Blood Pressure-Lowering Effect of an Orally Active Vasopressin V1 Receptor Antagonist in Mineralocorticoid Hypertension in the Rat

We studied the contribution of vasopressin to the maintenance of high blood pressure in deoxycorticosterone acetate (DOCA)-salt hypertension in the rat using the nonpeptide orally effective vasopressin VI receptor antagonist OPC-21268. Binding kinetic studies demonstrated that oral OPC-21268 (30 mg/...

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Veröffentlicht in:	Hypertension (Dallas, Tex. 1979) Tex. 1979), 1994-06, Vol.23 (6, Part 1), p.737-743
Hauptverfasser:	Burrell, Louise M, Phillips, Paddy A, Stephenson, J M, Risvanis, J, Rolls, K A, Johnston, C I
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antidiuretic Hormone Receptor Antagonists Arginine Vasopressin - metabolism Binding Sites Blood Pressure - drug effects Desoxycorticosterone Female Hypertension - chemically induced Hypertension - physiopathology Kinetics Mesenteric Arteries - drug effects Piperidines - pharmacology Quinolones - pharmacology Rats Rats, Sprague-Dawley Receptors, Vasopressin - classification Sodium Chloride Systole Vascular Resistance - drug effects
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Zusammenfassung:	We studied the contribution of vasopressin to the maintenance of high blood pressure in deoxycorticosterone acetate (DOCA)-salt hypertension in the rat using the nonpeptide orally effective vasopressin VI receptor antagonist OPC-21268. Binding kinetic studies demonstrated that oral OPC-21268 (30 mg/kg) acted as a competitive antagonist at the vasopressin VI receptor in DOCA-salt and salt control rats. Basal mean intra-arterial blood pressure was 140±4 mmHg (n=12) in DOCA-salt rats compared with 111±2 mm Hg in salt control rats (n=18). Acute oral OPC-21268 (30 mg/kg) significantly (P
ISSN:	0194-911X 1524-4563
DOI:	10.1161/01.hyp.23.6.737