THIQ is a selective and potent melanocortin 4 receptor (MC4-R) agonist (IC50 values are 1.2, 761 and 2067 nM for human MC4-R, MC3-R and MC1-R respectively). Following systemic administration, enhances intracavernosal pressure and stimulates erectile activity in rats ex copula.
Sebhat et al (2002) Design and pharmacology of N-[(3R)-1,2,3,4-Tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-methyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective melanocortin subtype-4 receptor agonist. J.Med.Chem. 45 4589. Martin et al (2002) Activation of melanocortin MC4 receptors increases erectile activity in rats ex copula. Eur.J.Pharmacol. 454 71. Mutulis et al (2004) New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ". J.Med.Chem. 47 4613.
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