Description
HS-024 is a cyclic peptide antagonist of melanocortin receptor 4 (MC4R; Ki = 0.29 nM).1 It is selective for MC4R over MC1R, MC3R, and MC5R (Kis = 18.6, 5.45, and 3.29 nM, respectively). HS-024 (100 nM) inhibits cAMP accumulation induced by α-melanocyte-stimulating hormone (α-MSH; Item No. 29923) in COS-1 cells expressing human MC1R, MC3R, MC4R, or MC5R. It increases food intake in rats when administered at doses of 0.3, 1, or 3 nmol/animal. Intrathecal administration of HS-024 (1.5 nmol/animal) inhibits mechanical allodynia at 30 minutes post-injection in a rat model of spinal nerve ligation-induced neuropathic pain.2 It reduces stress-induced reinstatement of nicotine seeking in the foot shock test in rats.3WARNING This product is not for human or veterinary use.
References
[1] A KASK. Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo.[J]. Endocrinology, 1998, 139 12: 5006-5014. DOI: 10.1210/endo.139.12.6352
[2] ROSALIA BERTORELLI. Endogenous and exogenous melanocortin antagonists induce anti-allodynic effects in a model of rat neuropathic pain[J]. Behavioural Brain Research, 2005, 157 1: Pages 55-62. DOI: 10.1016/j.bbr.2004.06.008
[3] XIAOLI QI. A critical role for the melanocortin 4 receptor in stress-induced relapse to nicotine seeking in rats[J]. Addiction Biology, 2014, 20 2: 324-335. DOI: 10.1111/adb.12129
