Chemical Name:4-[[(Hexylamino)carbonyl]amino]-N-[4-[2-[[(2S)-2-hydrox
y-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]-benzen
esulfonamide
Biological Activity:
Subnanomolar potent β3-adrenergic receptor
partial agonist that is > 1000-fold selective over β1- and β2-adrenoceptors (EC50
values are 0.43, 580 and > 10000 nM for activation of cloned human β3-, β1- and β2-adrenoceptors
respectively). In vitro, stimulates lipolysis in rhesus adipocytes with an EC50
of 3.9 nM.
Parmeeet al (1998) Discovery of
L-755,507: a subnanomolar human β3
adrenergic receptor agonist. Bioorg.Med.Chem.Lett. 8 1107. Fisher et
al (1998) A selective human β3
adrenergic receptor agonist increases metabolic rate in rhesus monkeys.
J.Clin.Invest. 101 2387.
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