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Titolo:
Analogues and homologues of N-palmitoylethanolamide, a putative endogenousCB2 cannabinoid, as potential ligands for the cannabinoid receptors
Autore:
Lambert, DM; DiPaolo, FG; Sonveaux, P; Kanyonyo, M; Govaerts, SJ; Hermans, E; Bueb, JL; Delzenne, NM; Tschirhart, EJ;
Indirizzi:
Univ Catholique Louvain, Unite Chim Pharmaceut & Radiopharm, Dept Pharmaceut Sci, B-1200 Brussels, Belgium Univ Catholique Louvain Brussels BelgiumB-1200 B-1200 Brussels, Belgium Univ Catholique Louvain, Fac Med, Unite Pharmacol Expt, Dept Physiol & Pharmacol, B-1200 Brussels, Belgium Univ Catholique Louvain Brussels BelgiumB-1200 B-1200 Brussels, Belgium Univ Catholique Louvain, Unite Pharmacocinet Metab Nutr & Toxicol, Dept Pharmaceut Sci, B-1200 Brussels, Belgium Univ Catholique Louvain Brussels Belgium B-1200 B-1200 Brussels, Belgium Ctr Rech Publ Sante, L-1150 Luxembourg, Luxembourg Ctr Rech Publ Sante Luxembourg Luxembourg L-1150 Luxembourg, Luxembourg
Titolo Testata:
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS
fascicolo: 2-3, volume: 1440, anno: 1999,
pagine: 266 - 274
SICI:
1388-1981(19990922)1440:2-3<266:AAHONA>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
MUCOSAL MAST-CELL; ANANDAMIDE; BRAIN; BINDING; RAT; IDENTIFICATION; LOCALIZATION; INHIBITION;
Keywords:
palmitoylethanolamide; endocannabinoid; CB1 and CB2 cannabinoid receptors; N-acylethanolamine;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
32
Recensione:
Indirizzi per estratti:
Indirizzo: Lambert, DM Univ Catholique Louvain, Unite Chim Pharmaceut & Radiopharm, Dept Pharmaceut Sci, UCL 7340,Ave Mounier 73, B-1200 Brussels, Belgium Univ Catholique Louvain UCL 7340,Ave Mounier 73 Brussels Belgium B-1200
Citazione:
D.M. Lambert et al., "Analogues and homologues of N-palmitoylethanolamide, a putative endogenousCB2 cannabinoid, as potential ligands for the cannabinoid receptors", BBA-MOL C B, 1440(2-3), 1999, pp. 266-274

Abstract

The presence of CB2 receptors was reported in the rat basophilic cell lineRBL-2H3 and N-palmitoylethanolamide was proposed as an endogenous, potent agonist of this receptor. We synthesized a series of 10 N-palmitoylethanolamide homologues and analogues, varying by the elongation of the fatty acid chain from caproyl to stearoyl and by the nature of the amide substituent, respectively, and evaluated the affinity of these compounds to cannabinoid receptors in the rat spleen, RBL-2H3 cells and CHO-CB1 and CHO-CB2 receptor-transfected cells. In rat spleen slices, CB2 receptors were the predominant form of the cannabinoid receptors. No binding of [H-3]SR141716A was observed. [H-3]CP-55,940 binding was displaced by WIN 55,212-2 and anandamide. No displacement of [H-3]CP-55,940 or [H-3]WIN 55,212-2 by palmitoylethanolamide derivatives was observed in rat spleen slices. In RBL-2H3 cells, no binding of [H-3]CP-55,940 or [H-3]WIN 55,212-2 could be observed and conversely, no inhibitory activity of N-palmitoylethanolamide derivatives and analogues was measurable. These compounds do not recognize the human CB1 and CB2 receptors expressed in CHO cells. In conclusion, N-palmitoylethanolamide was, in our preparations, a weak ligand while its synthesized homologues or analogues were essentially inactive. Therefore, it seems unlikely that N-palmitoylethanolamide is an endogenous agonist of the CB2 receptors but it maybe a compound with potential therapeutic applications since it may act viaother mechanisms than cannabinoid CB1-CB2 receptor interactions. (C) 1999 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 16:09:50