Velneperit

Velneperit (S-2367) is a drug developed by Shionogi, which acts as a potent and selective antagonist for the Neuropeptide Y receptor Y5. It has anorectic effects and was developed as a possible treatment for obesity, but was discontinued from further development after disappointing results in Phase II clinical trials. However it was still considered a successful proof of concept of the potential of Y5 receptor antagonists as possible anti-obesity agents in future.[1][2][3]

Velneperit
Clinical data
ATC code
  • None
Identifiers
IUPAC name
  • trans-4-(tert-butylsulfonylamino)-N-[5-(trifluoromethyl)pyridin-2-yl]cyclohexane-1-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H24F3N3O3S
Molar mass407.45 g·mol−1
3D model (JSmol)
SMILES
  • CC(C)(C)S(=O)(=O)NC2CCC(CC2)C(=O)Nc1ncc(C(F)(F)F)cc1
InChI
  • InChI=1S/C17H24F3N3O3S/c1-16(2,3)27(25,26)23-13-7-4-11(5-8-13)15(24)22-14-9-6-12(10-21-14)17(18,19)20/h6,9-11,13,23H,4-5,7-8H2,1-3H3,(H,21,22,24)/t11-,13-
  • Key:WGEWUYACXPEFPO-AULYBMBSSA-N

References

  1. Yukioka H (November 2010). "[A potent and selective neuropeptide Y Y5-receptor antagonist, S-2367, as an anti-obesity agent]". Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica (in Japanese). 136 (5): 270–4. doi:10.1254/fpj.136.270. PMID 21079365.
  2. Oda S, Manaka K, Kakiya K, Hozumi Y, Fukui Y, Omura S, et al. (April 2015). "Development of an Optimized Synthetic and Purification Process of S-2367 (Velneperit), a Novel Neuropeptide Y (NPY) Y5 Receptor Antagonist". Organic Process Research & Development. 19 (4): 531–6. doi:10.1021/acs.oprd.5b00023.
  3. George M, Rajaram M, Shanmugam E (January 2014). "New and emerging drug molecules against obesity". Journal of Cardiovascular Pharmacology and Therapeutics. 19 (1): 65–76. doi:10.1177/1074248413501017. PMID 24064009. S2CID 34327832.


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