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- W917814275 abstract "The only compounds with antagonistic activity via AT₁, receptor, one of two subtypes of angiotensin II (AII) receptor, have been demonstrated to block the vasoconstriction effects of All and thereby provide therapeutic potential. This initiated the search for compounds with high specific affinity to ATI receptor and their effective screening methods. The radioligand binding assay for the All receptor is regarded as the primary method for the evaluation of AT₁ receptor antagonists for their activity. In this paper, we characterized the liver AT₁, receptor and describe the efficient method of the radioligand binding assay using rat liver as a source of AT₁ receptor. Equilibrium binding studies with rat adrenal cortex, adrenal medulla, liver and bovine adrenal showed that the specific bindings of [³H] All were saturable in all tissues and the Scatchard plots of those data were linear, suggesting a single population of binding sites. Hill slopes were very near to the unity in all tissues. Kinetic studies of [³H] All binding in rat liver homogenates yielded two association rate constants, 4.10 X 10^7 M^(-1)min^(-1) and 4.02 X 10^9 M^(-1)min^(-1), with a single dissociation rate constant, 7.07 X 10^(-3) min^(-1), possibly due to the partial dissociation phenomenon. The rank order of inhibition potencies of [³H] All binding in rat liver was All>Sarile>Losartan>PD 123177. Rat liver homogenates revealed to have very high density of homogeneous population of the AT₁, receptor subtype, as the specifically bound [³H] All was not inhibited by PD 123177, the nonpeptde antagonist of AT₂. The results of this study demonstrated that the liver homogenates from rats could be the best receptor preparation for the AT₁1 receptor binding assay and provide an efficient system for the screening of newly synthesized candidate compounds of AT₁, receptor antagonist." @default.
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- W917814275 date "1995-01-01" @default.
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- W917814275 title "Rat Liver $AT_1$ Receptor Binding Analysis for Drug Screening" @default.
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