Biology:Gamma-aminobutyric acid receptor subunit alpha-1
Generic protein structure example |
Gamma-aminobutyric acid receptor subunit alpha-1 is a protein that in humans is encoded by the GABRA1 gene.[1]
GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At least 16 distinct subunits of GABA-A receptors have been identified.[2]
The GABRA1 receptor is the specific target of the z-drug class of nonbenzodiazepine hypnotic agents and is responsible for their hypnotic and hallucinogenic effects. The receptor also mediates the psychoactivity of muscimol, whose effects are qualitatively similar to those of Z-drugs.
See also
References
- ↑ "Confirmation of the localization of the human GABAA receptor alpha 1-subunit gene (GABRA1) to distal 5q by linkage analysis". Genomics 14 (3): 745–748. Dec 1992. doi:10.1016/S0888-7543(05)80178-8. PMID 1330891.
- ↑ "Entrez Gene: GABRA1 gamma-aminobutyric acid (GABA) A receptor, alpha 1". https://www.ncbi.nlm.nih.gov/gene?Db=gene&Cmd=ShowDetailView&TermToSearch=2554.
Further reading
- "Sequence and expression of human GABAA receptor alpha 1 and beta 1 subunits.". FEBS Lett. 244 (2): 361–364. 1989. doi:10.1016/0014-5793(89)80563-0. PMID 2465923. Bibcode: 1989FEBSL.244..361S.
- "Isolation of a cDNA clone for the alpha subunit of the human GABA-A receptor.". Biochem. Biophys. Res. Commun. 156 (2): 1039–1045. 1988. doi:10.1016/S0006-291X(88)80949-5. PMID 2847710.
- "Oligo-capping: a simple method to replace the cap structure of eukaryotic mRNAs with oligoribonucleotides.". Gene 138 (1–2): 171–174. 1994. doi:10.1016/0378-1119(94)90802-8. PMID 8125298.
- "Isolation and characterization of the promoter of the human GABAA receptor alpha 1 subunit gene.". J. Neurochem. 62 (4): 1643–1646. 1994. doi:10.1046/j.1471-4159.1994.62041643.x. PMID 8133292.
- "gamma-Aminobutyric acidA receptors displaying association of gamma 3-subunits with beta 2/3 and different alpha-subunits exhibit unique pharmacological properties.". J. Biol. Chem. 269 (17): 12993–12998. 1994. doi:10.1016/S0021-9258(18)99974-6. PMID 8175718.
- "Construction and characterization of a full length-enriched and a 5'-end-enriched cDNA library.". Gene 200 (1–2): 149–156. 1997. doi:10.1016/S0378-1119(97)00411-3. PMID 9373149.
- "Maintenance of recombinant type A gamma-aminobutyric acid receptor function: role of protein tyrosine phosphorylation and calcineurin.". J. Pharmacol. Exp. Ther. 286 (1): 243–255. 1998. doi:10.1016/S0022-3565(24)37581-0. PMID 9655866.
- "No interaction of GABA(A) alpha-1 subunit and dopamine receptor D4 exon 3 genes in symptomatology of major psychoses.". Am. J. Med. Genet. 88 (1): 44–49. 1999. doi:10.1002/(SICI)1096-8628(19990205)88:1<44::AID-AJMG8>3.0.CO;2-Y. PMID 10050966.
- "theta, a novel gamma-aminobutyric acid type A receptor subunit.". Proc. Natl. Acad. Sci. U.S.A. 96 (17): 9891–9896. 1999. doi:10.1073/pnas.96.17.9891. PMID 10449790. Bibcode: 1999PNAS...96.9891B.
- "Dopamine receptor D2 and D4 genes, GABA(A) alpha-1 subunit genes and response to lithium prophylaxis in mood disorders.". Psychiatry Research 87 (1): 7–19. 1999. doi:10.1016/S0165-1781(99)00056-6. PMID 10512150.
- "Mutation of GABRA1 in an autosomal dominant form of juvenile myoclonic epilepsy.". Nat. Genet. 31 (2): 184–189. 2002. doi:10.1038/ng885. PMID 11992121.
- "Association of protein kinase C with GABA(A) receptors containing alpha1 and alpha4 subunits in the cerebral cortex: selective effects of chronic ethanol consumption.". J. Neurochem. 82 (1): 110–117. 2002. doi:10.1046/j.1471-4159.2002.00943.x. PMID 12091471.
