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Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.

Abstract：

:An inactin-anesthetized rat cardiovascular (CV) assay was employed in a screening mode to triage multiple classes of melanin-concentrating hormone receptor 1 (MCHr1) antagonists. Lead identification was based on a compound profile producing high drug concentration in both plasma (>40 microM) and brain (>20 microg/g) with <15% change in cardiovascular endpoints. As a result of these stringent requirements, lead optimization activities on multiple classes of MCHr1 antagonists were terminated. After providing evidence that the cardiovascular liabilities were not a function of MCHr1 antagonism, continued screening identified the chromone-substituted aminopiperidine amides as a class of MCHr1 antagonists that demonstrated a safe cardiovascular profile at high drug concentrations in both plasma and brain. The high incidence of adverse cardiovascular effects associated with an array of MCHr1 antagonists of significant chemical diversity, combined with the stringent safety requirements for antiobesity drugs, highlight the importance of incorporating cardiovascular safety assessment early in the lead selection process.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Kym PR,Souers AJ,Campbell TJ,Lynch JK,Judd AS,Iyengar R,Vasudevan A,Gao J,Freeman JC,Wodka D,Mulhern M,Zhao G,Wagaw SH,Napier JJ,Brodjian S,Dayton BD,Reilly RM,Segreti JA,Fryer RM,Preusser LC,Reinhart GA,Hernand

doi

10.1021/jm0512286

keywords:

subject

Has Abstract

pub_date

2006-04-06 00:00:00

pages

2339-52

issue

7

eissn

0022-2623

issn

1520-4804

journal_volume

49

pub_type

杂志文章

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