Androgen discovery

Aminopyrine, 234 Aminotetradine, 265 2-Aminothiazole, 247 2-Aminothiazole synthesis, 126 Amisotetradine, 266 Amobarbital, 268 Amopyroquine, 342 Amoxycillin, 414 Amphetamine, 37, 70 Ampicillin, 413 Amprolium, 264 Amytriptylene, 141, 404 Anabolic effects, 169 Androgens, discovery, 155 Androstanolone, 173 Androstenedione, 158, 176 Anesthesia, parenteral, 56 Angst, 363 Anileridine, 300 Aniline, metabolism. 111 Anisindandione, 147 Anovlar , 186 Antagonists, 20, 65 Antazoline, 242 Antibodies, 41... 

As with the other sex hormones, the first clinical use of Hiidrogens was for support therapy in individuals deficient in the endogenous hormone. The discovery that androgens exert an ana-hnlic effect greatly extended the indications for their use. 

Structural modifications of bicalutamide led to the discovery of the first generation of selective androgen receptor modulators (SARMs). These compounds not only bind to the AR with an affinity in the nanomolar range, but they also show tissue selectivity in animal models [206]. 

Stanozolol is an androgenic anabolic steroid used in cases of deficiency in protein synthesis and osteoporosis. In spite of its prohibition by the International Olympic Committee since 1974, this compound has been often abused by athletes and in horse-races to enhance performance (25). In recent times, the discovery of stanozolol at injection sites revealed its illegal use as a growth promoter in breeding, despite the ban in the European Union in effect since 1988 (26). 

Hershberger et al. [187] discovered in 1953 that although 19-nor-testosterone and other 19-nor analogs exhibit only relatively weak androgenic properties the protein anabolic effects and myotrophic effects were of the same order of magnitude as those of testosterone. Since the anabolic-androgenic ratio of the 19-nortestosterone derivatives was very favorable, this discovery opened a new field of anabolic agents. 

Lanter, J.C., Fiordeliso, J.J., Allan, G.F., Musto, A., Hahn do, W. and Sui, Z. (2006) A bioisosteric approach to the discovery of indole carhinol androgen receptor ligands. Bioorganic et Medicinal Chemistry Letters, 16, 5646-5649. 

Hamann, L.G., Mani, N.S., Davis, R.L., Wang, X.N., Marschke, K.B. and Jones, T.K. (1999) Discovery of a potent, orally active, nonsteroidal androgen receptor agonist 4-ethyl-l,2,3,4-tetrahydro-6-(trifluoromethyl)-8-pyridono[5,6-g]-quinoline (LG 121071). Journal of Medicinal Chemistry, 42, 210-212. 

Zhang, X., Li, X., Allan, G.F., Sbriscia, T., Linton, O., Lundeen, S.G. and Sui, Z. (2007) Serendipitous discovery of novel imidazolopyrazole scaffold as selective androgen receptor modulators. Bioorganic el Medicinal Chemistry Letters, 17,439-443. 

Malley, M.F., Sack, J.S., Salvati, M.E., Grover, G.J., Ostrowski, J. and Hamann, L.G. (2006) Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold. Journal of Medicinal Chemistry, 49, 7596-7599. 

Androgen receptor-cofactor interactions as targets for new drug discovery. Trends in Pharmacological Sciences, 26, 225—228. 

Segal, S., Narayanan, R. and Dalton, J.T. (2006) Therapeutic potential of the SARMs Revisiting the androgen receptor for drug discovery. Expert Opin Invest Drugs, 15, 377-387. 

Discovery and therapeutic promise of selective androgen receptor modulators. Molecular Interventions, 5, 173-188. 

Testosterone is a male sex hormone, one of a class of compounds known as androgens. Included in this group are testosterone, dihydrotestosterone, and androstenedione. Androgens are synthesized from cholesterol and are considered steroid hormones, a category of hormones that includes female sex hormones such as estrogen. The isolation and synthesis of testosterone were reported in 1935. Chemists Adolf Butenandt and Leopold Ruzicka later received the Nobel Prize in chemistry (in 1939) for this work and related discoveries. 

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