- Trudell J (2002). "Unique assignment of inter-subunit association in GABA(A) alpha 1 beta 3 gamma 2 receptors determined by molecular modeling.". Biochim. Biophys. Acta 1565 (1): 91–96. doi:10.1016/S0005-2736(02)00512-6. PMID 12225856.
- "Homologous sites of GABA(A) receptor alpha(1), beta(3) and gamma(2) subunits are important for assembly.". Neuropharmacology 43 (4): 482–491. 2002. doi:10.1016/S0028-3908(02)00160-0. PMID 12367595.
- "Tryptophan scanning mutagenesis in TM4 of the GABA(A) receptor alpha1 subunit: implications for modulation by inhaled anesthetics and ion channel structure.". Neuropharmacology 43 (4): 669–678. 2002. doi:10.1016/S0028-3908(02)00175-2. PMID 12367612.
- "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–16903. 2003. doi:10.1073/pnas.242603899. PMID 12477932. Bibcode: 2002PNAS...9916899M.
- "Coupling of agonist binding to channel gating in the GABA(A) receptor.". Nature 421 (6920): 272–275. 2003. doi:10.1038/nature01280. PMID 12529644. Bibcode: 2003Natur.421..272K.
- "Gender-specific contribution of the GABA(A) subunit genes on 5q33 in methamphetamine use disorder.". Pharmacogenomics J. 3 (6): 349–355. 2004. doi:10.1038/sj.tpj.6500203. PMID 14569258.
- "Recombinant alpha 1 beta 2 gamma 2 GABA(A) receptors expressed in HEK293 and in QT6 cells show different kinetics.". Neurosci. Lett. 352 (3): 195–198. 2004. doi:10.1016/j.neulet.2003.08.060. PMID 14625018.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
{{Navbox | name = GABA receptor modulators | title = GABA receptor modulators | state = collapsed | bodyclass = hlist | groupstyle = text-align:center;
| group1 = Ionotropic | list1 = {{Navbox|subgroup | groupstyle = text-align:center | groupwidth = 5em
| group1 = GABAA | list1 =
- Agonists: (+)-Catechin
- Bamaluzole
- Barbiturates (e.g., phenobarbital)
- BL-1020
- DAVA
- Dihydromuscimol
- GABA
- Gabamide
- GABOB
- Gaboxadol (THIP)
- Homotaurine (tramiprosate, 3-APS)
- Ibotenic acid
- iso-THAZ
- iso-THIP
- Isoguvacine
- Isomuscimol
- Isonipecotic acid
- Kojic amine
- Lignans (e.g., honokiol)
- Methylglyoxal
- Monastrol
- Muscimol
- Nefiracetam
- Neuroactive steroids (e.g., allopregnanolone)
- Org 20599
- PF-6372865
- Phenibut
- Picamilon
- P4S
- Progabide
- Propofol
- Quisqualamine
- SL-75102
- TACA
- TAMP
- Terpenoids (e.g., borneol)
- Thiomuscimol
- Tolgabide
- ZAPA
- Positive modulators (abridged; see here for a full list): α-EMTBL
- Alcohols (e.g., ethanol)
- Anabolic steroids
- Avermectins (e.g., ivermectin)
- Barbiturates (e.g., phenobarbital)
- Benzodiazepines (e.g., diazepam)
- Bromide compounds (e.g., potassium bromide)
- Carbamates (e.g., meprobamate)
- Carbamazepine
- Chloralose
- Chlormezanone
- Clomethiazole
- Dihydroergolines (e.g., ergoloid (dihydroergotoxine))
- Etazepine
- Etifoxine
- Fenamates (e.g., mefenamic acid)
- Flavonoids (e.g., apigenin, hispidulin)
- Fluoxetine
- Flupirtine
- Imidazoles (e.g., etomidate)
- Kava constituents (e.g., kavain)<!--PMID: 9776662-->
- Lanthanum
- Loreclezole
- Monastrol
- Neuroactive steroids (e.g., allopregnanolone, [[Chemistry:Cholecholesterol]], THDOC)
- Niacin
- Nicotinamide (niacinamide)
