Section 12
Chapter 11,337

Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole

Clayson, J.; Jales, A.; Tyacke, R.J.; Hudson, A.L.; Nutt, D.J.; Lewis, J.W.; Husbands, S.M.

Bioorganic and Medicinal Chemistry Letters 11(7): 939-943


ISSN/ISBN: 0960-894X
PMID: 11294396
DOI: 10.1016/s0960-894x(01)00112-3
Accession: 011336469

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 higher 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.

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