1234977-97-9

1234977-97-9 structure

Name: SJM-3
Chemical Name: (6-Fluoro-2-methyl-3,4-dihydro-1(2H)-quinolinyl)[2-(2-pyrazinyl)-1,3-thiazol-4-yl]methanone
CAS Number: 1234977-97-9
Molecular Formula: C₁₈H₁₅FN₄OS
Molecular Weight: 354.401
Create Date: 2018-07-19 20:46:12
Modify Date: 2024-02-19 17:45:36
SJM-3 is a positive allosteric modulator of various isoforms of the GABAA receptor, specifically binding to the high-affinity benzodiazepine binding site located at the α+/γ- subunit interface.

Name	(6-Fluoro-2-methyl-3,4-dihydro-1(2H)-quinolinyl)[2-(2-pyrazinyl)-1,3-thiazol-4-yl]methanone
Synonyms	(6-Fluoro-2-methyl-3,4-dihydro-1(2H)-quinolinyl)[2-(2-pyrazinyl)-1,3-thiazol-4-yl]methanone Methanone, (6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinyl)[2-(2-pyrazinyl)-4-thiazolyl]-

Description	SJM-3 is a positive allosteric modulator of various isoforms of the GABAA receptor, specifically binding to the high-affinity benzodiazepine binding site located at the α+/γ- subunit interface.
In Vitro	SJM-3 binds at the high-affinity benzodiazepine binding site at theα+/γ- subunit interface but effects its action through another site presumably located within the transmembrane domain. The binding affinity of SJM-3 at wild type receptors is determined by displacement of [ 3 H]-Flunitrazepam and [ 3 H]-Ro15-1788 and indicates a K i of SJM-3 amounting to 218±70 nM and 242±38 nM, respectively[1].
References	1. Simon J Middendorp, et al. Positive modulation of synaptic and extrasynaptic GABAA receptors by an antagonist of the high affinity benzodiazepine binding site. Neuropharmacology. 2015 Aug;95:459-67.