Background: Transport inhibitors modulate endocannabinoid signaling by inhibiting their uptake through unknown mechanisms. Results: Effects of transport inhibitors upon endocannabinoid uptake and intracellular trafficking were lost in the absence of fatty acid-binding proteins. Conclusion: Fatty acid-binding proteins are physiological targets of transport inhibitors. Significance: These findings identify drug targets for modulating endocannabinoid signaling.
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