182133-27-3
基本信息
Ly 353381
Ly 353381 HCl
ARZOXIFENE HCL
Arzoxifene hydrochloride
NHSNLUIMAQQXGR-UHFFFAOYSA-N
2-(p-Methoxyphenyl)-3-(p-(2-(1-piperidinyl)ethoxy)phenoxy)benzo(B)thiophene-6-ol hydrochloride
2-(4-Methoxyphenyl)-3-(4-(2-(1-piperidinyl)ethoxy)phenoxy)benzo(B)thiophene-6-ol hydrochloride
Benzo(B)thiophene-6-ol, 2-(4-methoxyphenyl)-3-(4-(2-(1-piperidinyl)ethoxy)phenoxy)-, hydrochloride
常見(jiàn)問(wèn)題列表
Estrogen receptor
Arzoxifene inhibits cell growth as effectively as the antiestrogen tamoxifen. Northern analysis reveals that arzoxifene exerts a statistically significant inhibition of pS2 and progesterone receptor B mRNA expression. Significant agonistic effect is observed on the antitrypsin mRNA expression. In contrast to estradiol and tamoxifen, arzoxifene does not upregulate cathepsin D mRNA and protein expression.
Arzoxifene prevents the ovariectomy-induced increase in body weight and serum cholesterol levels of treated rats and lowers them to below sham levels in a dose dependent manner, with maximum efficacy similar to estrogen or raloxifene. Arzoxifene (LY353381.HCl) prevents loss of bone due to ovariectomy with an ED 50 of about 0.01 mg/kg with maximal efficacy observed at 0.1-1 mg/kg/day. Arzoxifene (LY353381.HCl) antagonizes the estrogen-induced elevation in uterine weight down to vehicle-dosed control levels with ED 50 of 0.03 mg/kg/day.