GABAA-rho receptor (previously known as the GABAC receptor) is a subclass of GABAA receptors composed entirely of rho (ρ) subunits. GABAA receptors including...
17 KB (1,673 words) - 21:43, 28 September 2024
Muscimol (category GABAA-rho receptor agonists)
selective GABAA agonist with exceptionally high affinity to GABAA-delta receptors, it is also a partial agonist at the GABAA-rho receptor, and so its...
37 KB (3,825 words) - 21:25, 7 October 2024
of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors); whereas GABAB receptors are G protein-coupled...
35 KB (3,892 words) - 05:20, 16 May 2024
5α-Dihydroprogesterone (category GABAA-rho receptor negative allosteric modulators)
modulator of the GABAA-rho receptor. The steroid has been found to possess 82% of the affinity of progesterone for the progesterone receptor in rhesus monkey...
10 KB (909 words) - 23:12, 9 November 2023
Allopregnanolone (category GABAA-rho receptor positive allosteric modulators)
is a neurosteroid and acts as a positive allosteric modulator of the GABAA receptor, the major biological target of the inhibitory neurotransmitter γ-aminobutyric...
50 KB (4,782 words) - 13:47, 19 July 2024
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory...
55 KB (5,956 words) - 21:34, 11 October 2024
Gaboxadol (category GABAA-rho receptor antagonists)
α4β3δ GABAA receptors, low-potency agonist at α1β3γ2, and partial agonist at α4β3γ. Its affinity for this α4-containing subtype of the GABAA receptor is...
7 KB (550 words) - 21:38, 16 June 2024
(+)-cis-2-Aminomethylcyclopropane carboxylic acid (category GABAA-rho receptor agonists)
(+)-cis-2-Aminomethylcyclopropane carboxylic acid ((+)-CAMP) is an agonist for the GABAA-rho receptor. "AC1LT400 - Compound Summary". PubChem Compound. USA: National Center...
3 KB (138 words) - 12:06, 18 September 2023
Ibotenic acid (category GABAA-rho receptor agonists)
decarboxylation into muscimol, it acts indirectly as a potent GABAA and GABAA-ρ receptor agonist. Unlike muscimol—the principal psychoactive constituent...
16 KB (1,473 words) - 00:34, 20 July 2024
Isoguvacine (category GABAA-rho receptor agonists)
Isoguvacine is a GABAA receptor agonist used in scientific research. Gaboxadol Muscimol Wahab A, Heinemann U, Albus K (October 2009). "Effects of gamma-aminobutyric...
1 KB (64 words) - 23:40, 3 April 2023
Gabazine (category GABAA-rho receptor antagonists)
Gabazine (SR-95531) is a drug that acts as an antagonist at GABAA receptors. It is used in scientific research and has no role in medicine, as it would...
4 KB (324 words) - 20:53, 23 September 2024
Bilobalide (category GABAA-rho receptor negative allosteric modulators)
been found to be a negative allosteric modulator at the GABAA and GABAA-rho receptors. Of GABAA, it may possibly be selective for the subunits predominantly...
7 KB (558 words) - 02:29, 26 June 2024
and metrazol, and the benzodiazepine GABAA receptor antagonist flumazenil. Other agents which may have GABAA receptor antagonism include the antibiotic ciprofloxacin...
3 KB (315 words) - 21:55, 14 April 2024
Picrotoxin (category GABAA-rho receptor negative allosteric modulators)
1126/science.127.3297.521. PMID 13529017. Rho JM, Donevan SD, Rogawski MA (December 1996). "Direct activation of GABAA receptors by barbiturates in cultured rat...
17 KB (1,614 words) - 19:29, 30 September 2024
Alfaxalone (category GABAA-rho receptor positive allosteric modulators)
positive allosteric modulator on GABAA receptors and, at high concentrations, as a direct agonist of the GABAA receptor. It is cleared quickly by the liver...
