GABAA receptor positive allosteric modulator information
GABAA receptor positive modulators
Fig 1. Chemical structure of gamma-aminobutyric acid or GABA
Fig 2. Schematic diagram of a GABAA receptor protein ((α1)2(β2)2(γ2)) which illustrates the five combined subunits that form the protein, the chloride (Cl-) ion channel pore, the two GABA active binding sites at the α1 and β2 interfaces, and the benzodiazepine (BZD) allosteric binding site at the α1 and γ2 interface.
In pharmacology, GABAA receptor positive allosteric modulators, also known as GABAkines or GABAA receptor potentiators,[1] are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system.
GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it triggers the GABAA receptor to open its chloride channel to allow chloride ions into the neuron, making the cell hyperpolarized and less likely to fire. GABAA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present.
Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-aminobutyric acid (GABA) neurotransmitter molecule: they affect the receptor by binding at a different site on the protein. This is called allosteric modulation.
In psychopharmacology, GABAA receptor PAMs used as drugs have mainly sedative and anxiolytic effects. Examples of GABAA PAMs include ethanol, benzodiazepines such as diazepam (Valium) and alprazolam (Xanax), Z-drugs such as zolpidem (Ambien) and the barbiturate drugs.
^Cerne R, Lippa A, Poe MM, Smith JL, Jin X, Ping X, Golani LK, Cook JM, Witkin JM (June 2022). "GABAkines - Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAA receptors". Pharmacol Ther. 234: 108035. doi:10.1016/j.pharmthera.2021.108035. PMC 9787737. PMID 34793859.
and 29 Related for: GABAA receptor positive allosteric modulator information
pharmacology, GABAAreceptorpositiveallostericmodulators, also known as GABAkines or GABAAreceptor potentiators, are positiveallostericmodulator (PAM) molecules...
A GABAAreceptor negative allostericmodulator is a negative allostericmodulator (NAM), or inhibitor, of the GABAAreceptor, a ligand-gated ion channel...
AMPA receptorpositiveallostericmodulators are positiveallostericmodulators (PAMs) of the AMPA receptor (AMPR), a type of ionotropic glutamate receptor...
Benzodiazepines like diazepam and midazolam act as positiveallostericmodulators for GABAAreceptors. When these receptors are activated, there's a rise in intracellular...
A receptormodulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical...
sedation or lack of coordination. Etifoxine acts as a GABAAreceptorpositiveallostericmodulator and as a ligand for translocator proteins. Both mechanisms...
inhibitory pregnane neurosteroid, zuranolone acts as a positiveallostericmodulator of the GABAAreceptor. Zuranolone was approved for medical use in the United...
consciousness. It is a neurosteroid and acts as a positiveallostericmodulator of the GABAAreceptor, the major biological target of the inhibitory neurotransmitter...
its mode of action via the benzodiazepine receptor and directly targeting GABAAallostericmodulatorreceptors. It possesses anxiolytic, amnesic, anticonvulsant...
"Indiplon is a high-affinity positiveallostericmodulator with selectivity for alpha1 subunit-containing GABAAreceptors". The Journal of Pharmacology...
inhibitory androstane neurosteroid, acting as a positiveallostericmodulator of the GABAAreceptor, and possesses anticonvulsant effects. The unnatural...
stimulate muscles. Some studies show that menthol acts as a GABAAreceptorpositiveallostericmodulator and increases GABAergic transmission in PAG neurons....
both through potentiation of GABAAreceptor activity and therefore acting as a GABAAreceptorpositiveallostericmodulator, thereby slowing the channel-closing...
anti-convulsant stiripentol acts directly on the GABA(A) receptor as a positiveallostericmodulator". Neuropharmacology. 56 (1): 190–7. doi:10.1016/j.neuropharm...
mainly acts as a GABAAreceptormodulator, leading to increased inhibitory transmission and downstream sedative effects via allosteric modulation and agonism...
concentration of circulating allopregnanolone, a potent GABAAreceptorpositiveallostericmodulator, in the brain. Norfluoxetine, a primary active metabolite...
administration. Darigabat acts as a GABAAreceptorpositiveallostericmodulator It is specifically a positiveallostericmodulator that selectively targets α2...
is a positiveallostericmodulator of the gamma-aminobutyric acid (GABA) type A receptor.[unreliable medical source?] When it binds to the receptor, effects...
mechanism of action to benzodiazepine drugs, acting as GABAAreceptorpositiveallostericmodulators of the benzodiazepine site, and therefore exhibit similar...
subtypes of a given receptor except the subtype of interest, which is termed "absolute subtype selectivity". If an allostericmodulator does not possess...
Benzodiazepine like compounds are acting as positiveallostericmodulators to the gamma-aminobutyric acid GABAAreceptor. GABA is the main inhibitor of neurotransmitters...
potent positiveallostericmodulator of the GABAAreceptor. Testosterone has been found to act as an antagonist of the TrkA and p75NTR, receptors for the...
subtype-selective GABAAreceptorpositiveallostericmodulator via a binding site in the transmembrane domain at the β+α− interface. At receptors expressed in...
"Indiplon is a high-affinity positiveallostericmodulator with selectivity for alpha1 subunit-containing GABAAreceptors". The Journal of Pharmacology...
Global Information
