Appelgren L E, Forsgren B, Gustafsson J A, Pousette A, Högberg B
Acta Pharmacol Toxicol (Copenh). 1978 Nov;43(5):368-74. doi: 10.1111/j.1600-0773.1978.tb02280.x.
The alkylating agent 3H-estramustine was administered to castrated male rats and found to accumulate in the epithelium of the ventral prostate 5 and 20 min. following intravenous administration, as judged from autoradiography. Four hrs. after intravenous injection of this isotope, the radioactivity was recovered in the secretion of the prostatic lobuli. A preferential accumulation of radioactivity in prostatic secretion was also observed 2 hrs. after intramuscular administration of 3H-estramustine to intact or castrated rats. In contrast, 3H-oestradiol and 3H-testosterone, which were also taken up by the ventral prostatic epithelium, were not recovered in prostatic secretion. The present results indicate that 3H-estramustine is secreted from the prostatic cells into the lumina of the prostatic lobuli. It is speculated that a recently detected estramustine-binding protein in rat ventral prostate may be involved in this process and that the present finding may be of relevance in the understanding of the mechanism of action of the chemotherapeutic agent Estracyt (estramustine phosphate) used in the treatment of advanced prostatic carcinoma.
将烷化剂3H-雌莫司汀给予去势雄鼠,经放射自显影判断,静脉注射后5分钟和20分钟,该药在前列腺腹叶上皮中蓄积。静脉注射该同位素4小时后,在前列腺小叶的分泌物中检测到放射性。给完整或去势大鼠肌肉注射3H-雌莫司汀2小时后,也观察到放射性在前列腺分泌物中有优先蓄积。相比之下,同样被前列腺腹叶上皮摄取的3H-雌二醇和3H-睾酮,并未在前列腺分泌物中检测到。目前的结果表明,3H-雌莫司汀从前列腺细胞分泌到前列腺小叶管腔中。推测最近在大鼠前列腺腹叶中检测到的雌莫司汀结合蛋白可能参与了这一过程,并且目前的发现可能有助于理解用于治疗晚期前列腺癌的化疗药物癌腺治(磷酸雌莫司汀)的作用机制。