Disease relevance of chlorotrianisene

• There was 13 patinets with histologically metastatic prostatic adenocarcinoma treated with a single oral dose of 80 mg. per kg. hydroxyurea every third day (based on ideal or actual weight, whichever is less) and 12.5 mg. chlorotrianisene per day [1].

High impact information on chlorotrianisene

• Inactivation of the uterine estrogen receptor binding of estradiol during P-450 catalyzed metabolism of chlorotrianisene (TACE). Speculation that TACE antiestrogenic activity involves covalent binding to the estrogen receptor [2].
• Increased inhibition of hepatic uroporphyrinogen decarboxylase by hexachlorobenzene in male rats given the oestrogenic drugs diethylstilboestrol and chlorotrianisene [3].
• Covalent binding of chlorotrianisene in hepatic microsomes is dramatically stimulated by treatment of rats with methylcholanthrene (MC), which is known to induce two major P-450 isozymes, P-450c (IA1) and P-450d (IA2) [4].
• To determine whether P-450c and/or P-450d are involved in catalysis of covalent binding of chlorotrianisene, antibodies to P-450c and P-450d were used [4].
• The epoxide hydratase inhibitor (1,1,1-trichloropropane oxide) failed to enhance covalent binding, suggesting that an epoxide of chlorotrianisene was not the reactive intermediate [5].

Biological context of chlorotrianisene

• At the dosages selected bromocriptine was more effective than chlorotrianisene in inhibiting lactation [6].
• We studied 50 postpartum patients who received chlorotrianisene (Tace) or placebo for lactation suppression in a prospective, double-blind, randomized fashion [7].
• The effects of chlorotrianisene (Tace) of kinetics of 3H-testosterone metabolism in patients with carcinoma of the prostate [8].

Anatomical context of chlorotrianisene

• Role of P-450c in the formation of a reactive intermediate of chlorotrianisene (TACE) by hepatic microsomes from methylcholanthrene-treated rats [4].

Gene context of chlorotrianisene

• Chlorotrianisene (TACE) exhibits in vitro little or no binding to the uterine estrogen receptor (ER) but demonstrates potent estrogenic activity in vivo, indicating that TACE is a proestrogen/proantiestrogen [2].
• Effect of bromocriptine and chlorotrianisene on inhibition of lactation and serum prolactin. A comparative double-blind study [6].

References