TM-38837

TM-38837 is a small molecule inverse agonist/antagonist of the CB1 cannabinoid receptor, with peripheral selectivity. It is being developed for the treatment of obesity and metabolic disorders by 7TM Pharma.[1] The company has announced phase I clinical trials.

TM-38837
Clinical data
ATC code
  • none
Identifiers
IUPAC name
  • 1-(2,4-Dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC30H25Cl2F3N4OS
Molar mass617.51 g·mol−1
3D model (JSmol)
SMILES
  • O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(C#CC4=CC=C(C(F)(F)F)C=C4)S3)=C1CC)NN5CCCCC5
InChI
  • InChI=1S/C30H25Cl2F3N4OS/c1-2-23-27(29(40)37-38-16-4-3-5-17-38)36-39(25-14-11-21(31)18-24(25)32)28(23)26-15-13-22(41-26)12-8-19-6-9-20(10-7-19)30(33,34)35/h6-7,9-11,13-15,18H,2-5,16-17H2,1H3,(H,37,40)
  • Key:VQOCBFYUDSBDCZ-UHFFFAOYSA-N

TM-38837 is among the first of a new generation of cannabinoid receptor antagonist designed to avoid the central nervous system liabilities of the first generation CB1 receptor antagonists such as rimonabant.[2]

See also

References
  1. "7TM Pharma". Archived from the original on July 7, 2011. Retrieved January 18, 2011.
  2. Hung MS, Chang CP, Li TC, Yeh TK, Song JS, Lin Y, et al. (September 2010). "Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist". ChemMedChem. 5 (9): 1439–43. doi:10.1002/cmdc.201000246. PMID 20652930. S2CID 34244587.
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