GABA Receptor | Biologically Active Compounds - chemsrc

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.

RO 4938581

RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.

CAS Number: 883093-10-5
MF: C₁₃H₈BrF₂N₅
MW: 352.137
Catalog: GABA Receptor

Density: 1.9±0.1 g/cm3
Boiling Point: 559.8±60.0 °C at 760 mmHg
Melting Point: N/A
Flash Point: 292.4±32.9 °C

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MRK-898

MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s)[1].

CAS Number: 461450-30-6
MF: C₂₀H₉F₅N₄
MW: 400.30
Catalog: GABA Receptor

Density: N/A
Boiling Point: N/A
Melting Point: N/A
Flash Point: N/A

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