THIQ is the first selective agonist of the melanocortin-4 receptor ( MC4R ) , with high affinity and potency for hMC4R ( IC 50 =1.2 nM, EC 50 =2.1 nM) and rMC4R ( IC 50 =0.6 nM, EC 50 =2.9 nM). THIQ maintains low potency at MC1R , MC3R and MC5R . THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants.
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