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Conformationally-restricted ligands for the histamine H1 receptor
C Upton1, R H Osborne, M Jaffar
1Department of Pharmacy and Pharmacology, University of Bath, UK. c.upton@bath.ac.uk
Bioorganic & Medicinal Chemistry Letters
|June 24, 2000
Abstract:
Potent H1-antagonistic activity in a series of novel indeno[2,1-c]pyridines and their 4-arylpiperidinol precursors is reported; one compound shows an in vitro activity four times that of the standard mepyramine that it was screened against. Their failure to translate this protection to in vivo tests is discussed.