Communication

Synthesis and Pharmacological Activity of a Potent Inhibitor of the Biosynthesis of the Endocannabinoid 2-Arachidonoylglycerol

  1. Tiziana Bisogno1,
  2. James J. Burston2,
  3. Ravi Rai3,
  4. Marco Allarà1,
  5. Bijali Saha3,
  6. Anu Mahadevan3,
  7. Raj K. Razdan3,
  8. Jenny L. Wiley2,
  9. Vincenzo Di Marzo1

Article first published online: 5 MAR 2009

DOI: 10.1002/cmdc.200800442

Issue

ChemMedChem

ChemMedChem

Special Issue: XIX NMMC Verona 2008

Volume 4, Issue 6, pages 946–950, June 8, 2009

Additional Information

How to Cite

Bisogno, T., Burston, James J., Rai, R., Allarà, M., Saha, B., Mahadevan, A., Razdan, Raj K., Wiley, Jenny L. and Di Marzo, V. (2009), Synthesis and Pharmacological Activity of a Potent Inhibitor of the Biosynthesis of the Endocannabinoid 2-Arachidonoylglycerol. ChemMedChem, 4: 946–950. doi: 10.1002/cmdc.200800442

Author Information

  1. 1

    Endocannabinoid Research Group, Institute of Biomolecular Chemistry, Consiglio Nazionale delle Ricerche, Via Campi Flegrei 34, Comprensorio Olivetti, Pozzuoli (NA) (Italy), Fax.: (+39) 081-8041770

  2. 2

    Department of Pharmacology and Toxicology, Virginia Commonwealth University, 410 North 12th St., Rm 746, P.O. Box 980613, Richmond, VA 23298 (USA)

  3. 3

    Organix Inc., 240 Salem St., Woburn, MA 01801 (USA)

Publication History

  1. Issue published online: 28 MAY 2009
  2. Article first published online: 5 MAR 2009
  3. Manuscript Revised: 3 FEB 2009
  4. Manuscript Received: 18 DEC 2008

Funded by

  • National Institutes of Health. Grant Numbers: DA-09789, DA-03672, DA 008904, DA-05488

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Keywords:

  • biosynthesis;
  • CB1;
  • DAGL;
  • endocannabinoids;
  • cannabinoids;
  • receptors

Abstract

Thumbnail image of graphical abstract

Biosynthesis Inhibition: O-5596, a new inhibitor of the biosynthesis of the endocannabinoid, 2-arachidonoylglycerol, was synthesized and found to be potent (IC50=100 nM) and selective versus other proteins and enzymes of the endocannabinoid system in vitro and active in vivo at reducing food intake in mice.

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