Alpha-adrenoceptor antagonistic effects and antihypertensive activity of SGB-1534 in conscious normotensive and deoxycorticosterone acetate (DOCA)-salt hypertensive dogs: comparison with prazosin.

In conscious normotensive and deoxycorticosterone acetate (DOCA)-salt hypertensive dogs, alpha-adrenoceptor antagonistic and antihypertensive actions of SGB-1534, given orally, were compared with those of prazosin. SGB-1534 and prazosin did not markedly influence systemic blood pressure (SBP) and heart rate (HR) in normotensive dogs. These alpha 1-adrenoceptor antagonists inhibited SBP and HR increases induced by i.v. adrenaline in a dose-dependent manner. In DOCA-salt hypertensive dogs, persistent hypotension, accompanied by a reflex tachycardia, occurred after oral administration of SGB-1534 and prazosin. The hypotensive activity of SGB-1534 was much more potent in magnitude and duration than that of prazosin. In isolated canine mesenteric and femoral arteries, SGB-1534, compared to prazosin, elicited a more potent inhibition on the contractile response to a relatively selective alpha 1-adrenoceptor agonist, phenylephrine. It appears that the antihypertensive activity of SGB-1534, like prazosin, is nearly in parallel with its alpha 1-adrenoceptor antagonistic effect.