publication . Article . 2006

Pharmacological Characterization of Hydrolysis-Resistant Analogs of Oleoylethanolamide with Potent Anorexiant Properties

Giuseppe Astarita; Barbara Di Giacomo; Silvana Gaetani; Fariba Oveisi; Timothy R. Compton; Silvia Rivara; Giorgio Tarzia; Marco Mor; Daniele Piomelli;
Open Access
  • Published: 20 Jul 2006 Journal: Journal of Pharmacology and Experimental Therapeutics, volume 318, pages 563-570 (issn: 0022-3565, eissn: 1521-0103, Copyright policy)
  • Publisher: American Society for Pharmacology & Experimental Therapeutics (ASPET)
  • Country: United States
Abstract
Oleoylethanolamide (OEA) is an endogenous lipid mediator that reduces food intake, promotes lipolysis, and decreases body weight gain in rodents by activating peroxisome proliferator-activated receptor-α (PPAR-α). The biological effects of OEA are terminated by two intracellular lipid hydrolase enzymes, fatty-acid amide hydrolase and N-acylethanolamine-hydrolyzing acid amidase. In the present study, we describe OEA analogs that resist enzymatic hydrolysis, activate PPAR-α with high potency in vitro, and persistently reduce feeding when administered in vivo either parenterally or orally. The most potent of these compounds, (Z)-(R)-9-octadecenamide,N-(2- hydroxyet...
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free text keywords: Molecular Medicine, Pharmacology, Lipolysis, Biology, Oral administration, Endogeny, Hydrolase, In vivo, Amidase, Oleoylethanolamide, chemistry.chemical_compound, chemistry, Agonist, medicine.drug_class, medicine
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