Satake N, Shibata S, Suh T K, Flores F
Blood Vessels. 1984;21(6):298-305. doi: 10.1159/000158532.
SGB (10(-7)-10(-5) M), a new piperazinyl antihypertensive agent, like prazosin (10(-8)-10(-6) M), a potent preferential alpha 1-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 F2 alpha, and excess Ca2+ in all preparations. In the rabbit aortic membrane preparation, the specific binding of [3H]-prazosin was inhibited, concentration-dependently, by SGB with IC50 value of 1.4 +/- 0.09 microM. These studies indicated that SGB has an alpha 1-adrenoceptor-blocking action though its potency is weaker than prazosin.
新型哌嗪基抗高血压药物SGB（10⁻⁷ - 10⁻⁵M），与强效选择性α₁肾上腺素受体拮抗剂哌唑嗪（10⁻⁸ - 10⁻⁶M）一样，以竞争性方式抑制兔主动脉对去甲肾上腺素和甲氧明的收缩反应，而在猫冠状动脉和兔基底动脉中，SGB的抑制作用并非竞争性的。在所使用的所有制剂中，SGB抑制作用的效力均低于哌唑嗪。在所有制剂中，SGB和哌唑嗪对钾、5-羟色胺、前列腺素F2α及过量Ca²⁺的反应均无抑制作用。在兔主动脉膜制剂中，SGB浓度依赖性地抑制[³H] - 哌唑嗪的特异性结合，IC50值为1.4 ± 0.09μM。这些研究表明，SGB具有α₁肾上腺素受体阻断作用，尽管其效力比哌唑嗪弱。
