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 language||English (US)|
|Number of pages||9|
|State||Published - Jan 1 1993|