DC Chemicals Limited
China
Product Name: JMV 2959
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Purity: 98.0%
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925238-89-7

925238-89-7 structure

925238-89-7 structure

Name: JMV 2959
Chemical Name: JMV 2959
CAS Number: 925238-89-7
Molecular Formula: C₃₀H₃₂N₆O₂
Molecular Weight: 508.61
Catalog: Signaling Pathways GPCR/G Protein GHSR
Create Date: 2018-06-28 07:15:59
Modify Date: 2024-01-04 18:55:41
JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.

Name	JMV 2959

Description	JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> GHSR Research Areas >> Neurological Disease
Target	IC50: 32 nM (GHS-R1a)
In Vitro	JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM. JMV 2959 does not induce any intracellular calcium mobilization by itself[1].
In Vivo	When administered alone, it does not increase food intake and does not significantly stimulate growth hormone (GH) release[1]. JMV 2959 dose dependently decreases the startle response (F(3.42)=4.4, p<0.01) and increases %prepulse inhibition (PPI) (F(3.42)=3.9, p<0.05) in the prepulse inhibition paradigm. The alteration in the startle response is mainly due to a 27% decrease in the startle seen in the highest dose of JMV 2959 (6 mg/kg) compare to vehicle (p<0.05)[2]. 6 mg/kg JMV 2959 induces a significant suppression of locomotion on days 1 to 7 relative to baseline day 0 (F(7,49)=2.21, p<0.05). Results also reveal a significant interaction between JMV 2959 treatment and day (F(1,14)=4.397, p<0.05)[3].
Animal Admin	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 injection of JMV 2959 (or vehicle) 17 min prior to being placed in the startle cages (i.e., 25 min prior to the first pulse). The doses of JMV 2959 used for the dose response are 1, 3, and 6 mg/kg[2].
References	[1]. Moulin A, et al. The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands: development of JMV 2959, a potent antagonist. Amino Acids. 2013 Feb;44(2):301-14. [2]. Engel JA, et al. Blockade of growth hormone secretagogue receptor 1A signaling by JMV 2959 attenuates the NMDAR antagonist, phencyclidine-induced impairments in prepulse inhibition. Psychopharmacology (Berl). 2015 Dec;232(23):4285-92. [3]. Clifford PS, et al. Attenuation of cocaine-induced locomotor sensitization in rats sustaining genetic or pharmacologic antagonism of ghrelin receptors. Addict Biol. 2012 Nov;17(6):956-63.

Molecular Formula	C₃₀H₃₂N₆O₂
Molecular Weight	508.61