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ebeinone系从王贝母(Fritillaria imperialis)中分离的生物碱,具甾体样结构。已知ebeinone为一种毒蕈碱类受体拮抗剂,为筛选对受体亚型有特异拮抗作用的有效药物。作者研究了该化合物对不同动物、不同器官受体的作用。结果:①在功能性研究中,ebeinone能拮抗氯化氨甲酰胆碱反应,其对豚鼠左心房心肌M_2受体的作用强度比回肠和气管平滑肌M-3受体高10倍,离散常数K_B分别为77.3、931.1和547.0nM。②ebeinone非选择性地拮抗~3H-N—甲基东莨菪碱与大鼠动脉匀浆的结合,K_1为80.9nM。另一甾体样结构物质双哌雄双酯对毒蕈碱类M_2受体的K_B值与ebeinone相似,经比较发现,两种物质均能延迟~3H-N-甲基东莨菪碱在主动脉的离散率,表明对M_2受体存在变构样相互作
Ebeinone is an alkaloid isolated from Fritillaria imperialis and has a steroid-like structure. It is known that ebeinone is a muscarinic receptor antagonist and is an effective drug for screening specific receptor antagonists. The authors studied the effects of the compound on different animal and organ receptors. RESULTS: 1 In the functional study, ebeinone was able to antagonize the carbamoylcholine response. The intensity of its action on left ventricle myocardium M2 receptors in guinea pigs was ten times higher than that of ileal and tracheal smooth muscle M-3 receptors, and the discrete constant K_B. They were 77.3, 931.1, and 547.0 nM, respectively. 2ebeinone non-selectively antagonized the binding of ~3H-N-methylscopolamine to rat arterial homogenates, Kl was 80.9 nM. The other steroid-like structure substance, bipipedodioldioate, has a similar K_B value to the muscarinic M2 receptor as ebeinone. After comparison, both substances can delay the dispersion of ~3H-N-methylscopolamine in the aorta. Rate, indicating that there is a metamorphic interaction with M_2 receptors