Testosterone antagonists

Nayebi AR, Rezazadeh H (2004) Involvement of serotonineigicic mechanism in analgesia by castration and flutamide, a testosterone antagonist, in the rat formalin test. Phaimacol Biochem Behav 77 9-14... 

Nielsen HM, Rassing MR (2000b) TR146 cells grown on filters as a model of human buccal epithelium IV. Permeability of water, mannitol, testosterone and P-adrenoceptor antagonists. Comparison to human, monkey and porcine buccal mucosa. Int J Pharm 194 155-167... 

Bicalutamide, flutamide and nilutamide are nonsteroidal antiandrogens that are used for the treatment of prostatic carcinoma. They act as competitive antagonists at the androgen receptor. Hutamide also inhibits the formation of dihydrotestosterone from testosterone. 

Kramer MS, Cutler NR, Ballenger JC, Patterson WM, Mendels J (1995) A placebo-controlled trial of L-365,260, a CCK antagonist, in panic disorder. Biol Psychiatry 37 462-466 Kramer MS, Cutler N, Feighner J, Shrivastava R, Carman J, Sramek IJ, Reines SA, Snavely D, Wyatt-Knowles E, Hayle EJ (1998) Distinct mechanism for antidepressant activity by blockade of central substance P receptors. Science 281 1640-1645 Kriegsfeld LJ, Dawson TM, Dawson VL, Nelson RJ, Snyder SH (1997) Aggressive behavior in male mice lacking the gene for neuronal nitric oxide synthase requires testosterone. Brain Res 769 66-70... 

At present, pituitary hormones—and potent antagonist analogs of GnRH—are receiving increased attention. A GnRH antagonist in combination with testosterone has been shown to produce reversible azoospermia in nonhuman primates. 

The clinical pharmacology of saw palmetto in humans is not well defined. One week of treatment in healthy volunteers failed to influence 5oo-reductase activity, DHT concentration, or testosterone concentration. Six months of treatment in patients with BPH also failed to affect prostate-specific antigen (PSA) levels, a marker that is typically reduced by enzymatic inhibition of 5ct-reductase. In contrast, other researchers have reported a reduction in epidermal growth factor, DHT levels, and antagonist activity at the nuclear estrogen receptor in the prostate after 3 months of treatment with saw palmetto in patients with BPH. 

Antagonists of biotin include desthiobiotin in some forms, ureylene phenyl, homobiotin, urelenecyclohexyl butync and valeric acid, norbiotin, avidin, lysolecithin. and biotin sulfone. Synergists indude vitamins B>. B6, B 2, folic acid, pantothenic add. somatotrophin (growth hormone), and testosterone. 

Antagonists of folic acid include aminoplerin (4-aniino-ptcroylglulamic acidj. methotrexate tamethopterin), pyrimethamine, and 4-ammo-picroylas-partic acid. Synergists include biotin, pantothenic acid, niacin, vitamins B. Bo Bf, B 2. C, and E. somatotrophin (growth hormone), and testosterone. 

Buchter D, Behre HM, Kliesch S, Chirazi A, Nieschlag E, Assmann G, von Eckardstein A. Effects of testosterone suppression in young men by the gonadotropin releasing hormone antagonist cetrorelix on plasma lipids, lipolytic enzymes, lipid transfer proteins, insulin, and leptin. Exp Clin Endocrinol Diabetes 1999 107(8) 522-9. 

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