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SRX246

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SRX246
File:SRX246 structure.png
Systematic (IUPAC) name
(2R)-4-oxo-2-[(3S,4R)-2-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-4-[(E)-2-phenylethenyl]azetidin-1-yl]-4-(4-piperidin-1-ylpiperidin-1-yl)-N-[(1R)-1-[3-(trifluoromethyl)phenyl]ethyl]butanamide
Clinical data
Identifiers
None
PubChem CID 44428551
ChemSpider 23290399
Chemical data
Formula C43H48F3N5O5
771.867 g/mol

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

  1. ^ Fabio, Karine M.; Guillon, Christophe D.; Lu, Shi-fang; Heindel, Ned D.; Brownstein, Michael J.; Lacey, Carl J.; Garippa, Carrie; Simon, Neal G. (2013). "Pharmacokinetics and metabolism of SRX246: A potent and selective vasopressin 1a antagonist". Journal of Pharmaceutical Sciences 102 (6): 2033–2043. ISSN 0022-3549. doi:10.1002/jps.23495. 
  2. ^ Simon, Neal; Guillon, Christophe; Fabio, Karine; Heindel, Ned; Lu, Shi-fang; Miller, Marvin; Ferris, Craig; Brownstein, Michael; Garripa, Carrie; Koppel, Gary (2008). "Vasopressin Antagonists as Anxiolytics and Antidepressants: Recent Developments". Recent Patents on CNS Drug Discovery 3 (2): 77–93. ISSN 1574-8898. doi:10.2174/157488908784534586. 
  3. ^ Associate Professor Iowa State University Matt Delisi; Matt DeLisi; Michael G Vaughn (5 December 2014). The Routledge International Handbook of Biosocial Criminology. Routledge. pp. 241–. ISBN 978-1-317-93674-9. 
  4. ^ Guillon, Christophe D.; Koppel, Gary A.; Brownstein, Michael J.; Chaney, Michael O.; Ferris, Craig F.; Lu, Shi-fang; Fabio, Karine M.; Miller, Marvin J.; Heindel, Ned D.; Hunden, David C.; Cooper, Robin D.G.; Kaldor, Stephen W.; Skelton, Jeffrey J.; Dressman, Bruce A.; Clay, Michael P.; Steinberg, Mitchell I.; Bruns, Robert F.; Simon, Neal G. (2007). "Azetidinones as vasopressin V1a antagonists". Bioorganic & Medicinal Chemistry 15 (5): 2054–2080. ISSN 0968-0896. doi:10.1016/j.bmc.2006.12.031. 
  5. ^ "Safety, Tolerability and Activity of SRX246 in Adults With Intermittent Explosive Disorder (AVN009)". Retrieved 11 March 2015. 
  6. ^ Griebel, Guy; Holmes, Andrew (2013). "50 years of hurdles and hope in anxiolytic drug discovery". Nature Reviews Drug Discovery 12 (9): 667–687. ISSN 1474-1776. doi:10.1038/nrd4075. 

External links



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