GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties.
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A clinically-effective anxiolytic that acts as a non-selective partial agonist of benzodiazepine receptor; exerts a partial suppression of activations by kainate, glutamate and acetylcholine in rats, also reduces the neuronal activation by kainate.
SAGE-217 (Zuranolone, SAGE217) is a potent, orally active GABAA receptor positive allosteric modulator with EC50 of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA r eceptors, respectively; effectively reduces pentylenetretazol (PTZ)-induced seizures in mice, abolishes both behavioral and electrographic seizure activity.
A potent benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity; induces hypoalgesia on a wide range of assays, inhibits pain and learning in rats.
LAU159 is a potent, functionally selective positive modulator of α6β3γ2 GABAA receptor.
A partial positive allosteric GABAA receptor modulator; displays activity at the alpha1-subunit, associated with promoting sleep.
A potent, subtype-selective, orally available GABAA receptor positive modulator with Ki of 0.4, 0.8, 0.5 and 0.1 nM for α1, α2, α3 and α5 subunits together with β3γ2; displays 600 to 2000-fold over GABAA-α4 or GABAA-α6 containing receptors; exhibits in vivo anxiolytic efficacy, attenuates spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin in rats.
A novel selective negative allosteric modulator of the GABAA receptor α5-subtype, which is under development for the treatment of cognitive impairment associated with Down syndrome.
PF-06372865 is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator; exhibits functional selectivity for receptors containing α2/3/5 subunits, with significant positive allosteric modulation (90-140%) but negligible activity (<20%) at GABAA receptors containing α1 subunits; demonstrates a robust increase in saccadic peak velocity, increases in beta frequency qEEG and a slight saturating increase in body sway in clinical trials.
AZD 3043 (THRX-918661) is a positive allosteric modulator of the GABAA receptor in vitro and a sedative/hypnotic agent in vivo, potentiates GABAA receptor-mediated chloride currents with EC50 of 36 uM; potentiates and directly activates the α1β2γ2, α2β2γ2 and α2β3γ2 GABA(A) receptor subtypes, produces hypnosis and electroencephalograph depression in rats.
TP003 is a potent, functional selectivity for α3 subunit-containing GABAA receptor agonist with Ki of <1 nM for α1β3γ2, α2β3γ2, α3β3γ2 and α5β3γ2, has no affinity for α4β3γ2 and α6β3γ2 (Ki>1 uM); produces a robust anxiolytic-like effect in both rodent and non-human primate behavioral models of anxiety, also retains efficacy in a stress-induced hyperthermia model.
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