Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 12, Issue 19, Pages 5161-5169Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2004.07.026
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A new series of anandamide and N-oleoylethanolamine analogs, most of which with aromatic moieties in the head group region, has been synthesized and evaluated as inhibitors of anandamide uptake. Some of them efficaciously inhibit the uptake process with K-i values in the low micromolar range (2.4-21.2 muM). Strict structural requisites are needed to observe a significant inhibition and in no case inhibition of fatty acid amidohydrolase overlaps with inhibition of anandamide uptake. (C) 2004 Elsevier Ltd. All rights reserved.
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