New tetrazole-based selective anandamide uptake inhibitors.
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.
Ortar
Giorgio
G
Dipartimento di Studi Farmaceutici, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy. giorgio.ortar@uniroma1.it
Schiano Moriello
Aniello
A
Cascio
Maria Grazia
MG
De Petrocellis
Luciano
L
Ligresti
Alessia
A
Morera
Enrico
E
Nalli
Marianna
M
Di Marzo
Vincenzo
V
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*
D001095:Arachidonic Acids; D063388:Endocannabinoids; D053284:Polyunsaturated Alkamides; D013777:Tetrazoles; C078814:anandamide