Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 7, Pages 939-943Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(01)00112-3
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- NIDA NIH HHS [DA 00254] Funding Source: Medline
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Two series of delta -selective ligands related to the prototypic delta -antagonist naltrindole have been prepared and evaluated in opioid binding assays with the aim of developing new PET ligands for the delta -opioid receptor. One compound (5d) had significantly here selectivity than naltrindole, but with substantially reduced binding affinity. For those compounds retaining similar affinity to naltrindole. those having ethyl and fluoroethyl substituents afforded the highest levels of selectivity. However, none of the compounds combined the high level of affinity and selectivity ideally suited to the development of an imaging agent. (C) 2001 Elsevier Science Ltd. All rights reserved.
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