGTAACCGAAGTGAAGACTGATATCTTCGTCACCAGTTTCGGACCCGTT
TCAGACCATGATATGGAATATACAATAGATGTATTTTTCCGTCAAAGCTGGAAGGATGAA
AGGTTAAAATTTAAAGGACCTATGACAGTCCTCCGGTTAAATAACCTAATGGCAAGTAAA
ATCTGGACTCCGGACACATTTTTCCACAATGGAAAGAAGTCAGTGGCCCACAACATGACC
ATGCCCAACAAACTCCTGCGGATCACAGAGGATGGCACCTTGCTGTACACCATGAGGCTG
ACAGTGAGAGCTGAATGTCCGATGCATTTGGAGGACTTCCCTATGGATGCCCATGCTTGC
CCACTAAAATTTGGAAGTTATGCTTATACAAGAGCAGAAGTTGTTTATGAATGGACCAGA
GAGCCAGCACGCTCAGTGGTTGTAGCAGAAGATGGATCACGTCTAAACCAGTATGACCTT
CTTGGACAAACAGTAGACTCTGGAATTGTCCAGTCAAGTACAGGAGAATATGTTGTTATG
ACCACTCATTTCCACTTGAAGAGAAAGATTGGCTACTTTGTTATTCAAACATACCTGCCA
TGCATAATGACAGTGATTCTCTCACAAGTCTCCTTCTGGCTCAACAGAGAGTCTGTACCA
GCAAGAACTGTCTTTGGAGTAACAACTGTGCTCACCATGACAACATTGAGCATCAGTGCC
AGAAACTCCCTCCCTAAGGTGGCTTATGCAACAGCTATGGATTGGTTTATTGCCGTGTGC
TATGCCTTTGTGTTCTCAGCTCTGATTGAGTTTGCCACAGTAAACTATTTCACTAAGAGA
GGTTATGCATGGGATGGCAAAAGTGTGGTTCCAGAAAAGCCAAAGAAAGTAAAGGATCCT
CTTATTAAGAAAAACAACACTTACGCTCCAACAGCAACCAGCTACACCCCTAATTTGGCC
AGGGGCGACCCGGGCTTAGCCACCATTGCTAAAAGTGCAACCATAGAACCTAAAGAGGTC
AAGCCCGAAACAAAACCACCAGAACCCAAGAAAACCTTTAACAGTGTCAGCAAAATTGAC
CGACTGTCAAGAATAGCCTTCCCGCTGCTATTTGGAATCTTTAACTTAGTCTACTGGGCT
ACGTATTTAAACAGAGAGCCTCAGCTAAAAGCCCCCACACCACATCAATAG
|
| Target 6 GenBank Gene ID |
|
| Target 6 GeneCard ID |
GABRA1  |
| Target 6 GenAtlas ID |
GABRA1  |
| Target 6 HGNC ID |
HGNC:4075  |
| Target 6 Chromosome Location |
5 |
| Target 6 Locus |
5q34-q35 |
| Target 6 SNPs |
SNPJam Report  |
| Target 6 General References |
- Cossette P, Liu L, Brisebois K, Dong H, Lortie A, Vanasse M, Saint-Hilaire JM, Carmant L, Verner A, Lu WY, Wang YT, Rouleau GA: Mutation of GABRA1 in an autosomal dominant form of juvenile myoclonic epilepsy. Nat Genet. 2002 Jun;31(2):184-9. Epub 2002 May 6. [PubMed
]
- Schofield PR, Pritchett DB, Sontheimer H, Kettenmann H, Seeburg PH: Sequence and expression of human GABAA receptor alpha 1 and beta 1 subunits. FEBS Lett. 1989 Feb 27;244(2):361-4. [PubMed
]
- Garrett KM, Duman RS, Saito N, Blume AJ, Vitek MP, Tallman JF: Isolation of a cDNA clone for the alpha subunit of the human GABA-A receptor. Biochem Biophys Res Commun. 1988 Oct 31;156(2):1039-45. [PubMed
]
|
| Target 6 Drug References |
- Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed
]
|