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Abstract

Photoreactive analogues of vasopressin have been synthesized and used to identify vasopressin receptor proteins in plasma membranes from different target organs (1,2):V₁ vasopressin receptors (coupled to Ca²⁺ -mobilization) in rat liver and V₂ vasopressin receptors (coupled to adenylate cyclase) in kidney medulla from different mammalian species. The question as to whether vasopressin agonists and antagonists interact with the same subunits of vasopressin receptor proteins remains open. Furthermore, at present we have no information which amino acid residues in the vasopressin molecule are close to the hormone binding site in the hormone-receptor complex. In this report we describe the synthesis of potent photoreactive vasopressin agonists and antagonists an their employment in receptor studies to answer these questions.