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In pharmacology, GABA A receptor positive allosteric modulators, also known as GABAkines or GABA A receptor potentiators, [1] are positive allosteric modulator (PAM) molecules that increase the activity of the GABA A receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system.
The ionotropic GABA A receptor protein complex is also the molecular target of the benzodiazepine class of tranquilizer drugs. Benzodiazepines do not bind to the same receptor site on the protein complex as does the endogenous ligand GABA (whose binding site is located between α- and β-subunits), but bind to distinct benzodiazepine binding sites situated at the interface between the α- and ...
The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric ... Two separate genes on two chromosomes control GABA synthesis ...
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It also has low micromolecular affinity to GABA with a Michaelis-Menten constant of 2.5 μM, [1] and requires the presence of Cl- ions in the extracellular matrix. The GABA transporter help creates an equilibrium of GABA and will work in the reverse direction if needed to maintain the baseline concentration of GABA in the system. [1]
In enzymology, 4-aminobutyrate transaminase (EC 2.6.1.19), also called GABA transaminase or 4-aminobutyrate aminotransferase, or GABA-T, is an enzyme that catalyzes the chemical reaction: 4-aminobutanoate + 2-oxoglutarate ⇌ {\displaystyle \rightleftharpoons } succinate semialdehyde + L-glutamate
GABA B Receptors are similar in structure to and in the same receptor family with metabotropic glutamate receptors. [10] There are two subunits of the receptor, GABA B1 and GABA B2, [11] and these appear to assemble as obligate heterodimers in neuronal membranes by linking up by their intracellular C termini. [10]
The GABA A-rho receptor (previously known as the GABA C receptor) is a subclass of GABA A receptors composed entirely of rho (ρ) subunits. GABA A receptors including those of the ρ-subclass are ligand-gated ion channels responsible for mediating the effects of gamma-amino butyric acid (), the major inhibitory neurotransmitter in the brain.