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Gamma-aminobutyric acid, a GABA-B receptor agonist. A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. [1] There are three receptors of the gamma-aminobutyric acid. The ...
A common drug, diazepam, acts as an allosteric enhancer at this binding site. [5] Another receptor for GABA, known as GABA B, can be enhanced by a molecule called baclofen. This molecule acts as an agonist, therefore activating the receptor, and is known to help control and decrease spastic movement. [citation needed]
Muscimol is a potent GABA A agonist, activating the receptor for the brain's principal inhibitory neurotransmitter, GABA. Muscimol binds to the same site on the GABA A receptor complex as GABA itself, as opposed to other GABAergic drugs such as barbiturates and benzodiazepines which bind to separate regulatory sites. [10]
Phenibut (β-phenyl-GABA) – sedative and anxiolytic from Russia; inhibitor of α 2 δ subunit-containing VGCCs and, to a lesser extent, GABA B receptor agonist. Baclofen (β-(4-chlorophenyl)-GABA) – antispasmodic drug; potent GABA B receptor agonist, weak inhibitor of α 2 δ subunit-containing VGCCs; Tolibut (β-(4-methylphenyl)-GABA ...
Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, and generalized anxiety disorder (GAD).
4-Fluorophenibut (developmental code name CGP-11130; also known as β-(4-fluorophenyl)-γ-aminobutyric acid or β-(4-fluorophenyl)-GABA) is a GABA B receptor agonist which was never marketed. [1] It is selective for the GABA B receptor over the GABA A receptor ( IC 50 = 1.70 μM and > 100 μM, respectively). [ 1 ]
GABOB is a GABA receptor agonist. [6] It has two stereoisomers, and shows stereoselectivity in its actions. [6] Specifically, (R)-(–)-GABOB is a moderate-potency agonist of the GABA B receptor, while (S)-(+)-GABOB is a partial agonist of the GABA B receptor and an agonist of the GABA A receptor. [6]
Pages in category "GABA receptor agonists" The following 7 pages are in this category, out of 7 total. This list may not reflect recent changes. ...