Design and Synthesis of Novel Aryloxyalkyl-arylpiperazine Derivatives as α_(1A)-Adrenoceptor Antagonists

A series of 1-[2-(substituted phenoxy)ethyl]-4-(2-methoxyphenyl)-piperazine deriva- tives have been synthesized. The radioligand receptor binding assay indicated that most of them bind with α1-adrenoceptor specifically, and one of the compound possessed subtype A selectivity.

3D-QSAR study on phenoxy-alkylamine compounds of α_1-adrenoceptor antagonist

The study of three-dimensional quantitative structure-activity relationship (3D-QSAR) of DDPH and its derivatives that have been known with their activity parameters has been developed using the comparative molecular field analysis (CoMFA) method. Here, (+)-DDPH crystal structure was selected as the active conformation model and comparisons between the influences of different charge calculation methods and grid setup were conducted. The coefficients of cross-validation (q2) and regression (r2) are 0.481 and 0.997, respectively. The standard error (SE) is 0.102. The research result suggests that the steric field makes more contributions to the activity than the electrostatic field. This model can help us not only in improving our understanding of the receptor-ligand interactions, but also in predicting the activity of derivatives and designing new compounds with better potency.

膀胱颈纤维组织增生性梗阻的诊断和治疗(附30例报告)

目的 报道膀胱颈纤维组织增生导致的膀胱出口梗阻 (BOO)的诊治体会。 方法 总结膀胱颈纤维组织增生BOO病例 30例 ,均行经尿道膀胱颈部切开或膀胱颈部分切除术 ,并联合应用α1受体拮抗剂如哈乐、特拉唑嗪或哌唑嗪治疗。 结果 30例病人随访 3～ 30个月 ,排尿情况均有不同程度改善 ,平均尿流率 >15ml/s,IPSS评分 5 .3± 1.7(术前 2 5 .4± 4.2 ) ,生活质量评分 1.4± 0 .6(术前 4.1± 0 .8)。病理检查示 30例有不同程度纤维组织增生 ,其中 18例有慢性炎性改变。 结论根据临床症状、压力 流率测定和膀胱镜检诊断膀胱颈纤维组织增生性梗阻简便有效 。