δ-opioid receptor: The third extracellular loop determines naltrindole selectivity

Xiaoping Li; Eva V. Varga; Dagmar Stropova; Teresa Zalewska; Ewa Malatynska; Richard J. Knapp; William R. Roeske; Henry I. Yamamura

doi:10.1016/0014-2999(96)00098-2

δ-opioid receptor: The third extracellular loop determines naltrindole selectivity

Xiaoping Li, Eva V. Varga, Dagmar Stropova, Teresa Zalewska, Ewa Malatynska, Richard J. Knapp, William R. Roeske, Henry I. Yamamura

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

25 Scopus citations

Abstract

Human δ/μ-opioid receptor chimeras were constructed to determine the role of the second and third extracellular loops in alkaloid ligand selectivity. Exchanging the third extracellular loop of the δ-opioid receptor with that of the μ-opioid receptor dramatically decreased the affinity of naltrindole, but not that of morphine. The results suggest that different domains of the opioid receptor are involved in the binding of naltrindole and morphine.

Original language	English (US)
Pages (from-to)	R1-R2
Journal	European Journal of Pharmacology
Volume	300
Issue number	1-2
DOIs	https://doi.org/10.1016/0014-2999(96)00098-2
State	Published - Apr 4 1996

Keywords

Binding site
Human
Opiate
Opioid receptor

ASJC Scopus subject areas

Pharmacology

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10.1016/0014-2999(96)00098-2

Cite this

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title = "δ-opioid receptor: The third extracellular loop determines naltrindole selectivity",

abstract = "Human δ/μ-opioid receptor chimeras were constructed to determine the role of the second and third extracellular loops in alkaloid ligand selectivity. Exchanging the third extracellular loop of the δ-opioid receptor with that of the μ-opioid receptor dramatically decreased the affinity of naltrindole, but not that of morphine. The results suggest that different domains of the opioid receptor are involved in the binding of naltrindole and morphine.",

keywords = "Binding site, Human, Opiate, Opioid receptor",

author = "Xiaoping Li and Varga, {Eva V.} and Dagmar Stropova and Teresa Zalewska and Ewa Malatynska and Knapp, {Richard J.} and Roeske, {William R.} and Yamamura, {Henry I.}",

note = "Funding Information: This work was supportedin part by grantsf rom the NIDA andt heA rizonaD iseaseC ontrolR esearchC ommis-sion. We thankC arol Hausslear ndM ichelleT hatchefro r assistancien maintainintgh eCOS-7 cell line.",

year = "1996",

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doi = "10.1016/0014-2999(96)00098-2",

language = "English (US)",

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pages = "R1--R2",

journal = "European Journal of Pharmacology",

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publisher = "Elsevier B.V.",

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TY - JOUR

T1 - δ-opioid receptor

T2 - The third extracellular loop determines naltrindole selectivity

AU - Li, Xiaoping

AU - Varga, Eva V.

AU - Stropova, Dagmar

AU - Zalewska, Teresa

AU - Malatynska, Ewa

AU - Knapp, Richard J.

AU - Roeske, William R.

AU - Yamamura, Henry I.

N1 - Funding Information: This work was supportedin part by grantsf rom the NIDA andt heA rizonaD iseaseC ontrolR esearchC ommis-sion. We thankC arol Hausslear ndM ichelleT hatchefro r assistancien maintainintgh eCOS-7 cell line.

PY - 1996/4/4

Y1 - 1996/4/4

N2 - Human δ/μ-opioid receptor chimeras were constructed to determine the role of the second and third extracellular loops in alkaloid ligand selectivity. Exchanging the third extracellular loop of the δ-opioid receptor with that of the μ-opioid receptor dramatically decreased the affinity of naltrindole, but not that of morphine. The results suggest that different domains of the opioid receptor are involved in the binding of naltrindole and morphine.

AB - Human δ/μ-opioid receptor chimeras were constructed to determine the role of the second and third extracellular loops in alkaloid ligand selectivity. Exchanging the third extracellular loop of the δ-opioid receptor with that of the μ-opioid receptor dramatically decreased the affinity of naltrindole, but not that of morphine. The results suggest that different domains of the opioid receptor are involved in the binding of naltrindole and morphine.

KW - Binding site

KW - Human

KW - Opiate

KW - Opioid receptor

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U2 - 10.1016/0014-2999(96)00098-2

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SN - 0014-2999

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SP - R1-R2

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 1-2

ER -

δ-opioid receptor: The third extracellular loop determines naltrindole selectivity

Abstract

Keywords

ASJC Scopus subject areas

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