TCS OX2 29

Names

[ Name ]:
TCS OX2 29

[Synonym ]:
(2S)-1-(6,7-Dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride (1:1)
(2S)-1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3,3-dimethyl-2-[(pyridin-4-ylmethyl)amino]butan-1-one hydrochloride (1:1)
1-Butanone, 1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-, (2S)-, hydrochloride (1:1)

Biological Activity

[Description]:

TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1[1][2].

[Related Catalog]:

Research Areas >> Cancer

Research Areas >> Endocrinology

Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor)

[References]

[1]. Hirose M, et al. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4497-9.

[2]. Tabaeizadeh M, et al. The differential effects of OX1R and OX2R selective antagonists on morphine conditioned place preference in naïve versus morphine-dependent mice. Behav Brain Res. 2013 Jan 15;237:41-8.

[3]. Mould R, et al. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br J Pharmacol. 2014 Jan;171(2):351-63.