中国临床药理学与治疗学2009，Vol.14Issue(7)：726-731,6.
苯乙胺类新化合物抗前列腺增生作用研究
Study on phenylethylamines new compounds against benign prostatic hyperplasia
摘要
Abstract
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.关键词
良性前列腺增生/离体肛尾肌/α_1-肾上腺素受体/钙流筛选模型Key words
benign prostatic hyperplasia (BPH)/ isolated rat anococcygeus musle/ α_1-adrenoceptor an-tagonist/ calcium influx screening essay分类
医药卫生引用本文复制引用
王荣荣,江振洲,习保民,王涛,刘晶,梁忠良,张陆勇..苯乙胺类新化合物抗前列腺增生作用研究[J].中国临床药理学与治疗学,2009,14(7):726-731,6.基金项目
国家自然科学基金资助(30690776) （30690776）
