| Abstract
| - A series consisting of spiroindanyl (5−7),benzospiroindanyl (8−10), andspiroperinaphthyl(11) derivatives of naltrexone and oxymorphone weresynthesized in order to investigate therole of an orthogonal-oriented “address” for δ opioid receptors.All of the ligands exhibited apreference for δ receptors in vitro. The 7-benzospiroindanylderivative 8 (BSINTX) was themost selective δ opioid receptor antagonist in vitro. In miceBSINTX antagonized the δ1-selective agonist,[d-Pen2,d-Pen5]enkephalinwithout significantly affecting the antinociceptivepotency of δ2, μ, and κ agonists. The results ofthis study are consistent with an orthogonally-oriented address favoring δ1 activity.
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