Investigations into the mechanism of the antihypertensive effect of SGB-1534, a novel .ALPHA.1-adrenoceptor antagonist, in rats.
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概要
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Experiments in vitro and in vivo were undertaken to examine possible involvement of a central effect in the hypotensive mechanism of SGB-1534. SGB-1534 selectively antagonized the contraction of isolated rat aortae to phenylephrine with a pA<SUB>2</SUB> value of 10.57, 3.9 times higher than prazosin, and markedly displaced the α<SUB>1</SUB>-adrenoceptor ligand <SUP>3</SUP>H-prazosin (pK<SUB>1</SUB>: 8.81) in rat brain. In anesthetized spontaneously hypertensive rats (SHRs), SGB-1534 (0.3-3 μg/kg) and prazosin (3-30 μg/kg) given intravenously (i.v.) and intracerebroventricularly (i.c.v.) produced a dose-dependent and long-lasting depressor response associated with no change in heart rate (HR). The two drugs (i.c.v.), however, significantly attenuated the pressor response to i.v. noradrenaline. Single i.v. injections of SGB-1534, prazosin and yohimbine dose-dependently inhibited the St 587 (a highly specific and centrally acting α<SUB>1</SUB>-adrenoceptor agonist) enhanced flexor reflex and the pressor response to i.v. phenylephrine in pithed rats. However, the activities of SGB-1534 and prazosin in inhibiting the St 587-enhanced flexor reflex were 16, 000 and 660 times, respectively, less than those in attenuating the pressor response to i.v. phenylephrine. It seems that the hypotensive action of SGB-1534 is due to the peripheral α<SUB>1</SUB>-adrenoceptor antagonistic mechanism rather than the central one.
- 公益社団法人 日本薬理学会の論文
著者
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SAKAI Kazushige
Departinent of Pharmacology, Research Laboratories, Chugai Pharmaceutical Co.
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AONO Junichiro
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Nagasaki University
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SAKAI Kazushige
Department of Pharmacology, Fujigotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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