29 KB (2,748 words) - 16:34, 17 September 2024
Isonipecotic acid (category GABAA-rho receptor antagonists)
Isonipecotic acid is a heterocyclic compound which acts as a GABAA receptor partial agonist. It consists of a piperidine ring with a carboxylic acid moiety...
2 KB (90 words) - 20:07, 27 December 2022
A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel...
9 KB (804 words) - 20:40, 30 September 2024
ROD-188 (category GABAA-rho receptor negative allosteric modulators)
derived from the GABAA antagonist bicuculline by a team at Roche. Unlike bicuculline, ROD-188 acts as an agonist at GABAA receptors, being a positive...
3 KB (239 words) - 12:46, 23 September 2024
GABA's effect in the brain, binding to GABA receptors and inhibiting neuronal signaling. GABAA receptor ligands include: Abecarnil Barbiturates (in high...
8 KB (740 words) - 14:44, 20 August 2024
5β-Dihydroprogesterone (category GABAA-rho receptor negative allosteric modulators)
allopregnanolone) and also as a negative allosteric modulator of the GABAA-rho receptor. In accordance with the former action, it has been found to possess...
10 KB (908 words) - 11:09, 3 December 2023
Progabide (category GABAA-rho receptor agonists)
conversion into GABA, progabide behaves as an agonist of the GABAA, GABAB, and GABAA-ρ receptors. Progabide is approved in France for either monotherapy or...
6 KB (506 words) - 01:33, 9 September 2024
(Z)-4-Amino-2-butenoic acid (category GABAA-rho receptor agonists)
(Z)-4-Amino-2-butenoic acid (CACA, cis-4-aminocrotonic acid) is a GABA receptor partial agonist selective for the GABAA-ρ (previously known as GABAC) subtype. cis-4-Aminocrotonic...
3 KB (161 words) - 12:06, 18 September 2023
Thiomuscimol (category GABAA-rho receptor agonists)
Thiomuscimol is a GABAA receptor agonist which is structurally related to muscimol. Lykkeberg, Jytte; Krogsgaard-Larsen, Povl; Garegg, Per J.; Norberg...
2 KB (97 words) - 05:20, 21 October 2021
and include: GABAA receptors GABAA-ρ receptors The GABAB receptor, a G protein-coupled receptor, is the only metabotropic GABA receptor and its mechanism...
7 KB (687 words) - 19:31, 11 February 2023
Loreclezole (category GABAA-rho receptor negative allosteric modulators)
Loreclezole is a sedative and an anticonvulsant which acts as a GABAA receptor positive allosteric modulator. The binding site of loreclezole has been...
4 KB (331 words) - 22:11, 13 August 2024
electrical activity of neurons by binding to GABAA receptors. There are three main ways the action of the receptor can be classified: relay of signal, amplification...
26 KB (2,672 words) - 14:14, 22 July 2024
Pregnanolone (category GABAA-rho receptor negative allosteric modulators)
positive allosteric modulator of the GABAA receptor, as well as a negative allosteric modulator of the glycine receptor. Pregnanolone has sedative, anxiolytic...
8 KB (515 words) - 18:47, 6 May 2023
N4-Chloroacetylcytosine arabinoside (category GABAA-rho receptor agonists)
Liu, H; Yan, Y; Li, Y (2008). "Identification and expression of GABAC receptor in rat testis and spermatozoa". Acta Biochimica et Biophysica Sinica. 40...
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Tolgabide (category GABAA-rho receptor agonists)
as a prodrug of GABA, and therefore as an indirect agonist of the GABA receptors. Progabide Fengabine Triggle DJ (1996). Dictionary of Pharmacological...
2 KB (87 words) - 08:56, 9 September 2024
Tetrahydrodeoxycorticosterone (category GABAA-rho receptor negative allosteric modulators)
dehydrogenase. THDOC is a potent positive allosteric modulator of the GABAA receptor, and has sedative, anxiolytic and anticonvulsant effects. Changes in...
6 KB (524 words) - 17:33, 15 July 2022