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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 ...
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 ...
The gabapentinoid drugs do not bind significantly to other known drug receptors and so the α 2 δ VGCC subunit has been called the gabapentin receptor. [ 15 ] [ 4 ] Recently, the same α 2 δ-1 protein has been found closely associated not with VGCCs but with other proteins such as presynaptic NMDA-type glutamate receptors , cell adhesion ...
A GABAergic or GABAnergic agent is any chemical that modifies the effects of GABA in the body or brain. Some different classes of GABAergic drugs include agonists, antagonists, modulators, reuptake inhibitors and enzymes. [1]
Keppra (levetiracetam) – an anticonvulsant drug which is sometimes used as a mood stabilizer and has potential benefits for other psychiatric and neurologic conditions such as Tourette syndrome, anxiety disorder, and Alzheimer's disease; Klonopin – anti-anxiety and anti-epileptic medication of the benzodiazepine class
IC 50 / pIC 50 values represent binding affinity only and do not reflect efficacy or pharmacokinetics, and some compounds listed are GABA A antagonists rather than agonists (e.g. flumazenil). Low IC 50 or high pIC 50 values indicate tighter binding (pIC 50 of 8.0 = IC 50 of 10nM, pIC 50 of 9.0 = IC 50 of 1nM, etc.)
Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat neuropathic pain and also for partial seizures [10] [7] of epilepsy. It is a commonly used medication for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central pain. [11]
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]
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