化合物 T11477 T11477

Product Introduction
Bioactivity


英文名: GSK1059865

描述: GSK1059865 is a potent antagonist of the orexin 1 receptor.

体内活性: GSK1059865 (0.3?nM-10?nM) produces non-surmountable antagonism with a dose-dependent rightward shift of the OXA EC50 and a concomitant decrease of the agonist maximal response.?The calculated pKB value is 8.77±0.12 for GSK1059865.?GSK1059865 (0.1-3.3?μM) produces a classical surmountable profile with parallel rightward shift of the OXA EC50 without depression of the agonist maximal response.?Intraperitoneal administration of GSK1059865 produces a region-dependent inhibition of yohimbine-induced relative cerebral blood volume response.?The administration of GSK1059865 per se produces a weak relative cerebral blood volume increase in several brain regions.?GSK1059865-pretreated animals exhibit slightly higher baseline mean arterial blood pressure values than controls.Treatment with GSK1059865 significantly decreases ethanol drinking in a dose-dependent manner in CIE-exposed mice.?In contrast GSK1059865 decreases drinking in air-exposed mice only at the highest dose used.?There is no effect of GSK1059865 on sucrose intake.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (114.59 mM)


关键字: GSK1059865 | GSK 1059865 | GSK-1059865

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途