LG121071 explained
LG121071 (or LGD-121071) is a selective androgen receptor modulator (SARM) developed by Ligand Pharmaceuticals that was first described in 1999 and was the first orally active nonsteroidal androgen to be discovered.[1] [2] It is a tricyclic quinolone derivative, structurally distinct from other nonsteroidal AR agonists like andarine and enobosarm (ostarine). The drug acts as a high-affinity full agonist of the androgen receptor (AR) (Ki = 17 nM), with a potency and efficacy that is said to be equivalent to that of dihydrotestosterone (DHT).[3] Unlike testosterone, but similarly to DHT, LG121071 and other nonsteroidal androgens cannot be potentiated by 5α-reductase in androgenic tissues (nor aromatized into estrogenic metabolites), and for this reason, show tissue-selective androgenic effects.[4] In accordance, they are said to possess full anabolic activity with reduced androgenic activity, similarly to anabolic-androgenic steroids.[5]
The in vitro metabolism of LG121071 has been characterized in anticipation of its possible use as a doping agent.[6]
See also
Notes and References
- Hamann LG, Mani NS, Davis RL, Wang XN, Marschke KB, Jones TK . Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071) . Journal of Medicinal Chemistry . 42 . 2 . 210–212 . January 1999 . 9925725 . 10.1021/jm9806648 .
- Gao W, Kim J, Dalton JT . Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands . Pharmaceutical Research . 23 . 8 . 1641–1658 . August 2006 . 16841196 . 2072875 . 10.1007/s11095-006-9024-3 .
- Chengalvala M, Oh T, Roy AK . Selective androgen receptor modulators. Expert Opinion on Therapeutic Patents. 13. 1. 2005. 59–66. 1354-3776. 10.1517/13543776.13.1.59. 219188263 .
- Elbers JM, Grootenhuis AJ . New tissue-selective androgens: perspectives in the treatment of androgen deficits . Annales d'Endocrinologie . 64 . 2 . 183–188 . April 2003 . 12773961 .
- Knoop A, Krug O, Vincenti M, Schänzer W, Thevis M . In vitro metabolism studies on the selective androgen receptor modulator (SARM) LG121071 and its implementation into human doping controls using liquid chromatography-mass spectrometry . European Journal of Mass Spectrometry . 21 . 1 . 27–36 . 2015 . 25906032 . 10.1255/ejms.1328 . 29918434 .
- Gerace E, Salomone A, Fasano F, Costa R, Boschi D, Di Stilo A, Vincenti M . Validation of a GC/MS method for the detection of two quinolinone-derived selective androgen receptor modulators in doping control analysis . Analytical and Bioanalytical Chemistry . 400 . 1 . 137–144 . April 2011 . 21165606 . 10.1007/s00216-010-4569-8 . free . 43268790 . 2318/86557 .