5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist

Robert M. Jones, Philip S. Portoghese

Research output: Contribution to journalArticle

71 Citations (Scopus)

Abstract

5'-Guanidinonaltrindole (GNTI) possesses 5-fold greater opioid antagonist potency (K(e)=0.04 nM) and an order of magnitude greater selectivity (selectivity ratios >500) than the prototypical κ-opioid receptor antagonist, norbinaltorphimine, in smooth muscle preparations. Binding and functional studies conducted on cloned human opioid receptors expressed in Chinese hamster ovarian (CHO) cells afforded pA2 values that were comparable to the smooth muscle data. In view of the high selectivity and potency of GNTI, it is a potentially valuable pharmacological tool for opioid research. Copyright (C) 2000 Elsevier Science B.V.

Original languageEnglish (US)
Pages (from-to)49-52
Number of pages4
JournalEuropean Journal of Pharmacology
Volume396
Issue number1
DOIs
StatePublished - May 12 2000

Fingerprint

Narcotic Antagonists
Smooth Muscle
Opioid Receptors
Cricetulus
Opioid Analgesics
Pharmacology
Research
17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan
norbinaltorphimine

Keywords

  • Binding
  • Norbinaltorphimine
  • κ-Opioid receptor

Cite this

5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist. / Jones, Robert M.; Portoghese, Philip S.

In: European Journal of Pharmacology, Vol. 396, No. 1, 12.05.2000, p. 49-52.

Research output: Contribution to journalArticle

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