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SJM-3

Names

[ CAS No. ]:
1234977-97-9

[ Name ]:
SJM-3

[Synonym ]:
(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]-

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
568.2±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C18H15FN4OS

[ Molecular Weight ]:
354.401

[ Flash Point ]:
297.4±32.9 °C

[ Exact Mass ]:
354.095062

[ LogP ]:
3.01

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.630

Related Compounds