The design of δ-selective opioid receptor antagonists

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Abstract

Naltrexone-derived antagonists which are highly selective for δ opioid receptors have been designed using the message-address concept. The prototypical member of this series, naltrindole 1, possesses very high affinity and selectivity for δ receptors, and a closely related benzofuran analogue, NTB 2, is a selective δ2 antagonist. The fact that 7-benzylidenenaltrexone (BNTX) was found to be a δ1 antagonist suggests that the conformation of the putative δ address component (phenyl group) of BNTX plays a role in modulating δ subtype selectivity.

Original languageEnglish (US)
Pages (from-to)243-251
Number of pages9
JournalFarmaco
Volume48
Issue number2
StatePublished - Jan 1 1993

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