N-Benzylnaltrindoles as Long-Acting δ-Opioid Receptor Antagonists

V. L. Korlipara, A. E. Takemori, P. S. Portoghese

Research output: Contribution to journalArticlepeer-review

25 Scopus citations

Abstract

The indolic nitrogen of the δ-opioid receptor antagonist, naltrindole (1), was derivatized with benzyl or substituted benzyl to afford a series (2-9) that retained δ-opioid receptor antagonist activity and selectivity in vitro. The two most potent members (2 and 8) of the series were evaluated in mice and were found to produce δ-selective antagonism of [d-Ser2,Leu5] enkephalin-Thr6 which lasted 5 days. N-Benzylnaltrindole (2) should be useful as a δ2-selective antagonist for in vivo studies where prolonged action is desired.

Original languageEnglish (US)
Pages (from-to)1882-1885
Number of pages4
JournalJournal of medicinal chemistry
Volume37
Issue number12
DOIs
StatePublished - Jun 1 1994

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