HT-2157

HT-2157
Clinical data
ATC code	none;
Identifiers
	IUPAC name 1-Phenyl-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one;
CAS Number	303149-14-6;
PubChem CID	1471834;
IUPHAR/BPS	6126;
ChemSpider	1213983;
Chemical and physical data
Formula	C21H13F3N2O
Molar mass	366.343 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c14ccccc4n(-c3ccccc3)c(=O)c1=N\c(c2)cccc2C(F)(F)F;
	InChI InChI=1S/C21H13F3N2O/c22-21(23,24)14-7-6-8-15(13-14)25-19-17-11-4-5-12-18(17)26(20(19)27)16-9-2-1-3-10-16/h1-13H/b25-19+; Key:TXCGMRVPXUBHAL-NCELDCMTSA-N;

HT-2157 (former development code SNAP-37889) is a drug which acts as a selective non-peptide antagonist for the receptor GAL-3, which is usually activated by the neuropeptide galanin. Blocking this receptor with HT-2157 produced increased serotonin release,[1] as well as producing antidepressant and anxiolytic effects in animal studies,[2] and it was also being researched for treatment of cognitive dysfunction.[3] All human clinical trials were terminated due to safety concerns however, and new GAL-3 antagonists are now being sought instead.[4]

References

"pA2 Online". www.pa2online.org.
Swanson, C. J.; Blackburn, T. P.; Zhang, X.; Zheng, K.; Xu, Z.-Q. D.; Hokfelt, T.; Wolinsky, T. D.; Konkel, M. J.; Chen, H.; Zhong, H.; Walker, M. W.; Craig, D. A.; Gerald, C. P. G.; Branchek, T. A. (2005). "Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299". Proceedings of the National Academy of Sciences. 102 (48): 17489–17494. doi:10.1073/pnas.0508970102. PMC 1283534. PMID 16287967.
US 8277842, Kaplan AP, "Enteric-coated HT-2157 compositions and methods of their use", published January 20, 2012
"Dart NeuroScience LLC -- Scientific Advisory Board". www.dartneuroscience.com.

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[1] "pA2 Online". www.pa2online.org.

[2] Swanson, C. J.; Blackburn, T. P.; Zhang, X.; Zheng, K.; Xu, Z.-Q. D.; Hokfelt, T.; Wolinsky, T. D.; Konkel, M. J.; Chen, H.; Zhong, H.; Walker, M. W.; Craig, D. A.; Gerald, C. P. G.; Branchek, T. A. (2005). "Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299". Proceedings of the National Academy of Sciences. 102 (48): 17489–17494. doi:10.1073/pnas.0508970102. PMC 1283534. PMID 16287967.

[3] US 8277842, Kaplan AP, "Enteric-coated HT-2157 compositions and methods of their use", published January 20, 2012

[DartNeuroScience-4] "Dart NeuroScience LLC -- Scientific Advisory Board". www.dartneuroscience.com.