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Vol. 292, Issue 3, 960-967, March 2000
Department of Medicinal Chemistry and Molecular Pharmacology,
Purdue University School of Pharmacy and Pharmacal Sciences, West
Lafayette, Indiana (F.R., T.A.D., E.L.B.); Center for Molecular
Neuroscience and Department of Pharmacology, Vanderbilt University
School of Medicine, Nashville, Tennessee (R.D.B.)
Anandamide (N-arachidonylethanolamide) is an endogenous
cannabinoid that mimics the pharmacologic effects of
9-tetrahydrocannabinol, the major bioactive
substance in marijuana. Anandamide appears to be synthesized, released,
and inactivated by mechanisms similar to those for other
neurotransmitters. Of interest to the present studies are reports that
anandamide undergoes carrier-mediated uptake into neuronal or glial
cells after release, followed by rapid intracellular degradation by the
intracellular fatty acid amidohydrolase. In addition to effects in the
brain, anandamide has multiple effects in the periphery, particularly on cells of the immune system that express both a peripheral
cannabinoid receptor and amidohydrolase enzyme. We have performed a
detailed characterization of anandamide uptake in the cognate mast cell line RBL-2H3 to test the hypothesis that the uptake system in peripheral cells is also carrier-mediated and functionally similar to
that observed in the central nervous system. RBL-2H3 cells exhibited
robust, saturable transport of [3H]anandamide that was
both time- and temperature-sensitive. This transport activity was not
dependent on extracellular ion gradients for uptake and was inhibited
selectively by other fatty acid-derived molecules, anandamide
congeners, and the psychoactive cannabinoids such as
9-tetrahydrocannabinol. We conclude that anandamide
transport in the RBL-2H3 cells is carrier-mediated, and uptake in
peripheral cells is functionally and pharmacologically identical with
that observed in neurons and astrocytes.
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