Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

AC-262,536

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
AC-262,536
Identifiers
  • 4-[(1R,3S,5S)-3-hydroxy-8-azabicyclo[3.2.1]octan-8-yl]naphthalene-1-carbonitrile
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC18H18N2O
Molar mass278.355 g·mol−1
3D model (JSmol)
  • OC1C[C@@H]2CC[C@H](C1)N2c3ccc(C#N)c4ccccc34
  • InChI=1S/C18H18N2O/c19-11-12-5-8-18(17-4-2-1-3-16(12)17)20-13-6-7-14(20)10-15(21)9-13/h1-5,8,13-15,21H,6-7,9-10H2/t13-,14+,15+
  • Key:ATKWLNSCJYLXPF-FICVDOATSA-N
  (verify)

AC-262536, also known asAccadrine, is a drug developed byAcadia Pharmaceuticals which acts as aselective androgen receptor modulator (SARM). Chemically it possessesendo-exo isomerism, with the endo form being the active form. It acts as apartial agonist for theandrogen receptor with aKi of 5 nM, and no significant affinity for any other receptors tested. In animal studies it produced a maximal effect of around 66% of thelevator animuscle weight increase oftestosterone, but only around 27% of its maximal effect onprostate gland weight.[1][2][3] It is ananiline SARM related toACP-105 andvosilasarm (RAD140).[4] The drug was encountered as a noveldesigner drug by at least 2020.[5]

Medical uses

[edit]

Accadrine is not approved for any medical use by theFood and Drug Administration and is not available as a licensedpharmaceutical drug as of 2025.[6]

Pharmacology

[edit]

Pharmacodynamics

[edit]

Accadrine isselective androgen receptor modulator (SARM), or atissue-selective mixedagonist orpartial agonist of theandrogen receptor (AR).[7][4] This receptor is thebiological target ofendogenousandrogens liketestosterone anddihydrotestosterone (DHT) and ofsyntheticanabolic steroids likenandrolone andoxandrolone.[8][9][10][11]Accadrine shows highaffinity for the AR, with a Ki value of 5 nM (relative to 29 nM for testosterone and 10 nM for DHT).[1][2][3]

References

[edit]
  1. ^abPiu F, Gardell LR, Son T, Schlienger N, Lund BW, Schiffer HH, Vanover KE, Davis RE, Olsson R, Bradley SR (March 2008). "Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator".J Steroid Biochem Mol Biol.109 (1–2):129–37.doi:10.1016/j.jsbmb.2007.11.001.PMID 18164613.S2CID 25172405.
  2. ^abCutler C, Viljanto M, Taylor P, Habershon-Butcher J, Muir T, Biddle S, Van Eenoo P (February 2021)."Equine metabolism of the selective androgen receptor modulator AC-262536 in vitro and in urine, plasma and hair following oral administration".Drug Testing and Analysis.13 (2):369–385.doi:10.1002/dta.2932.hdl:1854/LU-8694577.PMID 32959959.S2CID 221842707.
  3. ^abStacchini C, Botrè F, Comunità F, de la Torre X, Dima AP, Ricci M, Mazzarino M (February 2021). "Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques".Journal of Pharmaceutical and Biomedical Analysis.195 113849.doi:10.1016/j.jpba.2020.113849.PMID 33383501.S2CID 229941017.
  4. ^abZhang X, Sui Z (February 2013). "Deciphering the selective androgen receptor modulators paradigm".Expert Opinion on Drug Discovery.8 (2):191–218.doi:10.1517/17460441.2013.741582.PMID 23231475.S2CID 2584722.
  5. ^"AC-262,536".АИПСИН (in Russian). Retrieved2 January 2026.
  6. ^"FDA warns against using SARMs in body-building products".U.S. Food and Drug Administration. Food and Drug Administration. October 31, 2017. Retrieved2025-12-08.
  7. ^Machek SB, Cardaci TD, Wilburn DT, Willoughby DS (December 2020). "Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review".Steroids.164 108753.doi:10.1016/j.steroids.2020.108753.PMID 33148520.S2CID 225049089.
  8. ^Handelsman DJ (5 October 2020)."Androgen Physiology, Pharmacology, Use and Misuse". In Feingold KR, Anawalt B, Blackman MR, Boyce A, Chrousos G, Corpas E, et al. (eds.).Endotext [Internet]. South Dartmouth (MA): MDText.com, Inc.PMID 25905231.
  9. ^Wu C, Kovac JR (October 2016). "Novel Uses for the Anabolic Androgenic Steroids Nandrolone and Oxandrolone in the Management of Male Health".Current Urology Reports.17 (10): 72.doi:10.1007/s11934-016-0629-8.PMID 27535042.S2CID 43199715.
  10. ^Mohler ML, Nair VA, Hwang DJ, Rakov IM, Patil R, Miller DD (2005-10-28). "Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates".Expert Opinion on Therapeutic Patents.15 (11). Informa Healthcare:1565–1585.doi:10.1517/13543776.15.11.1565.ISSN 1354-3776.S2CID 96279138.
  11. ^Kicman AT (June 2008)."Pharmacology of anabolic steroids".British Journal of Pharmacology.154 (3):502–521.doi:10.1038/bjp.2008.165.PMC 2439524.PMID 18500378.
ARTooltip Androgen receptor
Agonists
SARMsTooltip Selective androgen receptor modulator
Antagonists
GPRC6A
Agonists
Retrieved from "https://en.wikipedia.org/w/index.php?title=AC-262,536&oldid=1330728283"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2026 Movatter.jp