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

Robert M. Jones; Philip S. Portoghese

doi:10.1016/S0014-2999(00)00208-9

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

Robert M. Jones, Philip S. Portoghese

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-review

74 Scopus citations

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 language	English (US)
Pages (from-to)	49-52
Number of pages	4
Journal	European Journal of Pharmacology
Volume	396
Issue number	1
DOIs	https://doi.org/10.1016/S0014-2999(00)00208-9
State	Published - May 12 2000

Keywords

Binding
Norbinaltorphimine
κ-Opioid receptor

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T1 - 5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist

AU - Jones, Robert M.

AU - Portoghese, Philip S.

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N2 - 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.

AB - 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.

KW - Binding

KW - Norbinaltorphimine

KW - κ-Opioid receptor

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