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[Vasopressin (ADH)].
Nihon Rinsho. Japanese Journal of Clinical Medicine
|December 1, 1992
Summary
Recent advances in vasopressin receptor molecular biology include cloning of V1a and V2 receptors. Novel antagonists, OPC-21268 and OPC-31260, show potential for treating cardiovascular disorders and SIADH.
Area of Science:
- Molecular endocrinology
- Receptor pharmacology
- Renal physiology
Context:
- Vasopressin (arginine vasopressin) is crucial for water-electrolyte balance and renal hemodynamics.
- Significant progress has been made in understanding vasopressin receptor molecular biology.
- Previous research identified the roles of vasopressin in physiological regulation.
Purpose:
- To report the cloning of complementary DNA (cDNA) for rat liver V1a and kidney V2 arginine vasopressin receptors.
- To describe the characteristics of the cloned receptors and their messenger RNA (mRNA) distribution.
- To review the development and potential applications of novel vasopressin receptor antagonists.
Summary:
- The V1a receptor cDNA encodes a protein with seven transmembrane domains, found in tissues expressing V1a receptors.
- The V2 receptor cDNA encodes a G protein-coupled receptor, with its mRNA detected exclusively in the kidney.
- Orally active antagonists OPC-21268 (V1 antagonist) and OPC-31260 (V2 antagonist) have been developed.
Impact:
- OPC-21268 inhibits vasopressin-induced vasoconstriction, suggesting potential for hypertensive cardiovascular disorders.
- OPC-31260 inhibits the antidiuretic action of vasopressin, indicating utility in treating SIADH.
- These findings advance the understanding of vasopressin signaling and pave the way for new therapeutic strategies.