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GABAA Receptor Agonists
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. There are three receptors of the ''gamma''-aminobutyric acid. The two receptors GABA-α and GABA-ρ are ion channels that are permeable to chloride ions which reduces neuronal excitability. The GABA-β receptor belongs to the class of G-Protein coupled receptors that inhibit adenylyl cyclase, therefore leading to decreased cyclic adenosine monophosphate (cAMP). GABA-α and GABA-ρ receptors produce sedative and hypnotic effects and have anti-convulsion properties. GABA-β receptors also produce similar effects. Furthermore, they lead to changes in gene transcription, and are mainly found in autonomic nervous system centers. Types Many commonly used sedative and anxiolytic drugs that affect the GABA receptor complex are not agonists. These drugs act ins ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eszopiclone
Eszopiclone, sold under the brand name Lunesta among others, is a nonbenzodiazepine medication used in the treatment of short-term and long-term insomnia. It holds the distinction of being one of the few FDA-approved hypnotic medications with a controlled substance designation that does not have restrictions on its length of use. Evidence supports benefits up to six months, with some studies suggesting similar efficacy after 12 months. It is taken by mouth. Eszopiclone's primary mechanism of action involves enhancing the natural effect of GABA receptors by acting as a Positive Allosteric Modulator on GABA-A expressing neurons. This increases the frequency of the chloride channel opening when GABA is present. This is an important distingisuhmentment, as Eszopiclone will not force sleep or act as a tranquilizer but instead encourages a positive sleep-wake routine. Common side effects include headache, dry mouth, nausea, and dizziness. Severe side effects may include suicidal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Progabide
Progabide ( INN; trade name Gabrene, Sanofi-Aventis) is an analogue and prodrug of γ-aminobutyric acid (GABA) used in the treatment of epilepsy. Via conversion into GABA, progabide behaves as an agonist of the GABAA, GABAB, and GABAA-ρ receptors. Uses Progabide is approved in France for either monotherapy or adjunctive use in the treatment of epilepsy—specifically, generalized tonic-clonic, myoclonic, partial, and Lennox-Gastaut syndrome seizures—in both children and adults. Progabide has been investigated for many diseases besides epilepsy, including Parkinson's disease, schizophrenia Schizophrenia () is a mental disorder characterized variously by hallucinations (typically, Auditory hallucination#Schizophrenia, hearing voices), delusions, thought disorder, disorganized thinking and behavior, and Reduced affect display, f ..., clinical depression, anxiety disorder and spasticity with various levels of success. In 1987, Bartolini and colleagues ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Picamilon
Picamilon (also known as ''N''-nicotinoyl-GABA, pycamilon, and pikamilon) is a drug formed by a synthetic combination of niacin and γ-aminobutyric acid (GABA). It was developed in the Soviet Union in 1969 and further studied in both Russia and Japan as a prodrug of GABA. In Russia, picamilon is sold as a prescription drug. The rights to the drug belong to the Russian pharmaceutical company NPK ECHO ("НПК ЭХО"). It is not approved for sale in the United States and has been deemed an adulterating agent in dietary supplements, with five American companies required to remove their picamilon products from the market in November 2015. However, as recently as 2020, picamilon has been found in pharmaceutical dosages in over-the-counter supplements in the US. Regulation In the United States, the Food and Drug Administration ruled in 2015 that picamilon does not fit any of the dietary ingredient categories in the Dietary Supplement Health and Education Act of 1994, namely that ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenibut
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 oral administration, orally (swallowed by mouth), but may be given intravenously. Side effects of phenibut can include sedation, sleepiness, nausea, irritability, psychomotor agitation, agitation, dizziness, euphoria, and sometimes headache, among others. Overdose of phenibut can produce marked central nervous system depression including unconsciousness. The medication is structurally related to the neurotransmitter γ-aminobutyric acid (GABA), and hence is a GABA analogue. Phenibut is thought to act as a GABAB receptor, GABAB receptor agonist, similarly to baclofen and γ-hydroxybutyrate (GHB). However, at low concentrations, phenibut mildly increases the concentration of dopamine in the brain, providing Stimulant, stimulatory effects in addition to the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscimol
