文章基本信息

标题：Binding Characteristics of α1-Adrenoceptors in Bovine Prostate Using a Radioligand Binding Assay
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作者：Keiko MARUYAMA ; Junji KINAMI ; Hiroshi TSUCHIHASHI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1991
卷号：14
期号：6
页码：315-319
DOI：10.1248/bpb1978.14.315
出版社：The Pharmaceutical Society of Japan
摘要：Binding characteristics of α₁-adrenoceptors in the bovine prostate were examined using a radioligand binding assay. [³H] Bunazosin was used as a radioligand. The optimal incubation conditions for the radioligand binding assay were determined : incubation time (30 min), protein concentration (0.2 mg/tube) and temperature (30°C). Scatchard plots for α₁-adrenoceptors in bovine prostates were linear and the K_d and B_max values were 0.61 nM and 49.8 fmol/mg protein, respectively. The pK_i value of terazosin was significantly higher than those of prazosin, bunazosin or phentolamine in the bovine prostate. Since this radioligand binding assay using [³H] bunazosin demonstrated the presence of α₁-adrenoceptors in bovine prostates, this method is useful for the assessment of α₁-blockers of new chemicals synthesized for the treatment of the benign prostatic hyperplasia.
关键词：bunazosin