SRX246, also known as API-246, is a small-molecule, centrally-active, highly-selective vasopressin V1A receptor antagonist which is under investigation by Azevan Pharmaceuticals for the treatment of affective and anger disorders.[1][2][3] It is an azetidinone derivative, and was developed from LY-307174 as a lead compound.[4] A phase II activity trial of the drug in the treatment of adults with intermittent explosive disorder is ongoing.[5] It is also being studied for the treatment of post-traumatic stress disorder.[6]
See also
References
- ^ Fabio KM, Guillon CD, Lu SF, Heindel ND, Brownstein MJ, Lacey CJ, et al. (June 2013). "Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist". Journal of Pharmaceutical Sciences. 102 (6): 2033–2043. doi:10.1002/jps.23495. PMID 23471831.
- ^ Simon NG, Guillon C, Fabio K, Heindel ND, Lu SF, Miller M, et al. (June 2008). "Vasopressin antagonists as anxiolytics and antidepressants: recent developments". Recent Patents on CNS Drug Discovery. 3 (2): 77–93. doi:10.2174/157488908784534586. PMID 18537767.
- ^ DeLisi M, Vaughn MG (5 December 2014). The Routledge International Handbook of Biosocial Criminology. Routledge. pp. 241–. ISBN 978-1-317-93674-9.
- ^ Guillon CD, Koppel GA, Brownstein MJ, Chaney MO, Ferris CF, Lu SF, et al. (March 2007). "Azetidinones as vasopressin V1a antagonists". Bioorganic & Medicinal Chemistry. 15 (5): 2054–80. doi:10.1016/j.bmc.2006.12.031. PMC 2067992. PMID 17234419.
- ^ Clinical trial number NCT02055638 for "Safety, Tolerability and Activity of SRX246 in Adults With Intermittent Explosive Disorder (AVN009)" at ClinicalTrials.gov
- ^ Griebel G, Holmes A (September 2013). "50 years of hurdles and hope in anxiolytic drug discovery". Nature Reviews. Drug Discovery. 12 (9): 667–87. doi:10.1038/nrd4075. PMC 4176700. PMID 23989795.
External links
- "Clinical Candidates". Azevan Pharmaceuticals, Inc.
- "SRX-246". AdisInsight. Springer Nature Switzerland AG.