几类α_1-肾上腺素受体拮抗剂体外生物活性的实验研究

Experimental Study of the Biological Activities of Several α_1-Adrenoceptor Antagonists in vitro

目的 :研究几类α1 肾上腺素受体拮抗剂的体外生物活性。 方法 :分离雄性SD大鼠 (30 0～ 35 0g)肛尾肌 ,置于盛Krebs液 (37℃、pH 7.4 )的 2 0ml浴槽内 ,静息负荷 1g ,平衡 1h。完全冲洗后 ,测定肛尾肌标本对浓度增加的受试化合物收缩功能的应答 ,求出pA2 值。 结果 :部分目标化合物具有一定的α1 肾上腺素受体拮抗活性。结论 :化合物WBⅣ 1和WBⅣ 3活性较好 ,值得进一步研究。

Objective: To study the biological activities of several α 1-adrenoceptor antagonists in vitro. Methods: The anococcygeal muscle from male Sprague-Dawley rats (300～350 g) was isolated, removed and suspended in a 20-ml organ chamber containing Krebs solution at 37 ℃, pH 7.4. The muscle preparations were set at a resting tension of 1.0 g and allowed to equilibrate for 1 h in the Krebs solution. After thorough washing, the anococcygeal muscle preparations were examined for the effects of the tested compounds with increased concentrationson its contractile/relaxant responses and the pA 2 of antagonistic activity was assessed. Results: Some of the target compounds displayed blocking activity to α 1-adrenoceptor. Conclusion: Compounds WBⅣ-1 and WBⅣ-3 showed good inhibiting activity,and were worth further studying.