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Wikipedia

HT-2157

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]

HT-2157
Clinical data
ATC code
  • none
Identifiers
  • 1-Phenyl-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one
CAS Number
  • 303149-14-6
PubChem CID
  • 1471834
IUPHAR/BPS
  • 6126
ChemSpider
  • 1213983
UNII
  • J4DRJ9BFS1
Chemical and physical data
FormulaC21H13F3N2O
Molar mass366.343 g·mol−1
3D model (JSmol)
  • Interactive image
  • 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

References Edit

  1. ^ "pA2 Online". www.pa2online.org.
  2. ^ Swanson CJ, Blackburn TP, Zhang X, Zheng K, Xu ZQ, Hökfelt T, et al. (November 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 of the United States of America. 102 (48): 17489–94. 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 
  4. ^ "Dart NeuroScience LLC -- Scientific Advisory Board". www.dartneuroscience.com.


2157, former, development, code, snap, 37889, drug, which, acts, selective, peptide, antagonist, receptor, which, usually, activated, neuropeptide, galanin, blocking, this, receptor, with, produced, increased, serotonin, release, well, producing, antidepressan. 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 HT 2157Clinical dataATC codenoneIdentifiersIUPAC name 1 Phenyl 3 3 trifluoromethyl phenyl iminoindol 2 oneCAS Number303149 14 6PubChem CID1471834IUPHAR BPS6126ChemSpider1213983UNIIJ4DRJ9BFS1Chemical and physical dataFormulaC 21H 13F 3N 2OMolar mass366 343 g mol 13D model JSmol Interactive imageSMILES c14ccccc4n c3ccccc3 c O c1 N c c2 cccc2C F F FInChI 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 NReferences Edit pA2 Online www pa2online org Swanson CJ Blackburn TP Zhang X Zheng K Xu ZQ Hokfelt T et al November 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 of the United States of America 102 48 17489 94 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 This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title HT 2157 amp oldid 1136546834, wikipedia, wiki, book, books, library,

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