NTI4F: A non-peptide fluorescent probe selective for functional delta opioid receptors

Tushar Kshirsagar; Albert H. Nakano; Ping Yee Law; Robert Elde; Philip S. Portoghese

doi:10.1016/S0304-3940(98)00379-6

NTI4F: A non-peptide fluorescent probe selective for functional delta opioid receptors

Tushar Kshirsagar, Albert H. Nakano, Ping Yee Law, Robert Elde, Philip S. Portoghese

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23 Scopus citations

Abstract

A non-peptide fluorescent probe, NTI4F, has been developed for the delta (δ) opioid receptor. The probe is a potent δ-antagonist in the mouse vas deferens (MVD) smooth muscle assay and it binds to the δ opioid receptor with high affinity (K(i) = 1 nM) and selectivity. Confocal microscopy indicates that the probe binds to Madin-Darby canine kidney (MDCK) cells transfected with the δ opioid receptor. This binding can be blocked by the δ opioid receptor antagonist, naltrindole (NTI), but not by morphine or ethylketazocine (EK) which are mu (μ)- and kappa (κ)-selective ligands. This fluorescent probe should prove useful in the study of the distribution of the δ opioid receptor.

Original language	English (US)
Pages (from-to)	83-86
Number of pages	4
Journal	Neuroscience Letters
Volume	249
Issue number	2-3
DOIs	https://doi.org/10.1016/S0304-3940(98)00379-6
State	Published - Jun 19 1998

Bibliographical note

Funding Information:
We gratefully acknowledge the financial support of the National Institute on Drug Abuse. The authors would also like to thank Mike Powers and Veronika Phillips for technical assistance.

Keywords

Delta opioid receptor
Fluorescent probe
Naltrindole

UN SDGs

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

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10.1016/S0304-3940(98)00379-6

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title = "NTI4F: A non-peptide fluorescent probe selective for functional delta opioid receptors",

abstract = "A non-peptide fluorescent probe, NTI4F, has been developed for the delta (δ) opioid receptor. The probe is a potent δ-antagonist in the mouse vas deferens (MVD) smooth muscle assay and it binds to the δ opioid receptor with high affinity (K(i) = 1 nM) and selectivity. Confocal microscopy indicates that the probe binds to Madin-Darby canine kidney (MDCK) cells transfected with the δ opioid receptor. This binding can be blocked by the δ opioid receptor antagonist, naltrindole (NTI), but not by morphine or ethylketazocine (EK) which are mu (μ)- and kappa (κ)-selective ligands. This fluorescent probe should prove useful in the study of the distribution of the δ opioid receptor.",

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AU - Kshirsagar, Tushar

AU - Nakano, Albert H.

AU - Law, Ping Yee

AU - Elde, Robert

AU - Portoghese, Philip S.

N1 - Funding Information: We gratefully acknowledge the financial support of the National Institute on Drug Abuse. The authors would also like to thank Mike Powers and Veronika Phillips for technical assistance.

PY - 1998/6/19

Y1 - 1998/6/19

N2 - A non-peptide fluorescent probe, NTI4F, has been developed for the delta (δ) opioid receptor. The probe is a potent δ-antagonist in the mouse vas deferens (MVD) smooth muscle assay and it binds to the δ opioid receptor with high affinity (K(i) = 1 nM) and selectivity. Confocal microscopy indicates that the probe binds to Madin-Darby canine kidney (MDCK) cells transfected with the δ opioid receptor. This binding can be blocked by the δ opioid receptor antagonist, naltrindole (NTI), but not by morphine or ethylketazocine (EK) which are mu (μ)- and kappa (κ)-selective ligands. This fluorescent probe should prove useful in the study of the distribution of the δ opioid receptor.

AB - A non-peptide fluorescent probe, NTI4F, has been developed for the delta (δ) opioid receptor. The probe is a potent δ-antagonist in the mouse vas deferens (MVD) smooth muscle assay and it binds to the δ opioid receptor with high affinity (K(i) = 1 nM) and selectivity. Confocal microscopy indicates that the probe binds to Madin-Darby canine kidney (MDCK) cells transfected with the δ opioid receptor. This binding can be blocked by the δ opioid receptor antagonist, naltrindole (NTI), but not by morphine or ethylketazocine (EK) which are mu (μ)- and kappa (κ)-selective ligands. This fluorescent probe should prove useful in the study of the distribution of the δ opioid receptor.

KW - Delta opioid receptor

KW - Fluorescent probe

KW - Naltrindole

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JF - Neuroscience Letters

IS - 2-3

ER -

NTI4F: A non-peptide fluorescent probe selective for functional delta opioid receptors

Abstract

Bibliographical note

Keywords

UN SDGs

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