Discovery and preliminary pharmacology of Sch 37370, a dual antagonist of PAF and histamine.

Autor: Motasim Billah, M., Egan, Robert, Ganguly, Ashit, Green, Michael, Kreutner, William, Piwinski, John, Siegel, Marvin, Villani, Frank, Wong, Jesse
Zdroj: Lipids; Dec1991, Vol. 26 Issue 12, p1172-1174, 3p
Abstrakt: From a series of amide analogs of the histamine H antagonist, azatadine, a potent, orally active, dual platelet-activating factor (PAF) and histamine antagonist, Sch 37370, namely 1-acetyl-4-(8-chloro-5,6-dihydro-11 H-benzo-[5,6]cyclohepta[1,2-b]pyridin-11-ylidine)piperidine, was discovered. Sch 37370 selectively inhibits PAF-induced aggregation of human platelets in vitro (IC=0.6 μM), and in vivo inhibits PAF- and histamine-induced bronchospasm in guinea pigs with ED values of 6.0 and 2.4 mg/kg p.o., respectively. Sch 37370 is expected to be more efficacious than single mediator antagonists in allergic diseases, such as asthma. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index