The design of delta-selective opioid receptor antagonists
Portoghese, P.S.
Farmaco 48(2): 243-251
1993
ISSN/ISBN: 0014-827X PMID: 8388215 Document Number: 411860
Naltrexone-derived antagonists which are highly selective for delta 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 delta receptors, and a closely related benzofuran analogue, NTB 2, is a selective delta 2 antagonist. The fact that 7-benzylidenenaltrexone (BNTX) was found to be a delta 1 antagonist suggests that the conformation of the putative delta address component (phenyl group) of BNTX plays a role in modulating delta subtype selectivity.
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