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| Other names | Thioacetolutamide |
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| Formula | C20H18F3N3O3S |
| Molar mass | 437.44 g·mol−1 |
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Acetothiolutamide is aselective androgen receptor modulator (SARM) derived from thenonsteroidal antiandrogenbicalutamide 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, selectiveligand of theandrogen receptor (AR) (Ki = 2.1–4.9 nM), where it acts as afull agonistin vitro, and hasin vitropotency comparable to that oftestosterone.[2][4][5] However,in vivo, acetothiolutamide displayed overall negligibleandrogenic 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 withtestosterone propionate.[2] The discrepancy between thein vitro andin vivo actions of acetothiolutamide was determined to be related to rapidplasma clearance and extensivehepaticmetabolism into a variety ofmetabolites with differingpharmacological activity, including ARpartial agonism andantagonism.[2][4][6] In accordance with its poormetabolic stability, acetothiolutamide is notorallybioavailable, and shows activity only viainjectedroutes such assubcutaneous andintravenous.[2]
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