| Bioactivity | JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM. | ||||||||||||
| Target | IC50: 32 nM (GHS-R1a) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | JMV 2959 | ||||||||||||
| CAS | 925238-89-7 | ||||||||||||
| Formula | C30H32N6O2 | ||||||||||||
| Molar Mass | 508.61 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |