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

作　　者：王荣荣[1] 江振洲[1,2] 习保民[3] 王涛[1,4] 刘晶[1] 梁忠良[1] 张陆勇[1,2] 

机构地区：[1]中国药科大学江苏省新药筛选中心 [2]药物质量与安全预警教育部重点实验室(中国药科大学) [3]南方医科大学药学院药物化学系 [4]江苏省药效研究与评价服务中心

出　　处：《中国临床药理学与治疗学》2009年第7期726-731,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家自然科学基金资助(30690776)

摘　　要：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系列新化合物具有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71.5 nmol/L、1.03μmol/L、65 nmol/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。AIM： To study the bioactivities in vitro and the pharmaeodynamic action in vivo of XBM series phenyiethylamines as α1-adrenocepter antagonist on benign prostatic hyperplasia.METHODS ：The antagonism of XBMs on： isoiated, SD rat anococcygeus musle was observed by isometric tension experiment. The adrenoceptor 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 α1-AR,the pA2 of XBM-21 was,8.42.The IC50 of XBM-21 on α1A-AR,α1B-AR and α1D-AR were 71.5nmol/L,1.03μmol/L and 65nmol/L,respectively.XBM-21 could obviously improve the dry and humid weight index of hyperplasia of prostate gland model rats. CONCLUSION ： XBM-21 has siginificant antagonism on blocking α1-adrenoeeptor, it has good selectivities on α1 A-AR and α1 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 α1-肾上 腺素受体 钙流筛选模型 

分 类 号：R965.2[医药卫生—药理学]