Relative potency of antiandrogens with reference to intracellular testosterone in the rat prostate

Prostate

Volumn 29, Issue 3, 1996, Pages 146-152

  Kondo, Yasushi ^a   Homma, Yukio ^a   Aso, Yoshio ^a   Kawabe, Kazuki ^a   Mieda, Mamoru ^b   Takahashi, Hiroo ^b  

^a UNIVERSITY OF TOKYO   (Japan)

^b Grelan Pharmaceutical Co Ltd   (Japan)

Author keywords

antiandrogen; prostate; relative potency; testosterone

Indexed keywords

ANTIANDROGEN; CHLORMADINONE ACETATE; CYPROTERONE ACETATE; FLUTAMIDE; OSATERONE ACETATE; TESTOSTERONE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG POTENCY; MALE; NONHUMAN; PRIORITY JOURNAL; PROSTATE; RAT; TESTOSTERONE METABOLISM; WEIGHT GAIN;

ANDROGEN ANTAGONISTS; ANIMALS; INTRACELLULAR MEMBRANES; MALE; ORCHIECTOMY; ORGAN SIZE; PROSTATE; RATS; RATS, WISTAR; TESTOSTERONE; TISSUE DISTRIBUTION;

EID: 0029840529     PISSN: 02704137     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1097-0045(199609)29:3<146::AID-PROS1>3.0.CO;2-C     Document Type: Article

References (19)

1. Miquel J, Gilbert J: A chemical classification of nonsteroidal antagonists of sex-steroid hormone action. J Steroid Biochem 31:524-544, 1988.
2. Crawford ED, Eisenberger MA, McLeod DG, Spaulding JT, Benson R, Dorr FA, Blumenstein BA, Davis MA, Goodman PJ: A controlled trial of leuprolide with and without flutamide in prostatic carcinoma. N Engl J Med 321:419-424, 1989.
3. Labrie F, Dupont A, Cusan L, Gomez J, Emond J, Monfette G: Combination therapy with flutamide and medical (LHRH agonist) or surgical castration in advanced prostate cancer: 7-year clinical experience. J Steroid Biochem Mol Biol 37:943-950, 1990.
4. Johansson JE, Lingardth G, Andersson SO, Zador G, Beckman KW: Clinical evaluation of flutamide and estramustine as initial treatment of metastatic carcinoma of prostate. Urology 29:55-59, 1987.
5. Moguilewsky M, Cotard M, Proulx L, Tournemine C, Raynaud JP: What is an antiandrogen and what is the physiological and pharmacological rationale for combined "castration" + "antiandrogen" therapy. Prog Clin Biol Res 243A:315-340, 1987.
6. Brogden RN, Clissold SP: Flutamide. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in advanced prostatic cancer. Drugs 38:185-203, 1989.
7. Takezawa Y, Fukabori Y, Yamanaka H, Mieda M, Honma S, Kushitani M, Hamataki N: Effects of the new steroidal antiandrogen TZP-4238 on hormone-induced canine prostatic hyperplasia. Prostate 21:315-329, 1992.
8. Callaway TW, Bruchovsky N, Rennie PS, Comeau T: Mechanisms of action of androgens and antiandrogens: Effects of antiandrogens on translocation of cytoplasmic androgen receptor and nuclear abundance of dihydrotestosterone. Prostate 3:599-610, 1982.
9. Honma S, Iwamura S, Iizuka K, Kambegawa A, Shida K: Identification and antiandrogenic activity of the metabolites of 17 alpha-acetoxy-6-chloropregna-4,6-diene-3,20-dione (chlormadinone acetate) in the rat, rabbit, dog and man. Chem Pharm Bull (Tokyo) 25:2019-2021, 1977.
10. Shibata K, Takegawa S, Koizumi N, Yamakoshi N, Shimazawa E: Antiandrogen. I. 2-azapregnane and 2-oxapregnane steroids. Chem Pharm Bull (Tokyo) 40:935-941, 1992.
11. Duax WL, Griffin JF, Weeks CM, Wawrzak Z: The mechanism of action of steroid antagonists: Insights from crystallographic studies. J Steroid Biochem 31: 481-492, 1988.
12. Starka L, Hampl R, Kasal A, Kohout L: Androgen receptor binding and antiandrogenic activity of some 4,5-secoandrostanes and ring B cyclopropanoandrostanes. J Steroid Biochem 17:331-334, 1982.
13. Szego CM, Sjostrand BM, Seeler BJ, Baumer BJ, Sjostrand FS: Microtubular and plasmalemmal reorganization: acute response to estrogen. Am J Physiol 254:775-785, 1988.
14. Kontula KK, Seppanen PJ, van Duyne P, Bardin CW, Janne OA: Effect of a nonsteroidal antiandrogen, flutamide, on androgen receptor dynamics and ornithine decarboxylase gene expression in mouse kidney. Endocrinology 116:226-233, 1985.
15. Labrie F: Mechanism of action and pure antiandrogenic properties of flutamide. Cancer 72:3816-3827, 1993.
16. Fawell SE, Lees JA, White R, Parker MG: Inhibition of estrogen receptor-DNA binding by the "pure" antiestrogen ICI164,384 appears to be mediated by impaired receptor dimerization. Proc Natl Acad Sci USA 87: 6883-6887, 1990.
17. Baulieu EE: Steroid hormone antagonists at the receptor level: A role for the heat-shock protein MW 90,000 (hsp 90). J Cell Biochem 35:161-174, 1987.
18. Belis JA, Lizza EF, Tarry WF: Progesterone receptors in the prostate. Prog Clin Biol Res 145:345-361, 1984.
19. Ojasoo T, Delettre J, Mornon JP, Turpin VC, Raynaud JP: Towards the mapping of the progesterone and androgen receptors. J Steroid Biochem 27:255-269, 1987.