title: Vasopressin V2 (SR121463A) and V1a (SR49059) receptor antagonists both inhibit desmopressin vasorelaxing activity.
abstract: Although [Arg(8)]vasopressin is a potent vasoconstrictor, it possesses vasorelaxant properties manifested either after vasopressin V1 receptor blockade or directly in some vascular beds. The nature of the receptor involved in the vasorelaxant effect of [deamino-Cys(1) D-Arg(8)]vasopressin (desmopressin), a vasopressin V2 receptor agonist, was studied on rat precontracted aortic rings by the use of highly selective new non-peptide vasopressin receptor antagonists. The present study demonstrates for the first time that desmopressin relaxant effect is antagonized by the vasopressin V2 receptor antagonist SR121463A, but also by the vasopressin V1A receptor antagonist SR49059, suggesting that desmopressin-induced relaxation is mediated by a receptor subtype sharing both V1A and V2 pharmacological profiles.
authors.affiliation: Laboratoire de Pharmacologie et Physiopathologie Expérimentales (EA 2035), Faculté de Pharmacie, 34060, Montpellier, France.
authors.forename: I
authors.initials: I
authors.lastname: Méchaly
authors.forename: F
authors.initials: F
authors.lastname: Laurent
authors.forename: K
authors.initials: K
authors.lastname: Portet
authors.forename: J
authors.initials: J
authors.lastname: Serrano
authors.forename: G
authors.initials: G
authors.lastname: Cros
mesh_terms: D000818:Animals; D065092:Antidiuretic Hormone Receptor Antagonists; D001011:Aorta / Q000187:drug effects; D001127:Arginine Vasopressin / Q000494:pharmacology; D003894:Deamino Arginine Vasopressin / Q000494:pharmacology*; D004730:Endothelium, Vascular / Q000187:drug effects*; D006490:Hemostatics / Q000494:pharmacology*; D006727:Hormone Antagonists / Q000494:pharmacology; D007211:Indoles / Q000494:pharmacology; D008297:Male; D009025:Morpholines / Q000494:pharmacology*; D011759:Pyrrolidines / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013141:Spiro Compounds / Q000494:pharmacology*
chemical_list: D065092:Antidiuretic Hormone Receptor Antagonists; D006490:Hemostatics; D006727:Hormone Antagonists; D007211:Indoles; D009025:Morpholines; D011759:Pyrrolidines; D013141:Spiro Compounds; D001127:Arginine Vasopressin; C103281:satavaptan; C082134:relcovaptan; D003894:Deamino Arginine Vasopressin