Acetothiolutamide
| Acetothiolutamide | |
|---|---|
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| CAS Number | 216665-38-2 |
| PubChem | 10873814 |
| DrugBank | |
| ChemSpider | 9049091 |
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Acetothiolutamide is a selective androgen receptor modulator (SARM) derived from the nonsteroidal antiandrogen bicalutamide that was described in 2002 and was one of the first SARMs to be discovered and developed.[1][2][3][4] It is a high-affinity, selective ligand of the androgen receptor (AR) (Ki = 2.1–4.9 nM), where it acts as a full agonist in vitro, and has in vitro potency comparable to that of testosterone.[2][4][5] However, in vivo, acetothiolutamide displayed overall negligible androgenic effects, though significant (albeit very low) anabolic effects were observed at high doses.[2] In addition, notable antiandrogen effects were observed in castrated male rats treated with testosterone propionate.[2] The discrepancy between the in vitro and in vivo actions of acetothiolutamide was determined to be related to rapid plasma clearance and extensive hepatic metabolism into a variety of metabolites with differing pharmacological activity, including AR partial agonism and antagonism.[2][4][6] In accordance with its poor metabolic stability, acetothiolutamide is not orally bioavailable, and shows activity only via injected routes such as subcutaneous and intravenous.[2]
See also[edit | edit source]
References[edit | edit source]
- ↑ , Discovery of nonsteroidal androgens, Biochemical and Biophysical Research Communications, Vol. 244(Issue: 1), pp. 1–4, DOI: 10.1006/bbrc.1998.8209, PMID: 9514878,
- ↑ 2.0 2.1 2.2 2.3 2.4 2.5 , Pharmacology, pharmacokinetics, and metabolism of acetothiolutamide, a novel nonsteroidal agonist for the androgen receptor, The Journal of Pharmacology and Experimental Therapeutics, Vol. 304(Issue: 3), pp. 1323–33, DOI: 10.1124/jpet.102.040832, PMID: 12604713, PMC: 2040235,
- ↑
- ↑ 4.0 4.1 4.2 , In vivo metabolism and final disposition of a novel nonsteroidal androgen in rats and dogs, Drug Metabolism and Disposition, Vol. 34(Issue: 10), pp. 1713–21, DOI: 10.1124/dmd.106.009985, PMID: 16815963,
- ↑ , The para substituent of S-3-(phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamides is a major structural determinant of in vivo disposition and activity of selective androgen receptor modulators, The Journal of Pharmacology and Experimental Therapeutics, Vol. 315(Issue: 1), pp. 230–9, DOI: 10.1124/jpet.105.088344, PMID: 15987833, PMC: 2039880,
- ↑ , Pharmacodynamics of selective androgen receptor modulators, The Journal of Pharmacology and Experimental Therapeutics, Vol. 304(Issue: 3), pp. 1334–40, DOI: 10.1124/jpet.102.040840, PMID: 12604714, PMC: 2040238,
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