Chemical Name: N-[[3-[(2S)-2-Hydroxy-3-[[2-[4-[(phenylsulfonyl)amino]phenyl]ethyl]amino]propoxy]phenyl]methyl]-acetamide
Biological ActivityCompetitive β3-adrenoceptor antagonist that displays selectivity over β1 and β2 receptors (Ki values are 4.0, 204 and 390 nM for β3-, β2- and β1-adrenoceptors respectively). Inhibits cAMP accumulation in response to isoproterenol (IC50 = 6 nM). Reduces iNOS expression, attenuates nitric oxide-induced cell proliferation and induces apoptosis in a melanoma cell line.
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β3-adrenergic receptor activity modulates melanoma cell proliferation and survival through nitric oxide signaling.
Dal Monte et al.
Naunyn Schmiedebergs Arch.Pharmacol., 2014;387:533
Potent and selective human β3-adrenergic receptor antagonist.
Candelore et al.
The function of α- and β-adrenoceptors of the saphenous artery in caveolin-1 knockout and wild-type mice.
Neidhold et al.
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