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

…, JA Dority, R Goswami, PL Hall, V Kumar…

Index: Venepalli; Aimone; Appell; Bell; Dority; Goswami; Hall; Kumar; Lawrence; Logan; Scensny; Seelye; Tomczuk; Yanni Journal of Medicinal Chemistry, 1992 , vol. 35, # 2 p. 374 - 378

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Citation Number: 63

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 (58) established that these compounds are competitive antagonists at the substance P ...