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Comparative Study
. 2009 Apr 15;19(8):2206-10.
doi: 10.1016/j.bmcl.2009.02.126. Epub 2009 Mar 9.

A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties

Neil Moss  1 , Younggi Choi, Derek Cogan, Adam Flegg, Andreas Kahrs, Pui Loke, Orietta Meyn, Raj Nagaraja, Spencer Napier, Ashley Parker, J Thomas Peterson, Philip Ramsden, Christopher Sarko, Donna Skow, Josh Tomlinson, Heather Tye, Mark Whitaker
Affiliations
Comparative Study

A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties

Neil Moss et al. Bioorg Med Chem Lett. .

Abstract

We have been exploring the potential of 5-HT(2B) antagonists as a therapy for chronic heart failure. To assess the potential of this therapeutic approach, we sought compounds possessing the following attributes: (a) potent and selective antagonism of the 5-HT(2B) receptor, (b) low impact of serum proteins on potency, and (c) desirable pharmacokinetic properties. This Letter describes our investigation of a biphenyl benzimidazole class of compounds that resulted in 5-HT(2B) antagonists possessing the above attributes. Improving potency in a human serum albumin shift assay proved to be the most significant SAR discovery.

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