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      An α-Adrenoceptor-Blocking Action of SGB-483, a New Piperazine Antihypertensive Agent in Isolated Vascular Smooth Muscles

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          SGB (10<sup>-7</sup>–10<sup>–5</sup> M), a new piperazinyl antihypertensive agent, like prazosin (10<sup>–8_</sup>10<sup>–6</sup> M), a potent preferential α<sub>1</sub>-adrenoceptor antagonist, inhibited the contractile response of rabbit aorta to norepinephrine and methoxamine in a competitive manner whereas in the cat coronary and rabbit basilar artery, the inhibition by SGB was not a competitive one. The potency of the inhibitory action of SGB was less than that of prazosin in all preparations used. Neither SGB nor prazosin had any inhibitory effect on the response to potassium, 5-hydroxytryptamine, prostaglandin F<sub>2α</sub>, and excess Ca<sup>2+</sup> in all preparations. In the rabbit aortic membrane preparation, the specific binding of [<sup>3</sup>H]-prazosin was inhibited, concentration-dependently, by SGB with IC<sub>50</sub> value of 1.4 ± 0.09 µ M. These studies indicated that SGB has an α<sub>1-</sub>adrenoceptor-blocking action though its potency is weaker than prazosin.

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          Author and article information

          J Vasc Res
          Journal of Vascular Research
          S. Karger AG
          23 September 2008
          : 21
          : 6
          : 298-305
          Department of Pharmacology, School of Medicine, University of Hawaii, Honolulu, Hawaii, USA
          158532 Blood Vessels 1984;21:298–305
          © 1984 S. Karger AG, Basel

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          Pages: 8
          Research Paper


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