GABAA receptor agonists

Propofol is the active component of an intravenous anesthetic formulation used for induction and maintenance of general anesthesia. The formulation was approved under the brand name Diprivan. Numerous generic versions have since been released. Intravenous administration is used to induce unconsciousness, after which anesthesia may be maintained using a combination of medications. It is manufactured as part of a sterile injectable emulsion formulation using soybean oil and lecithin, giving it a white milky coloration.

Muscimol, also known as agarin, pantherine, or pyroibotenic acid, is a GABAA receptor agonist with sedative and hallucinogenic effects and the principal psychoactive constituent of Amanita mushrooms such as Amanita muscaria (fly agaric) and Amanita pantherina (panther cap). It is a 3-hydroxyisoxazole alkaloid and is closely related structurally to the neurotransmitter γ-aminobutyric acid (GABA). The compound is widely used as a ligand and agonist of the GABAA receptor in scientific research. Muscimol is typically taken orally, but may also be smoked. Peak effects occur after 1 to 3hours orally

Methylglyoxal (MGO) is the organic compound with the formula CH3C(O)CHO. It is a reduced derivative of pyruvic acid. It is a reactive compound that is implicated in the biology of diabetes. Methylglyoxal is produced industrially by degradation of carbohydrates using overexpressed methylglyoxal synthase.

group of stereoisomers

Phenibut, sold under the brand name Anvifen among others, is a central nervous system (CNS) depressant with anxiolytic effects, and is used to treat anxiety, insomnia, and for a variety of other indications. It is usually taken orally (swallowed by mouth), but may be given intravenously.

Thiocolchicoside (Muscoril, Myoril, Neoflax) is a semi-synthetic derivative of colchicine, used as muscle relaxant with anti-inflammatory and analgesic effects. Its mechanism of action is unknown, but it is believed to act via antagonism of nicotinic acetylcholine receptors (nAchRs). However, it also appears to be a competitive antagonist of GABAA and glycine receptors. As such, it has powerful convulsant activity and should not be used in seizure-prone individuals.

Homotaurine, also known as tramiprosate (INN), 3-amino-1-propanesulfonic acid, or 3-APS, is a natural sulfonic acid found in seaweed. It is analogous to taurine, but with an extra carbon in its chain. It has GABAergic activity, apparently by mimicking GABA, which it resembles.

chemical compound

Gaboxadol, also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP) and by its former developmental code names Lu-2-030, MK-0928, and OV101, is a GABAA receptor agonist related to muscimol which was investigated for the treatment of insomnia and other conditions like Angelman syndrome but was never marketed. At lower doses, the drug has sedative and hypnotic effects, and at higher doses, it produces hallucinogenic effects. It is taken orally.

pair of isomers

ORG-20599 is a synthetic neuroactive steroid, with sedative effects resulting from its action as a GABAA receptor positive allosteric modulator and, at higher concentrations, agonist. It was developed for use as an anaesthetic agent but was never marketed for this purpose, although it is still used in scientific research.

Progabide, sold under the brand name Gabrene, is a GABA receptor agonist which is used in the treatment of epilepsy. It is an analogue of γ-aminobutyric acid (GABA) and acts both via a metabolite and as a prodrug of GABA, in turn behaving as an agonist of the GABA receptors.

Quisqualamine is the α-decarboxylated analogue of the glutamate receptor agonist and neurotoxin quisqualic acid and an analogue of the neurotransmitter γ-aminobutyric acid (GABA).

Nefiracetam is a nootropic drug of the racetam family. Preliminary research suggests that it may possess certain antidementia properties in rats.