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Minimization of potential hERG liability in histamine H3 receptor antagonists.

Authors :
Black, L. A.
H. Liu
Diaz, G. J.
Fox, G. B.
Browman, K. E.
J. Wetter
Marsh, K. C.
Miller, T. R.
Esbenshade, T. A.
J. Brioni
Cowart, M. D.
Source :
Inflammation Research; Apr2008, Vol. 57 Issue 0, p45-46, 2p
Publication Year :
2008

Abstract

The article presents a research study on the medical chemistry strategy that produced histamine H<subscript>3</subscript> selectivity relative to the hERG potassium channel involved in cardiac repolarization. It describes the assessment of pharmacokinetic profiles of the male rats. It states that the polarity in form of heterocycles were able to minimize hERG interaction while preserving behavioral efficacy.

Details

Language :
English
ISSN :
10233830
Volume :
57
Issue :
0
Database :
Complementary Index
Journal :
Inflammation Research
Publication Type :
Academic Journal
Accession number :
32952231
Full Text :
https://doi.org/10.1007/s00011-007-0622-2