Methasterone resurfaced in 2005 as a “designer steroid”. It was brought to market by Designer Supplements as the primary ingredient of a dietary supplement named Superdrol. Its introduction into commerce may have represented an attempted circumvention of the U.S. Anabolic Steroids Control Act of 1990, since the law is, in part, drug-specific; methasterone, as is the case with many designer steroids, was not declared a Schedule III class anabolic steroid in that act because it was not commercially available at the time the act, and its subsequent revision, were signed into law. Methasterone was therefore being sold as an over-the-counter dietary supplement.
Methasterone, also known as 2α,17α-dimethyl-5α-dihydrotestosterone or as 2α,17α-dimethyl-5α-androstan-17β-ol-3-one, is a synthetic androstane steroid and a 17α-alkylatedderivative of DHT. Mebolazine is formed by hydrazone formation between two equivalents of methasterone with one equivalent of hydrazine.
History
The synthesis of methasterone is first mentioned in the literature in 1956 in connection with research conducted by Syntex Corporation in order to discover a compound with anti-tumor properties. In a 1959 research journal article, it is initially mentioned and is elaborated upon where its method of synthesis is discussed in greater detail, its tumor inhibiting properties are verified, and it is noted as being a “potent orally active anabolic agent exhibiting only weak androgenic activity.” The results of subsequent assays to determine methasterone's anabolic and androgenic activity were published in Vida's Androgens and Anabolic Agents, a dated but still standard reference, where it was noted that methasterone possessed the oral bioavailability of methyltestosterone while being 400% as anabolic and 20% as androgenic, yielding a Q-ratio of 20, which is considered very high.
Designer steroid
It was in late 2005 that the reclassification of methasterone as AAS was brought to public awareness via an article published in the Washington Post. Don Catlin of the UCLA Olympic Laboratory, who conducted the studies, noted methasterone's similarity to drostanolone. A warning by the FDA was issued soon after to the general public as well as to the distributor, Designer Supplements LLC, for the marketing of this compound. Methasterone was subsequently added to the World Anti-Doping Agencylist of prohibited substances in sport. Despite all of this, methasterone has resurfaced within the supplement industry on several occasions since its banning by WADA.
