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JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a ( GHS-R 1a ) antagonist with an IC 50 of 32±3 nM in LLC-PK 1 cells.
In Vitro
JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R 1a ) antagonist with an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
Rats Two-hundred-gram male Sprague-Dawley rats are used in the study. The animals (n=15) are randomly assigned to an initial treatment dose or vehicle and subsequently receive all the different doses tested in a counter balanced design. Each test is separated by a 3- to 4-day-long washout period. The rats are given the i.p. injection of JMV 2959 (1, 3, and 6 mg/kg) (or vehicle) 17 min prior to being placed in the startle cages (i.e., 25 min prior to the first pulse) . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:IC50: 32±3 nM (GHS-R 1a , in LLC-PK 1 cells)