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Trestolone

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Trestolone
Clinical data
Other namesMENT; 7α-Methylnandrolone; 7α-methyl-19-nortestosterone; 17β-hydroxy-7α-methylestr-4-en-3-one
ATC code
  • none
Legal status
Legal status
  • Unclassified
Identifiers
  • (7R,8R,9S,10R,13S,14S,17S)-17-Hydroxy-7,13-dimethyl-
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
ECHA InfoCard100.184.887 Edit this at Wikidata
Chemical and physical data
FormulaC19H28O2
Molar mass288.424 g·mol−1
3D model (JSmol)
  • O=C2\C=C3\CC(C)[C@H]1[C@@H]4CCC(O)[C@@]4(C)CC[C@@H]1[C@H]3CC2
  • InChI=1S/C19H28O2/c1-11-9-12-10-13(20)3-4-14(12)15-7-8-19(2)16(18(11)15)5-6-17(19)21/h10-11,14-18,21H,3-9H2,1-2H3/t11?,14-,15+,16-,17?,18+,19-/m0/s1 checkY
  • Key:YSGQGNQWBLYHPE-XOGXAEGHSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Trestolone is a synthetic androgen taken to build muscle rapidly, and is a theoretical candidate drug for use in hormonal male contraceptive methods. In males, regular administration of sufficient quantities of trestolone induces a state of temporary infertility.[1][unreliable medical source?]

Trestolone is an experimental contraceptive treatment and is not yet available commercially. It is currently being evaluated for safety and effectiveness in scientific studies, supported by the Population Council.[citation needed]

Mechanism of action

As a derivative of the anabolic steroid hormone nandrolone, trestolone's viability as a male contraceptive is twofold.

Inhibition of sperm production

Spermatozoa are produced in the testes of males in a process called spermatogenesis. In order to render a man infertile, a hormone-based male contraceptive method must stop spermatogenesis by interrupting the release of gonadotropins from the pituitary gland. Even in low concentrations, trestolone is a potent inhibitor of the release of the gonadotropin hormones, luteinizing hormone (LH) and follicle stimulating hormone (FSH).[citation needed]

In order for spermatogenesis to occur in the testes, both FSH and the male hormone testosterone must be present. By inhibiting release of FSH, trestolone creates an endocrine environment in which conditions for spermatogenesis are not ideal. Manufacture of sperm is further impaired by the suppression of LH, which in turn drastically curtails the production of testosterone. Sufficient regular doses of trestolone cause severe oligozoospermia or azoospermia, and therefore infertility, in most male patients.[citation needed]

Trestolone-induced sterility has been found to be quickly reversible upon discontinuation.[citation needed]

Support of secondary sex characteristics

When LH release is inhibited, the amount of testosterone made in the testes declines dramatically. As a result of trestolone's gonadotropin-suppressing qualities, levels of serum testosterone fall sharply in patients. Testosterone is the primary hormone responsible for maintenance of male secondary sex characteristics.

Normally, inadequate testosterone levels cause undesirable effects, such as fatigue, loss of skeletal muscle mass, reduced libido, and weight gain. However, the androgenic and anabolic properties of trestolone largely ameliorate this problem. Essentially, trestolone replaces testosterone's role as the primary male hormone in the body.

References

  • MENT – project information from the Population Council