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.
MeSH terms
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Alkylation
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Animals
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Arachidonic Acids / antagonists & inhibitors*
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Arachidonic Acids / metabolism
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Biological Transport / drug effects
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COS Cells / drug effects
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Cell Line, Tumor / drug effects
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Chlorocebus aethiops
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Endocannabinoids
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Humans
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Inhibitory Concentration 50
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Magnetic Resonance Spectroscopy
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Models, Chemical
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Polyunsaturated Alkamides / antagonists & inhibitors*
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Polyunsaturated Alkamides / metabolism
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Structure-Activity Relationship
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Tetrazoles / chemical synthesis
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Tetrazoles / pharmacology*
Substances
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Arachidonic Acids
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Endocannabinoids
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Polyunsaturated Alkamides
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Tetrazoles
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anandamide