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SRX246

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SRX246
Clinical data
ATC code
  • None
Identifiers
  • (R)-4-([1,4'-bipiperidin]-1'-yl)-4-oxo-2-((3S,4R)-2-oxo-3-((S)-2-oxo-4-phenyloxazolidin-3-yl)-4-((E)-styryl)azetidin-1-yl)-N-((R)-1-phenylethyl)butanamide
CAS Number
Chemical and physical data
FormulaC42H49N5O5
Molar mass703.88 g/mol g·mol−1
3D model (JSmol)
  • O=C1[C@@H](N2C(OC[C@@H]2C3=CC=CC=C3)=O)[C@@H](/C=C/C4=CC=CC=C4)N1[C@@H](C(N[C@H](C)C5=CC=CC=C5)=O)CC(N6CCC(N7CCCCC7)CC6)=O
  • InChI=1S/C42H49N5O5/c1-30(32-16-8-3-9-17-32)43-40(49)36(28-38(48)45-26-22-34(23-27-45)44-24-12-5-13-25-44)46-35(21-20-31-14-6-2-7-15-31)39(41(46)50)47-37(29-52-42(47)51)33-18-10-4-11-19-33/h2-4,6-11,14-21,30,34-37,39H,5,12-13,22-29H2,1H3,(H,43,49)/b21-20+/t30-,35-,36-,37-,39+/m1/s1
  • Key:FJUKOXWSIGULLE-JVOQCOEYSA-N

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. doi:10.1002/jps.23495. ISSN 0022-3549.
  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. doi:10.2174/157488908784534586. ISSN 1574-8898.
  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. doi:10.1016/j.bmc.2006.12.031. ISSN 0968-0896.
  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. doi:10.1038/nrd4075. ISSN 1474-1776. PMID 23989795.



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