Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

LG121071

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
LG121071
Clinical data
Other namesLG-121071; LGD-121071
Identifiers
  • 6-Ethyl-4-(trifluoromethyl)-1H,2H,6H,7H,8H,9H-pyrido[3,2-g]quinolin-2-one
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC15H15F3N2O
Molar mass296.293 g·mol−1
3D model (JSmol)
  • CCC1CCNC2=C1C=C3C(=CC(=O)NC3=C2)C(F)(F)F
  • InChI=1S/C15H15F3N2O/c1-2-8-3-4-19-12-7-13-10(5-9(8)12)11(15(16,17)18)6-14(21)20-13/h5-8,19H,2-4H2,1H3,(H,20,21)
  • Key:SZPPQFARTYXRKU-UHFFFAOYSA-N

LG121071 (orLGD-121071) is aselective androgen receptor modulator (SARM) developed byLigand Pharmaceuticals that was first described in 1999 and was the firstorallyactivenonsteroidalandrogen to be discovered.[1][2] It is atricyclicquinolone derivative, structurally distinct from other nonsteroidal AR agonists likeandarine andenobosarm (ostarine).[2] The drug acts as a high-affinityfull agonist of theandrogen receptor (AR) (Ki = 17 nM),[2] with apotency andefficacy that is said to be equivalent to that ofdihydrotestosterone (DHT).[3] Unlike testosterone, but similarly to DHT, LG121071 and other nonsteroidal androgens cannot be potentiated by5α-reductase in androgenic tissues (noraromatized intoestrogenicmetabolites), and for this reason, show tissue-selective androgenic effects.[4] In accordance, they are said to possess fullanabolic activity with reducedandrogenic activity, similarly toanabolic-androgenic steroids.[5]

Thein vitrometabolism of LG121071 has been characterized in anticipation of its possible use as adoping agent.[5][6]

See also

[edit]

References

[edit]
  1. ^Hamann LG, Mani NS, Davis RL, Wang XN, Marschke KB, Jones TK (January 1999). "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.doi:10.1021/jm9806648.PMID 9925725.
  2. ^abcGao W, Kim J, Dalton JT (August 2006)."Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands".Pharmaceutical Research.23 (8):1641–1658.doi:10.1007/s11095-006-9024-3.PMC 2072875.PMID 16841196.
  3. ^Chengalvala M, Oh T, Roy AK (2005). "Selective androgen receptor modulators".Expert Opinion on Therapeutic Patents.13 (1):59–66.doi:10.1517/13543776.13.1.59.ISSN 1354-3776.S2CID 219188263.
  4. ^Elbers JM, Grootenhuis AJ (April 2003). "New tissue-selective androgens: perspectives in the treatment of androgen deficits".Annales d'Endocrinologie.64 (2):183–188.PMID 12773961.
  5. ^abKnoop A, Krug O, Vincenti M, Schänzer W, Thevis M (2015). "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.doi:10.1255/ejms.1328.PMID 25906032.S2CID 29918434.
  6. ^Gerace E, Salomone A, Fasano F, Costa R, Boschi D, Di Stilo A, Vincenti M (April 2011). "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.doi:10.1007/s00216-010-4569-8.hdl:2318/86557.PMID 21165606.S2CID 43268790.
ARTooltip Androgen receptor
Agonists
SARMsTooltip Selective androgen receptor modulator
Antagonists
GPRC6A
Agonists
Retrieved from "https://en.wikipedia.org/w/index.php?title=LG121071&oldid=1300885295"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp