In vivo and in vitro characterisation of a nonpeptide vasopressin V(1A) and V2 receptor antagonist (YM087) in the rat

Abstract

This paper reports the in vitro and in vivo characterisation of a nonpeptide, orally active, vasopressin V(1A) and V2 receptor antagonist, YM087 (methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzoazepine-6-carbonyl)-2- phenylbenzanilide monohydrochloride) in the rat. YM087 dose dependently displaced the vasopressin V(1A) receptor antagonist radioligand, 125I- labelled [d(CH2)5,sarcosine7]vasopressin at vasopressin V(1A) receptors in liver and kidney medulla membranes and caused a concentration dependent displacement of the vasopressin V2 receptor antagonist radioligand [3H]desGly-NH2/9[d(CH2)5, D-Ile2, Ile4]vasopressin at vasopressin V2 receptors in kidney medulla membranes. In vitro binding ki..