苯乙胺类新化合物抗前列腺增生作用研究

目的：探讨具有α1-肾上腺素受体（α1-AR）拮抗作用的XBM系列苯乙胺类新化合物的体外生物活性及体内药效作用。方法：SD大鼠离体肛尾肌等张力试验，观察XBM系列新化合物的拮抗作用；流式细胞术检测XBM-21的α1-AR亚型选择性；采用大鼠前列腺增生模型，观察XBM-21的抗前列腺增生作用。结果：大部分XBM系刳新化合物具有α1-AR拮抗作用，XBM-21的pA2值为8．42。钙流筛选测得XBM-21在α1A-AR、α1B-AR和α1D—AR上的IC50值分别为71．5mmol／L、1．03μmol／L、65nmol／L，且XBM-21能明显改善大鼠前列腺增生模型的干湿重指数。结论：新化合物XBM-21具有明显的α1-AR拮抗作用，且亚型选择性较强，提示该新化合物对良性前列腺增生所引起的症状将有较好的改善作用。

Study on phenylethylamines new compounds against benign prostatic hyperplasia

To study the bioactivities in vitro and the pharmacodynamic action in vivo of XBM series phenylethylamines as α_1 -adrenocepter antagonist on be-nign prostatic hyperplasia. METHODS: The antago-nism of XBMs on isolated SD rat anococcygeus musle was observed by isometric tension experiment. The ad-renoceptor subtype selectivity of XBM-21 was identified by flow cytometry, and the effect of XBM-21 on benign prostatic hyperplasia model rats was also identified. RESULTS: Most of the XBM new compounds have antagonism on α_1-AR,the pA2 of XBM-21 was 8.42. The IC_(50) of XBM-21 on α_1 A-AR,α_1 B-AR and α_1 D-AR were 71.5 nmol/L, 1.03 μmol/L and 65 nmol/L, re-spectively. XBM-21 could obviously improve the dry and humid weight index of hyperplasia of prostate gland model rats. CONCLUSION: XBM-21 has significant antagonism on blocking α_1-adrenoceptor, it has good selectivities on α_1 A-AR and α_1 D-AR, which indicateed the new compound could better improve the symptom induced by benign prostatic hyperplasia.