Study on phenylethylamines new compounds against benign prostatic hyperplasia

Abstract

Abstract: AIM: To study the bioactivities in vitro and the pharmacodynamic action in vivo of XBM series phenylethylamines as α₁-adrenocepter antagonist on benign prostatic hyperplasia.METHODS: The antagonism of XBMs on isolated 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 71.5 nmol/L, 1.03 μmol/L and 65 nmol/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-adrenoceptor, it has good selectivities on α₁A-AR and α₁D-AR, which indicateed the new compound could better improve the symptom induced by benign prostatic hyperplasia.

Key words: benign prostatic hyperplasia (BPH), isolated rat anococcygeus musle, α₁-adrenoceptor antagonist, calcium influx screening essay

CLC Number:

R965.2

WANG Rong-rong, JIANG Zhen-zhou, XI Bao-min, WANG Tao, LIU Jing, LIANG Zhongliang, ZHANG Lu-yong. Study on phenylethylamines new compounds against benign prostatic hyperplasia[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2009, 14(7): 726-735.

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