SB-334867 free base 是一种选择性orexin-1 (OX1) 受体拮抗剂，对OX2有选择性，pKb为7.4，对 5-HT2B、5-HT2C的选择性是 100 倍，pKi值分别为 5.4 和 5.3。它减少乙醇消耗，还抑制吗啡诱导的体内运动活动敏感性的获得。

SB-334867 is a selective orexin-1 (OX1) receptor antagonist.

In CHO-OX1 cells, SB-334867 inhibits the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses with pKB of 7.27 and 7.23 respectively, without effect on the UTP (3 microM)-induced calcium response. [1]

In both male and female rats, SB-334867 (30 mg/kg, i.p.) significantly reduces natural and orexin-A-induced food intake. [2] SB-334867 (2 mg/kg, i.v.) blocks the effects of antipsychotic drugs on dopamine neuronal activity in rats. [3] SB-334867 also inhibits the development of morphine analgesic tolerance in rats. [4]

792173-99-0

C17H13N5O2

319.324

SB334867;SB334867A free base;SB-334867;SB 334867

DMSO:31.9 mg/mL (100 mM)),with gentle warming
Ethanol:3.2 mg/mL (10 mM)),with gentle warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years