Chemistry:SRX246

SRX246
Clinical data
ATC code	None;
Identifiers
	IUPAC name (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	512784-93-9;
ChemSpider	23290398;
UNII	372X2P22UY;
Chemical and physical data
Formula	C42H49N5O5
Molar mass	703.884 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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;

Short description: Chemical compound

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.^[5] It is also being studied for the treatment of post-traumatic stress disorder.^[6]

References

↑ "Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist". Journal of Pharmaceutical Sciences 102 (6): 2033–2043. June 2013. doi:10.1002/jps.23495. PMID 23471831.
↑ "Vasopressin antagonists as anxiolytics and antidepressants: recent developments". Recent Patents on CNS Drug Discovery 3 (2): 77–93. June 2008. doi:10.2174/157488908784534586. PMID 18537767.
↑ The Routledge International Handbook of Biosocial Criminology. Routledge. 5 December 2014. pp. 241–. ISBN 978-1-317-93674-9. https://books.google.com/books?id=Bmy2BQAAQBAJ&pg=PA241.
↑ "Azetidinones as vasopressin V1a antagonists". Bioorganic & Medicinal Chemistry 15 (5): 2054–80. March 2007. doi:10.1016/j.bmc.2006.12.031. PMID 17234419.
↑ Clinical trial number NCT02055638 for "Safety, Tolerability and Activity of SRX246 in Adults With Intermittent Explosive Disorder (AVN009)" at ClinicalTrials.gov
↑ "50 years of hurdles and hope in anxiolytic drug discovery". Nature Reviews. Drug Discovery 12 (9): 667–87. September 2013. doi:10.1038/nrd4075. PMID 23989795.

External links

"Clinical Candidates". Azevan Pharmaceuticals, Inc.. http://www.azevan.com/pipeline/default.asp.
"SRX-246". AdisInsight. Springer Nature Switzerland AG. http://adisinsight.springer.com/drugs/800023656.

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Original source: https://en.wikipedia.org/wiki/SRX246. Read more

[FabioGuillon2013-1] "Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist". Journal of Pharmaceutical Sciences 102 (6): 2033–2043. June 2013. doi:10.1002/jps.23495. PMID 23471831.

[SimonGuillon2008-2] "Vasopressin antagonists as anxiolytics and antidepressants: recent developments". Recent Patents on CNS Drug Discovery 3 (2): 77–93. June 2008. doi:10.2174/157488908784534586. PMID 18537767.

[DelisiDeLisi2014-3] The Routledge International Handbook of Biosocial Criminology. Routledge. 5 December 2014. pp. 241–. ISBN 978-1-317-93674-9. https://books.google.com/books?id=Bmy2BQAAQBAJ&pg=PA241.

[GuillonKoppel2007-4] "Azetidinones as vasopressin V1a antagonists". Bioorganic & Medicinal Chemistry 15 (5): 2054–80. March 2007. doi:10.1016/j.bmc.2006.12.031. PMID 17234419.

[5] Clinical trial number NCT02055638 for "Safety, Tolerability and Activity of SRX246 in Adults With Intermittent Explosive Disorder (AVN009)" at ClinicalTrials.gov

[GriebelHolmes2013-6] "50 years of hurdles and hope in anxiolytic drug discovery". Nature Reviews. Drug Discovery 12 (9): 667–87. September 2013. doi:10.1038/nrd4075. PMID 23989795.

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Clinical data

ATC code	None
Identifiers
IUPAC name (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	512784-93-9
ChemSpider	23290398
UNII	372X2P22UY
Chemical and physical data
Formula	C₄₂H₄₉N₅O₅
Molar mass	703.884 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES 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 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

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