JMV 2959 (hydrochloride)

JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a (GHS-R_1a) antagonist with an IC₅₀ of 32±3 nM in LLC-PK₁ cells. IC50 & Target:IC50: 32±3 nM (GHS-R_1a, in LLC-PK₁ cells)^[1] 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^[1]. 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)^[2].