Pharmacodynamics of selective androgen receptor modulators

Journal of Pharmacology and Experimental Therapeutics

Volumn 304, Issue 3, 2003, Pages 1334-1340

  Yin, Donghua ^a   Gao, Wenqing ^a   Kearbey, Jeffrey D ^a   Xu, Huiping ^a   Chung, Kiwon ^b   He, Yali ^b   Marhefka, Craig A ^b   Veverka, Karen A ^c   Miller, Duane D ^b   Dalton, James T ^a,d  

^a OHIO STATE UNIVERSITY   (United States)

^b UNIVERSITY OF TENNESSEE HEALTH SCIENCE CENTER   (United States)

^c GTx Inc   (United States)

^d LM Parks Hall ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 CHLORO 2,4 DIHYDROXYPYRIDINE PLUS OXONATE POTASSIUM PLUS TEGAFUR; ANDROGEN RECEPTOR; DIMETHYL SULFOXIDE; FOLLITROPIN; LUTEINIZING HORMONE; MACROGOL; MEGESTROL ACETATE; PHTHALIDE; S 2; SELECTIVE ANDROGEN RECEPTOR MODULATOR; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TESTOSTERONE PROPIONATE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BIOSYNTHESIS; CASTRATION; CHIRALITY; CONTROLLED STUDY; DOSE TIME EFFECT RELATION; DRUG ACTIVITY; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG SELECTIVITY; EVALUATION; GENE EXPRESSION REGULATION; HORMONE ACTION; HORMONE RECEPTOR INTERACTION; ISOMERISM; LEVATOR ANI MUSCLE; MALE; MUSCLE MASS; NONHUMAN; ORGAN WEIGHT; PRIORITY JOURNAL; PROSTATE; RAT; REFERENCE VALUE; REPORTER GENE; SEMINAL VESICLE; SYNTHESIS; TISSUE SPECIFICITY;

ANILIDES; ANIMALS; GONADAL STEROID HORMONES; MALE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, ANDROGEN; TESTOSTERONE;

EID: 0037371461     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.102.040840     Document Type: Article

References (31)

1. Bagatell CJ and Bremner WJ (1996) Androgens in men-uses and abuses. N Engl J Med 334:707-714.
2. Battmann T, Branche C, Bouchoux F, Cerede E, Philibert D, Goubet F, Teutsch G, and Gaillard-Kelly M (1998) Pharmacological profile of RU 58642, a potent systemic antiandrogen for the treatment of androgen-dependent disorders. J Steroid Biochem Mol Biol 64:103-111.
3. Bhasin S and Bremner WJ (1997) Emerging issues in androgen replacement therapy. J Clin Endocrinol Metab 82:3-8.
4. Bhasin S and Tenover JS (1997) Age-associated sarcopenia-issues in the use of testosterone as an anabolic agent in older men. J Clin Endocrinol Metab 82:1659-1660.
5. Conway AJ, Boylan LM, Howe C, Ross G, and Handelsman DJ (1988) Randomized clinical trial of testosterone replacement therapy in hypogonadal men. Int J Androl 11:247-264.
6. Dalton JT, Mukherjee A, Zhu Z, Kirkovsky L, and Miller DD (1998) Discovery of nonsteroidal androgens. Biochem Biophys Res Commun 244:1-4.
7. Davis S (1999a) Androgen replacement in women: a commentary. J Clin Endocrinol Metab 84:1886-1891.
8. Davis SR (1999b) The therapeutic use of androgens in women. J Steroid Biochem Mol Biol 69:177-184.
9. Davis SR and Burger HG (1996) Androgens and the postmenopausal woman. J Clin Endocrinol Metab 81:2759-2763.
10. George FW and Wilson JD (1986) Hormonal control of sexual development. Vitam Horm 43:145-196.
11. Hamann LG, Mani NS, Davis RL, Wang XN, Marschke KB, and Jones TK (1999) Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6-(trifluoromethyl)-8-pyridono(5,6-g]-quinoline (LG121071). J Med Chem 42:210-212.
12. Handelsman DJ, Conway AJ and Boylan LM (1990) Pharmacokinetics and pharmacodynamics of testosterone pellets in man. J Clin Endocrinol Metab 71:216-222.
13. He Y, Yin D, Perera M, Kirkovsky L, Stourman N, Dalton JT, and Miller DD (2002) Novel nonsteroidal ligands with high binding affinity and potent functional activity for the androgen receptor. Eur J Med Chem 37:619-634.
14. Heywood R, Chesterman H, Ball SA, and Wadsworth PF (1977) Toxicity of methyl testosterone in the beagle dog. Toxicology 7:357-365.
15. Ishak KG and Zimmerman HJ (1987) Hepatotoxic effects of the anabolic/androgenic steroids. Semin Liver Dis 7:230-236.
16. Mooradian AD, Morley JE and Korenman SG (1987) Biological actions of androgens. Endocr Rev 8:1-28.
17. Mukherjee A, Kirkovsky LI, Kimura Y, Marvel MM, Miller DD, and Dalton JT (1999) Affinity labeling of the androgen receptor with nonsteroidal chemoaffinity ligands. Biochem Pharmacol 58:1259-1267.
18. Mukherjee A, Kirkovsky L, Yao XT, Yates RC, Miller DD, and Dalton JT (1996) Enantioselective binding of Casodex to the androgen receptor. Xenobiotica 26:117-122.
19. Negro-Vilar A (1999) Selective androgen receptor modulators (SARMs): a novel approach to androgen therapy for the new millennium. J Clin Endocrinol Metab 84:3459-3462.
20. Nieschlag E (1996) Testosterone replacement therapy: something old, something new. Clin Endocrinol 45:261-262.
21. Saksena SK and Chaudhury RR (1970) Androgenic, anti-androgenic and anabolic activity of azasteroids on immature castrated rats. Indian J Med Res 58:513-518.
22. Snyder PJ and Lawrence DA (1980) Treatment of male hypogonadism with testosterone enanthate. J Clin Endocrinol Metab 51:1335-1339.
23. Takeda H, Chodak G, Mutchnik S, Nakamoto T, and Chang C (1990) Immunohistochemical localization of androgen receptors with mono- and polyclonal antibodies to androgen receptor. J Endocrinol 126:17-25.
24. Tenover JL (1997) Testosterone and the aging male. J Androl 18:103-106.
25. Teutsch G, Goubet F, Battmann T, Bonfils A, Bouchoux F, Cerede E, Gofflo D, Gaillard-Kelly M, and Philibert D (1994) Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor. J Steroid Biochem Mol Biol 48:111-119.
26. Velazquez E and Bellabarba Arata G (1998) Testosterone replacement therapy. Arch Androl 41:79-90.
27. Wilson JD (1996) Role of dihydrotestosterone in androgen action. Prostate Suppl 6:88-92.
28. Wilson JD, Aiman J, and MacDonald PC (1980) The pathogenesis of gynecomastia. Adv Intern Med 25:1-32.
29. Wu FC (1992) Testicular steroidogenesis and androgen use and abuse. Baillieres Clin Endocrinol Metab 6:373-403.
30. Yin D, He Y, Hong SS, Marhefka C, Stourman N, Kirkovsky L, Miller DD and Dalton JT (2003a) Key structural features of nonsteroidal ligands for binding and activation of the androgen receptor. Mol Pharmacol 63:211-223.
31. Yin D, Xu H, He Y, Kirkovsky L, Miller DD, and Dalton JT (2003b) Pharmacology, pharmacokinetics and metabolism of acetothiolutamide, a novel nonsteroidal agonist for the androgen receptor. J Pharmacol Exp Ther 304:1323-1333.