Metabolically labile cannabinoid esters: a 'soft drug' approach for the development of cannabinoid-based therapeutic drugs.
Biphenylic ester derivatives, designed by using a 'soft-drug' approach, proved to possess good binding properties toward cannabinoid CB(1) and CB(2) receptors and, at the same time, their metabolically labile ester portion would promote a rapid systemic inactivation. This may constitute a possible solution to the psychotropic side effects encountered when cannabinoids are therapeutically employed as local analgesic or antiglaucoma agents.
Minutolo
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F
Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126, Pisa, Italy. minutolo@farm.unipi.it
Cascio
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MG
Carboni
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I
Bisogno
T
T
Prota
G
G
Bertini
S
S
Digiacomo
M
M
Bifulco
M
M
Di Marzo
V
V
Macchia
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M
D000700:Analgesics / Q000737:chemistry; D000818:Animals; D002186:Cannabinoids / Q000737:chemistry*; D002264:Carboxylic Acids / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004952:Esters / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008024:Ligands; D008099:Liver / Q000378:metabolism; D008956:Models, Chemical; D051381:Rats; D043882:Receptors, Cannabinoid / Q000378:metabolism*
D000700:Analgesics; D002186:Cannabinoids; D002264:Carboxylic Acids; D004952:Esters; D008024:Ligands; D043882:Receptors, Cannabinoid