Journal of Medicinal Chemistry 1992-01-24

Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles.

B R Venepalli, L D Aimone, K C Appell, M R Bell, J A Dority, R Goswami, P L Hall, V Kumar, K B Lawrence, M E Logan

Index: J. Med. Chem. 35 , 374, (1992)

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Abstract

Several heterosteroids containing a dihydroethisterone skeleton were prepared and shown to displace substance P in a receptor binding assay. Further biochemical (kinetic and Scatchard analyses) and pharmacological evaluation (substance P-induced plasma extravasation and salivation in the rat) of a representative example in this series (5a) established that these compounds are competitive antagonists at the substance P receptor.