Human δ opioid receptor: A stable cell line for functional studies of opioids

Ewa Malatynska; Yu Wang; Richard J. Knapp; Giovanna Santoro; Xaoping Li; Sue Waite; William R. Roeske; Henry I. Yamamura

doi:10.1097/00001756-199503000-00007

Human δ opioid receptor: A stable cell line for functional studies of opioids

Ewa Malatynska, Yu Wang, Richard J. Knapp, Giovanna Santoro, Xaoping Li, Sue Waite, William R. Roeske, Henry I. Yamamura

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

29 Scopus citations

Abstract

A Human δ opioid receptor cDNA clone (pREPIO/ hDOR) was transfected into Chinese hamster ovary (CHO) cells. The stable cell line expressed a high density of δ opioid receptors (137 000 ± 21 600 receptors/cell). DPDPE inhibited 90% of the forskolin-stimulated cAMP accumulation in these cells with high potency (EC₅₀ = 1.3 nM). This effect of DPDPE was antagonized by nal-trindole. The pseudo-pA₂ value (K_e)of 155 pM for naltrin-dole is consistent with that measured for δ receptor antagonism in the mouse vas deferens. This is the first detailed characterization of DPDPE activity on forskolin-stimulated cAMP accumulation mediated through a human δ opioid receptor. The data support the use of the recombinant cell line for functional studies of opioid drugs.

Original language	English (US)
Pages (from-to)	613-616
Number of pages	4
Journal	NeuroReport
Volume	6
Issue number	4
DOIs	https://doi.org/10.1097/00001756-199503000-00007
State	Published - Mar 1995

Keywords

Adenylyl cyclase
CHO cells
Camp
DPDPE
Human δ opioid receptor
Naltrindole
Radioligand binding
Stable expression
Transfection

ASJC Scopus subject areas

General Neuroscience

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10.1097/00001756-199503000-00007

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title = "Human δ opioid receptor: A stable cell line for functional studies of opioids",

abstract = "A Human δ opioid receptor cDNA clone (pREPIO/ hDOR) was transfected into Chinese hamster ovary (CHO) cells. The stable cell line expressed a high density of δ opioid receptors (137 000 ± 21 600 receptors/cell). DPDPE inhibited 90% of the forskolin-stimulated cAMP accumulation in these cells with high potency (EC50 = 1.3 nM). This effect of DPDPE was antagonized by nal-trindole. The pseudo-pA2 value (Ke)of 155 pM for naltrin-dole is consistent with that measured for δ receptor antagonism in the mouse vas deferens. This is the first detailed characterization of DPDPE activity on forskolin-stimulated cAMP accumulation mediated through a human δ opioid receptor. The data support the use of the recombinant cell line for functional studies of opioid drugs.",

keywords = "Adenylyl cyclase, CHO cells, Camp, DPDPE, Human δ opioid receptor, Naltrindole, Radioligand binding, Stable expression, Transfection",

author = "Ewa Malatynska and Yu Wang and Knapp, {Richard J.} and Giovanna Santoro and Xaoping Li and Sue Waite and Roeske, {William R.} and Yamamura, {Henry I.}",

year = "1995",

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doi = "10.1097/00001756-199503000-00007",

language = "English (US)",

volume = "6",

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T2 - A stable cell line for functional studies of opioids

AU - Malatynska, Ewa

AU - Wang, Yu

AU - Knapp, Richard J.

AU - Santoro, Giovanna

AU - Li, Xaoping

AU - Waite, Sue

AU - Roeske, William R.

AU - Yamamura, Henry I.

PY - 1995/3

Y1 - 1995/3

N2 - A Human δ opioid receptor cDNA clone (pREPIO/ hDOR) was transfected into Chinese hamster ovary (CHO) cells. The stable cell line expressed a high density of δ opioid receptors (137 000 ± 21 600 receptors/cell). DPDPE inhibited 90% of the forskolin-stimulated cAMP accumulation in these cells with high potency (EC50 = 1.3 nM). This effect of DPDPE was antagonized by nal-trindole. The pseudo-pA2 value (Ke)of 155 pM for naltrin-dole is consistent with that measured for δ receptor antagonism in the mouse vas deferens. This is the first detailed characterization of DPDPE activity on forskolin-stimulated cAMP accumulation mediated through a human δ opioid receptor. The data support the use of the recombinant cell line for functional studies of opioid drugs.

AB - A Human δ opioid receptor cDNA clone (pREPIO/ hDOR) was transfected into Chinese hamster ovary (CHO) cells. The stable cell line expressed a high density of δ opioid receptors (137 000 ± 21 600 receptors/cell). DPDPE inhibited 90% of the forskolin-stimulated cAMP accumulation in these cells with high potency (EC50 = 1.3 nM). This effect of DPDPE was antagonized by nal-trindole. The pseudo-pA2 value (Ke)of 155 pM for naltrin-dole is consistent with that measured for δ receptor antagonism in the mouse vas deferens. This is the first detailed characterization of DPDPE activity on forskolin-stimulated cAMP accumulation mediated through a human δ opioid receptor. The data support the use of the recombinant cell line for functional studies of opioid drugs.

KW - Adenylyl cyclase

KW - CHO cells

KW - Camp

KW - DPDPE

KW - Human δ opioid receptor

KW - Naltrindole

KW - Radioligand binding

KW - Stable expression

KW - Transfection

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AN - SCOPUS:0028950666

SN - 0959-4965

VL - 6

SP - 613

EP - 616

JO - NeuroReport

JF - NeuroReport

IS - 4

ER -

Human δ opioid receptor: A stable cell line for functional studies of opioids

Abstract

Keywords

ASJC Scopus subject areas

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