1025438-03-2Relevant academic research and scientific papers
Novel and potent small-molecule urotensin II receptor agonists
Lehmann, Fredrik,Currier, Erika A.,Clemons, Bryan,Hansen, Lars K.,Olsson, Roger,Hacksell, Uli,Luthman, Kristina
experimental part, p. 4657 - 4665 (2009/12/06)
A series of analogs of the non-peptidic urotensin II receptor agonist N-[1-(4-chlorophenyl)-3-(dimethylamino)propyl]-4-phenylbenzamide (FL104) has been synthesized and evaluated pharmacologically. The enantiomers of the two most potent racemic analogues were obtained from the corresponding diastereomeric mandelic amides. In agreement with previously observed SAR, most of the agonist potency resided in the (S) enantiomers. The most potent UII receptor agonist in the new series was (S)-N-[3-dimethylamino-1-(2-naphthyl)propyl]-4-(4-chlorophenyl)benzamide (EC50 = 23 nM at the urotensin II receptor).
UII-MODULATING COMPOUNDS AND THEIR USE
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Page/Page column 47; 55, (2008/12/05)
Disclosed herein are novel aromatic-containing compounds and methods for using various aromatic-containing compounds for treatment and prevention of diseases and disorders related to the Urotensin II receptor.
