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- W2276333604 abstract "Arginine vasopressin (AVP) plays as important role in control of circulation and may be involved in pathophysiology of cardiovascular diseases. Recently a novel oral V1-receptor antagonist, OPC-21268, has been produced for possible human therapeutic use (Y. Yamamure et al. Science Wash. DC 252: 572-574, 1991). OPC-21268 is a nonpeptide antagonist and inhibits AVP-induced vasoconstriction in rats and humans. In this study, we examined the influence of OPC-21268 on the sympathoinhibitory and bradycardic effects of AVP in conscious rabbits. Before OPC-21268, AVP at doses of 1, 3, 10, and 30 mU/kg decreased renal sympathetic nerve activity (RSNA) by 24 +/- 5, 40 +/- 5, 65 +/- 6 and 86 +/- 5%, respectively, and decreased heart rate from 243 +/- 10 beats/min at control to 232 +/- 11, 221 +/- 10, 197 +/- 9, and 166 +/- 6 beats/min, respectively (n = 12). Oral OPC-21268 at 30 mg/kg (n = 12) and 90 mg/kg (n = 5) did not alter the baseline values of arterial pressure, heart rate, and RSNA. After oral OPC-21268 the decreases in RSNA and heart rate evoked with AVP at graded doses were partially but significantly attenuated (P < 0.01). The attenuation of the AVP-induced decreases in RSNA and heart rate was similar between the two doses of OPC-21268. In another group of rabbits (n = 6), intravenous OPC-21268 at 30 mg/kg almost completely abolished AVP-induced decreases in heart rate and RSNA.(ABSTRACT TRUNCATED AT 250 WORDS)" @default.
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- W2276333604 date "1993-06-01" @default.
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- W2276333604 title "Effects of a novel orally effective V1-receptor antagonist, OPC-21268, on AVP-induced sympathoinhibition" @default.
- W2276333604 doi "https://doi.org/10.1152/ajpregu.1993.264.6.r1089" @default.
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