Comparative pharmacodynamic analysis of TAT-59 and tamoxifen in rats bearing DMBA-induced mammary carcinoma

Toshiyuki Toko, Jiro Shibata, Yoshikazu Sugimoto, Hidetoshi Yamaya, Masahiko Yoshida, Kazuo Ogawa, Eiji Matsushima

研究成果: Article査読

13 被引用数 (Scopus)

抄録

TAT-59 suppressed the growth fo DMBA-induced mammary tumors in rats earlier and more strongly than tamoxifen (TAM). After oral administration of the drugs, DP-TAT-59, one of the main metabolites of TAT-59, was found in 10- to 15-fold higher concentrations in both the tumor and blood compared to 4-OH-TAM, an active metabolite of TAM. In a 3-day antiuterotrophic test, every detected metabolite of TAT-59 showed stronger antiestrogenic activity than did TAM. In a competition assay, the affinity of the metabolites for estrogen receptors ranged from that of estradiol to that of TAM. These results suggest that the superior antiestrogenic activity of TAT-59 compared to TAM was either due to its higher penetration into tumor tissue or to the stronger antiestrogenic activity of its metabolites.

本文言語English
ページ(範囲)7-13
ページ数7
ジャーナルCancer Chemotherapy and Pharmacology
37
1-2
DOI
出版ステータスPublished - 1995 1 1
外部発表はい

ASJC Scopus subject areas

  • 腫瘍学
  • 毒物学
  • 薬理学
  • 癌研究
  • 薬理学(医学)

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