α-Methylated derivatives of 2-arachidonoyl glycerol: Synthesis, CB1 receptor activity, and enzymatic stability

α-Methylated analogues of the endogenous cannabinoid, 2-arachidonoyl glycerol (2-AG), were synthesized aiming to the improved enzymatic stability of 2-AG. In addition, the CB1 activity properties of fluoro derivatives of 2-AG were studied. The CB1 receptor activity was determined by the [ 35S]GTPγS...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-05, Vol.16 (9), p.2437-2440
Hauptverfasser:	Parkkari, Teija, Myllymäki, Mikko, Savinainen, Juha R., Saario, Susanna M., Castillo-Meléndez, Joel A., Laitinen, Jarmo T., Nevalainen, Tapio, Koskinen, Ari M.P., Järvinen, Tomi
Format:	Artikel
Sprache:	eng
Schlagworte:	2-AG Animals Arachidonic Acids - chemical synthesis Arachidonic Acids - chemistry Arachidonic Acids - pharmacology Biological and medical sciences Cannabinoid CB1 receptor Cell Membrane - drug effects Cell Membrane - enzymology Cerebellum - drug effects Cerebellum - enzymology Endocannabinoids Enzymatic stability Enzyme Stability - drug effects Glycerides - chemical synthesis Glycerides - chemistry Glycerides - pharmacology Medical sciences Methylation Miscellaneous Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Rats Receptor, Cannabinoid, CB1 - agonists Stereoisomerism Stereoselective synthesis Structure-Activity Relationship
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