title: New tetrazole-based selective anandamide uptake inhibitors.
abstract: A new series of 1,5- and 2,5-disubstituted tetrazoles have been synthesized and evaluated as inhibitors of anandamide cellular uptake. Some of them inhibit the uptake process with a relatively high potency (IC(50)=2.3-5.1microM) and selectively over other proteins involved in endocannabinoid action and metabolism.
authors.affiliation: Dipartimento di Studi Farmaceutici, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy. giorgio.ortar@uniroma1.it
authors.forename: Giorgio
authors.initials: G
authors.lastname: Ortar
authors.forename: Aniello
authors.initials: A
authors.lastname: Schiano Moriello
authors.forename: Maria Grazia
authors.initials: MG
authors.lastname: Cascio
authors.forename: Luciano
authors.initials: L
authors.lastname: De Petrocellis
authors.forename: Alessia
authors.initials: A
authors.lastname: Ligresti
authors.forename: Enrico
authors.initials: E
authors.lastname: Morera
authors.forename: Marianna
authors.initials: M
authors.lastname: Nalli
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Di Marzo
mesh_terms: D000478:Alkylation; D000818:Animals; D001095:Arachidonic Acids / Q000037:antagonists & inhibitors* / Q000378:metabolism; D001692:Biological Transport / Q000187:drug effects; D019556:COS Cells / Q000187:drug effects; D045744:Cell Line, Tumor / Q000187:drug effects; D002522:Chlorocebus aethiops; D063388:Endocannabinoids; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D053284:Polyunsaturated Alkamides / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D001095:Arachidonic Acids; D063388:Endocannabinoids; D053284:Polyunsaturated Alkamides; D013777:Tetrazoles; C078814:anandamide