Conformationally-restricted ligands for the histamine H1 receptor.
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.
Upton
C
C
Department of Pharmacy and Pharmacology, University of Bath, UK. c.upton@bath.ac.uk
Osborne
R H
RH
Jaffar
M
M
D000818:Animals; D006168:Guinea Pigs; D017442:Histamine Agonists / Q000378:metabolism*; D066298:In Vitro Techniques; D008024:Ligands; D008968:Molecular Conformation; D011725:Pyridines / Q000737:chemistry / Q000378:metabolism*; D011969:Receptors, Histamine H1 / Q000378:metabolism*
D017442:Histamine Agonists; D008024:Ligands; D011725:Pyridines; D011969:Receptors, Histamine H1