Muscimol, also known as agarin or pantherine, as well as 5-(aminomethyl)-1,2-oxazol-3-ol, is the principal psychoactive constituent of ''Amanita muscaria'' and '' Amanita pantherina''. Muscimol is an isoxazole alkaloid and a potent and selective orthosteric agonist for the GABAA receptor It displays sedative-hypnotic, depressant and hallucinogenic psychoactivity. It is widely used to study GABAergic function in the brain. Muscimol is under investigation for its potential to treat anxiety, insomnia, and neurological disorders, though its psychoactive nature requires careful regulation. A systematic review and meta-analysis of 22 studies found that muscimol reduces neuropathic pain symptoms, with effects beginning within 15 minutes and lasting up to three hours. Muscimol was tested in small clinical trials between 1977 and 1982 for conditions like schizophrenia, Huntington’s disease, and tardive dyskinesia, but showed limited efficacy and was eventually supplanted by the re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isonipecotic Acid
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 Moiety may refer to: __NOTOC__ Anthropology * Moiety (kinship), either of two groups into which a society is divided ** A division of society in the Iroquois societal structure in North America ** An Australian Aboriginal kinship group ** Native Ha ... in the ''iso'' position (and as such is also known as "4-piperidinecarboxylic acid"). References 4-Piperidinyl compounds Carboxylic acids GABAA receptor agonists GABAA-rho receptor antagonists Glycine receptor antagonists Sedatives {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isoguvacine
Isoguvacine is a GABAA receptor agonist used in scientific research. See also * Gaboxadol * Muscimol Muscimol, also known as agarin or pantherine, as well as 5-(aminomethyl)-1,2-oxazol-3-ol, is the principal psychoactive constituent of ''Amanita muscaria'' and '' Amanita pantherina''. Muscimol is an isoxazole alkaloid and a potent and selectiv ... References Carboxylic acids Tetrahydropyridines GABAA receptor agonists GABAA-rho receptor agonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ibotenic Acid
Ibotenic acid or (''S'')-2-amino-2-(3-hydroxyisoxazol-5-yl)acetic acid, also referred to as ibotenate, is a naturally occurring alpha-amino acid found in certain ''Amanita'' mushrooms, that primarily acts as a potent glutamate receptor agonist that precipitates neurological effects and is used experimentally as a brain-lesioning agent in mice and rats. Ibotenic acid is a conformationally-restricted analogue of glutamate that acts as a non-selective glutamate receptor agonist, strongly activating NMDA, group I and II metabotropic glutamate receptors, and weakly activating AMPA and kainate receptors. It is a prodrug of muscimol, broken down by the liver into this more stable compound, which acts as a potent GABAA and GABAA-ρ receptor agonist. Although its psychoactive effects are not well understood, some researchers speculate that ibotenic acid itself may have stimulant properties. Ibotenic acid is biosynthesized from glutamic acid by hydroxylation catalyzed by an F ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gaboxadol
Gaboxadol, also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP), is a conformationally constrained derivative of the alkaloid muscimol (a constituent of ''Amanita muscaria'') that was first synthesized in 1977 by the Danish chemist Povl Krogsgaard-Larsen. In the early 1980s, gaboxadol was the subject of a series of pilot studies that tested its efficacy as an analgesic and anxiolytic, as well as a treatment for tardive dyskinesia, Huntington's disease, Alzheimer's disease, and spasticity. It was not until 1996 that researchers attempted to harness gaboxadol's frequently reported sedative "adverse effect" for the treatment of insomnia, resulting in a series of clinical trials sponsored by Lundbeck and Merck. In March 2007, Merck and Lundbeck cancelled work on the drug, citing safety concerns and the failure of an effectiveness trial. The drug acts on the GABA system, but in a different way from benzodiazepines, Z-Drugs, and barbiturates. More specifically, gabox ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
