TCS OX2 29 |
| رقم الكتالوجGC10549 |
TCS OX2 29 هو أحد مضادات مستقبلات orexin-2 (OX2R) القوية وذات الصلة العالية ومضاد مستقبلات orexin-2 (OX2R) بقيمة IC50 تبلغ 40 نانومتر وقيمة pKI تساوي 7.5.
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Cas No.: 372523-75-6
Sample solution is provided at 25 µL, 10mM.
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TCS-OX2-29 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].
TCS-OX2-29 inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor[2].
TCS-OX2-29 (5-10 mg/kg; intraperitoneal injection; adult male NMRI mice) treatment suppresses conditioned place preference (CPP) acquisition and expression in both naïve and dependent mice significantly[3].
References:
[1]. Hirose M et al. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidicantagonist. 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]. R Mould et al. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br J Pharmacol. 2014 Jan; 171(2): 351-363.
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