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JMV 2959 hydrochloride

CAS No. :

MCE 站：JMV 2959 hydrochloride

产品活性：JMV 2959 hydrochloride 是一种生长激素促分泌素受体 1a 型 (GHS-R_1a) 拮抗剂，作用于 LLC-PK₁ 细胞，抑制 GHS-R_1a，IC₅₀ 值为 32±3 nM。

研究领域：GPCR/G Protein

作用靶点：GHSR

In Vitro: JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R_1a) antagonist with an IC₅₀ of 32 nM. JMV 2959 does not induce any intracellular calcium mobilization by itself. The dissociation constant of the receptor/JMV 2959 complex is determined by the Schild method. This experiment reveals a dissociation constant Kb of 19±6 nM.

In Vivo: Intraperitoneal (i.p.) administration of Ghrelin (0.033, 0.1, and 0.33 mg/kg) does not alter the acoustic startle responses (ASR) or prepulse inhibition (PPI) in rats. Conversely, i.p. injection of JMV 2959 (1, 3, and 6 mg/kg), dose dependently decrease the ASR and increase PPI. Pretreatment with JMV 2959 at a dose with no effect on ASR or PPI per se, completely blocks Phencyclidine (PCP)-induced (2 mg/kg) deficits in PPI while pretreatment with the highest dose of Ghrelin does not potentiate or alter PPI responses of a sub-threshold dose of PCP (0.75 mg/kg).

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