- Nonbenzodiazepines (e.g., β-carbolines (e.g., [[abecarnil), cyclopyrrolones (e.g., zopiclone), imidazopyridines (e.g., zolpidem), pyrazolopyrimidines (e.g., zaleplon))
- Norfluoxetine
- Petrichloral
- Phenols (e.g., propofol)
- Phenytoin
- Piperidinediones (e.g., glutethimide)
- Propanidid
- Pyrazolopyridines (e.g., etazolate)
- Quinazolinones (e.g., methaqualone)
- Retigabine (ezogabine)
- ROD-188
- Skullcap constituents (e.g., baicalin)
- Stiripentol
- Sulfonylalkanes (e.g., sulfonmethane (sulfonal))
- Topiramate
- Valerian constituents (e.g., valerenic acid)
- Volatiles/gases (e.g., chloral hydrate, chloroform, [[Chemistry:Diethyl diethyl ether, Parparaldehyde]], sevoflurane)
- Antagonists: Bicuculline
- Coriamyrtin
- Dihydrosecurinine
- Gabazine (SR-95531)
- Hydrastine
- Hyenachin (mellitoxin)
- PHP-501
- Pitrazepin
- Securinine
- Sinomenine
- SR-42641
- SR-95103
- Thiocolchicoside
- Tutin
- Negative modulators: 1,3M1B
- 3M2B
- 11-Ketoprogesterone
- 17-Phenylandrostenol
- α5IA (LS-193,268)
- β-CCB
- β-CCE
- β-CCM
- β-CCP
- β-EMGBL
- Anabolic steroids
- Amiloride
- Anisatin
- β-Lactams (e.g., penicillins, cephalosporins, carbapenems)
- Basmisanil
- Bemegride
- Bicyclic phosphates (TBPS, TBPO, IPTBO)
- BIDN
- Bilobalide
- Bupropion
- CHEB
- Chlorophenylsilatrane
- Cicutoxin
- Cloflubicyne
- Cyclothiazide
- DHEA
- DHEA-S
- Dieldrin
- (+)-DMBB
- DMCM
- DMPC
- EBOB
- Etbicyphat
- FG-7142 (ZK-31906)
- Fiproles (e.g., fipronil)
- Flavonoids (e.g., amentoflavone, oroxylin A)
- Flumazenil
- Fluoroquinolones (e.g., ciprofloxacin)
- Flurothyl
- Furosemide
- Golexanolone
- Iomazenil (123I)
- IPTBO
- Isopregnanolone (sepranolone)
- L-655,708
- Laudanosine
- Leptazol
- Lindane
- MaxiPost
- Morphine
- Morphine-3-glucuronide
- MRK-016
- Naloxone
- Naltrexone
- Nicardipine
- Nonsteroidal antiandrogens (e.g., [[apalutamide, [[Chemistry:Bicalutbicalutamide, Enzalutenzalutamide, Chemistry:Flutamide|flut]]amide]], nilutamide)
- Oenanthotoxin
- Pentylenetetrazol (pentetrazol)
- Phenylsilatrane
- Picrotoxin (i.e., picrotin, picrotoxinin and dihydropicrotoxinin)
- Pregnenolone sulfate
- Propybicyphat
- PWZ-029
- Radequinil
- Ro 15-4513
- Ro 19-4603
- RO4882224
- RO4938581
- Sarmazenil
- SCS
- Suritozole
- TB-21007
- TBOB
- TBPS
- TCS-1105
- Terbequinil
- TETS
- Thujone
- U-93631
- Zinc
- ZK-93426
| group2 = GABAA-ρ | list2 =
- Agonists: BL-1020
- CACA
- CAMP
- Homohypotaurine
- GABA
- GABOB
- Ibotenic acid
- Isoguvacine
- Muscimol
- N4-Chloroacetylcytosine arabinoside
- Picamilon
- Progabide
- TACA
- TAMP
- Thiomuscimol
- Tolgabide
- Positive modulators: Allopregnanolone
- Alphaxolone
- ATHDOC
- Lanthanides
- Antagonists: (S)-2-MeGABA
- (S)-4-ACPBPA
- (S)-4-ACPCA
- 2-MeTACA
- 3-APMPA
- 4-ACPAM
- 4-GBA
- cis-3-ACPBPA
- CGP-36742 (SGS-742)
- DAVA
- Gabazine (SR-95531)
- Gaboxadol (THIP)
- I4AA
- Isonipecotic acid
- Loreclezole
- P4MPA
- P4S
- SKF-97541
- SR-95318
- SR-95813
- TPMPA
- trans-3-ACPBPA
- ZAPA
- Negative modulators: 5α-Dihydroprogesterone
- Bilobalide
- Loreclezole
- Picrotoxin (picrotin, picrotoxinin)
- Pregnanolone
- ROD-188
- THDOC
- Zinc
}}
| group2 = Metabotropic
| list2 =
| below =
- See also
- Receptor/signaling modulators
- GABAA receptor positive modulators
- GABA metabolism/transport modulators
}}
