SRX246 explained

SRX246, also known as API-246, is a small-molecule, centrally-active, highly-selective vasopressin V_1A 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. It is also being studied for the treatment of post-traumatic stress disorder.^[5]

See also

• List of investigational anxiolytics
• ABT-436
• Balovaptan
• Nelivaptan
• TS-121

External links

• Web site: Clinical Candidates . Azevan Pharmaceuticals, Inc. .
• Web site: SRX-246 . AdisInsight . Springer Nature Switzerland AG .

Notes and References

1. Fabio KM, Guillon CD, Lu SF, Heindel ND, Brownstein MJ, Lacey CJ, Garippa C, Simon NG . 6 . Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist . Journal of Pharmaceutical Sciences . 102 . 6 . 2033–2043 . June 2013 . 23471831 . 10.1002/jps.23495 .
2. Simon NG, Guillon C, Fabio K, Heindel ND, Lu SF, Miller M, Ferris CF, Brownstein MJ, Garripa C, Koppel GA . 6 . Vasopressin antagonists as anxiolytics and antidepressants: recent developments . Recent Patents on CNS Drug Discovery . 3 . 2 . 77–93 . June 2008 . 18537767 . 10.2174/157488908784534586 .
3. Book: DeLisi M, Vaughn MG . The Routledge International Handbook of Biosocial Criminology. 5 December 2014. Routledge. 978-1-317-93674-9. 241–.
4. Guillon CD, Koppel GA, Brownstein MJ, Chaney MO, Ferris CF, Lu SF, Fabio KM, Miller MJ, Heindel ND, Hunden DC, Cooper RD, Kaldor SW, Skelton JJ, Dressman BA, Clay MP, Steinberg MI, Bruns RF, Simon NG . 6 . Azetidinones as vasopressin V1a antagonists . Bioorganic & Medicinal Chemistry . 15 . 5 . 2054–80 . March 2007 . 17234419 . 2067992 . 10.1016/j.bmc.2006.12.031 .
5. Griebel G, Holmes A . 50 years of hurdles and hope in anxiolytic drug discovery . Nature Reviews. Drug Discovery . 12 . 9 . 667–87 . September 2013 . 23989795 . 4176700 . 10.1038/nrd4075 .