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1: J Med Chem. 1997 May 23;40(11):1720-5.Click here to read Links

7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.

Ohkawa S, DiGiacomo B, Larson DL, Takemori AE, Portoghese PS.

Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis 55455, USA.

A series consisting of spiroindanyl (5-7), benzospiroindanyl (8-10), and spiroperinaphthyl (11) derivatives of naltrexone and oxymorphone were synthesized in order to investigate the role of an orthogonal-oriented "address" for delta opioid receptors. All of the ligands exhibited a preference for delta receptors in vitro. The 7-benzospiroindanyl derivative 8 (BSINTX) was the most selective delta opioid receptor antagonist in vitro. In mice BSINTX antagonized the delta 1-selective agonist, [D-Pen2,D-Pen5]enkephalin without significantly affecting the antinociceptive potency of delta 2, mu, and kappa agonists. The results of this study are consistent with an orthogonally-oriented address favoring delta 1 activity.

PMID: 9171881 [PubMed - indexed for MEDLINE]

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