HS014

Potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively) . Increases food intake in rats and nociception in mice following central administration in vivo. Also inhibits IL-1β-induced Fos expression in the paraventricular hypothalamus.

C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(=O)N7[C@H](C(=O)N8[C@H](C(N[C@H](C(N[C@@H](CC(O)=O)C(N)=O)=O)CCCCN)=O)CCC8)CCC7)NC(=O)CNC3=O