Chemistry:AC-262,536
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| Formula | C18H18N2O |
| Molar mass | 278.355 g·mol−1 |
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AC-262536, also known as Accadrine, is a drug developed by Acadia Pharmaceuticals which acts as a selective androgen receptor modulator (SARM). Chemically it possesses endo-exo isomerism, with the endo form being the active form. It acts as a partial agonist for the androgen receptor with a Ki of 5 nM, and no significant affinity for any other receptors tested. In animal studies it produced a maximal effect of around 66% of the levator ani muscle weight increase of testosterone, but only around 27% of its maximal effect on prostate gland weight.[1][2][3] It is an aniline SARM related to ACP-105 and vosilasarm (RAD140).[4] The drug was encountered as a novel designer drug by at least 2020.[5]
Medical uses
Accadrine is not approved for any medical use by the Food and Drug Administration and is not available as a licensed pharmaceutical drug as of 2025.[6]
Pharmacology
Pharmacodynamics
Accadrine is selective androgen receptor modulator (SARM), or a tissue-selective mixed agonist or partial agonist of the androgen receptor (AR).[7][4] This receptor is the biological target of endogenous androgens like testosterone and dihydrotestosterone (DHT) and of synthetic anabolic steroids like nandrolone and oxandrolone.[8][9][10][11] Accadrine shows high affinity 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
- ↑ 1.0 1.1 "Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator". J Steroid Biochem Mol Biol 109 (1–2): 129–37. March 2008. doi:10.1016/j.jsbmb.2007.11.001. PMID 18164613.
- ↑ 2.0 2.1 "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. February 2021. doi:10.1002/dta.2932. PMID 32959959. https://biblio.ugent.be/publication/8694577.
- ↑ 3.0 3.1 "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. February 2021. doi:10.1016/j.jpba.2020.113849. PMID 33383501.
- ↑ 4.0 4.1 "Deciphering the selective androgen receptor modulators paradigm". Expert Opinion on Drug Discovery 8 (2): 191–218. February 2013. doi:10.1517/17460441.2013.741582. PMID 23231475.
- ↑ "AC-262,536" (in ru). https://aipsin.com/newsubstance/413/.
- ↑ "FDA warns against using SARMs in body-building products". Food and Drug Administration. October 31, 2017. https://www.fda.gov/news-events/fda-brief/fda-brief-fda-warns-against-using-sarms-body-building-products.
- ↑ "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. December 2020. doi:10.1016/j.steroids.2020.108753. PMID 33148520.
- ↑ "Androgen Physiology, Pharmacology, Use and Misuse". Endotext [Internet]. South Dartmouth (MA): MDText.com, Inc.. 5 October 2020. https://www.ncbi.nlm.nih.gov/books/NBK279000/.
- ↑ "Novel Uses for the Anabolic Androgenic Steroids Nandrolone and Oxandrolone in the Management of Male Health". Current Urology Reports 17 (10): 72. October 2016. doi:10.1007/s11934-016-0629-8. PMID 27535042.
- ↑ "Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates". Expert Opinion on Therapeutic Patents (Informa Healthcare) 15 (11): 1565–1585. 2005-10-28. doi:10.1517/13543776.15.11.1565. ISSN 1354-3776.
- ↑ "Pharmacology of anabolic steroids". British Journal of Pharmacology 154 (3): 502–521. June 2008. doi:10.1038/bjp.2008.165. PMID 18500378.
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