GSK1059865是有效地食欲素1受体 (orexin 1 receptor) 拮抗剂。

GSK1059865 is a potent orexin 1 receptor antagonist.

Solid

Orexin 1 receptor

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. GSK1059865 (0.3?nM-10?nM) produces non-surmountable antagonism with a dose-dependent rightward shift of the OXA EC 50 and a concomitant decrease of the agonist maximal response. The calculated pK B 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 EC 50 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

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[1]. Lopez MF, et al. The highly selective orexin/hypocretin 1 receptor antagonist GSK1059865 potently reduces ethanol drinking in ethanol dependent mice. Brain Res. 2016 Apr 1;1636:74-80.
[2]. Piccoli L, et al. Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats. Neuropsychopharmacology. 2012 Aug;37(9):1999-2011.

In Vitro: DMSO : 200 mg/mL (458.38 mM; Need ultrasonic)配制储备液