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

86 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

Bibliographical note

Funding Information:
This investigation was supported by the National Institute on Drug Abuse. We thank the Opiate Treatment Discovery Program for supplying the human cloned receptor data, and we thank Mike Powers and Veronika Phillips for their competent technical assistance in generating the smooth muscle data.

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Binding
Norbinaltorphimine
κ-Opioid receptor

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10.1016/S0014-2999(00)00208-9

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

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.",

keywords = "Binding, Norbinaltorphimine, κ-Opioid receptor",

author = "Jones, \{Robert M.\} and Portoghese, \{Philip S.\}",

note = "Funding Information: This investigation was supported by the National Institute on Drug Abuse. We thank the Opiate Treatment Discovery Program for supplying the human cloned receptor data, and we thank Mike Powers and Veronika Phillips for their competent technical assistance in generating the smooth muscle data.",

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

AU - Jones, Robert M.

AU - Portoghese, Philip S.

N1 - Funding Information: This investigation was supported by the National Institute on Drug Abuse. We thank the Opiate Treatment Discovery Program for supplying the human cloned receptor data, and we thank Mike Powers and Veronika Phillips for their competent technical assistance in generating the smooth muscle data.

PY - 2000/5/12

Y1 - 2000/5/12

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

UR - https://www.scopus.com/pages/publications/0034640189

UR - https://www.scopus.com/pages/publications/0034640189#tab=citedBy

U2 - 10.1016/S0014-2999(00)00208-9

DO - 10.1016/S0014-2999(00)00208-9

M3 - Article

C2 - 10822054

AN - SCOPUS:0034640189

SN - 0014-2999

VL - 396

SP - 49

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JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 1

ER -

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

Abstract

Bibliographical note

UN SDGs

Keywords

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