HT-2157

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HT-2157
File:HT-2157 structure.png
Systematic (IUPAC) name
1-phenyl-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one
Identifiers
CAS Number 303149-14-6
ATC code none
PubChem CID: 1471834
IUPHAR/BPS 6126
Chemical data
Formula C21H13F3N2O
Molecular mass 366.335 g/mol
  • c14ccccc4n(-c3ccccc3)c(=O)c1=N\c(c2)cccc2C(F)(F)F

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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