HT-2157

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HT-2157
Structural formula
Space-filling model
Clinical data
ATC code
  • none
Identifiers
  • 1-phenyl-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
Chemical and physical data
FormulaC21H13F3N2O
Molar mass366.335 g/mol g·mol−1
3D model (JSmol)
  • c14ccccc4n(-c3ccccc3)c(=O)c1=N\c(c2)cccc2C(F)(F)F
  • 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 code name 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

  1. ^ Rowley HL, et al. Effects of HT 2157, a galanin 3 receptor antagonist, on extracellular levels of 5 HT in various brain regions of freely moving rats. Proceedings of the British Pharmacological Society Winter Meeting December 2005
  2. ^ Swanson CJ, et al. Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299. PNAS 2005; 102(48):17489-17494. doi 10.1073/pnas.0508970102
  3. ^ Kaplan AP. Enteric-coated HT-2157 compositions and methods of their use. Patent US 8277842, filed Jan 20th 2012.
  4. ^ http://www.dartneuroscience.com/DrugPrograms.php


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