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GSK1059865

CAS No. : 1191044-58-2

MCE 站：GSK1059865

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

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Orexin Receptor (OX Receptor)

In Vivo: 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 EC₅₀ 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 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.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  Endocrinology Compound Library  |  Orexin A (human, rat, mouse)  |  TCS-OX2-29  |  SB-674042  |  TCS 1102  |  EMPA  |  SB-408124  |  Orexin B, human TFA  |  IPSU  |  SB-649868  |  Orexin B, rat, mouse  |  Orexin receptor antagonist 2  |  OXA(17-33)  |  [Ala11,D-Leu15]-Orexin B(human)

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