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. 1992 Jan 24;35(2):374-8.
doi: 10.1021/jm00080a025.

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

B R Venepalli  1 , 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, et al.
Affiliations

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

B R Venepalli et al. J Med Chem. .

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.

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