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Comparative Study
. 1991 Dec;26(12):1172-4.
doi: 10.1007/BF02536525.

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

M M Billah  1 , R W Egan, A K Ganguly, M J Green, W Kreutner, J J Piwinski, M I Siegel, F J Villani, J K Wong
Affiliations
Comparative Study

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

M M Billah et al. Lipids. 1991 Dec.

Abstract

From a series of amide analogs of the histamine H1 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-11H-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 (IC50 = 0.6 microM), and in vivo inhibits PAF- and histamine-induced bronchospasm in guinea pigs with ED50 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.

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