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PT-141, measured in a single radioligand displacement series against I-NDP-alpha-MSH on membranes from BHK570 cells stably expressing each human subtype, returned Ki 0.25 nM at MC4R, 6.4 nM at MC1R, 17 nM at MC5R and 53 nM at MC3R, roughly 26-fold, 68-fold and 210-fold preference for MC4R over MC1R, MC5R and MC3R respectively
Supplemental Material Abbreviations cAMP cyclic AMP IR insulin receptor PKB protein kinase B PDE3B phosphodiesterase 3B AR adrenergic receptor HSL hormone-sensitive lipase AC adenylyl cyclase ODE ordinary differential equation
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