Wikipedia

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
  • 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
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC30H25Cl2F3N4OS
Molar mass617.51 g·mol−1
3D model (JSmol)
  • 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=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

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References

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  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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