Opioid peptide receptor studies. 8. One of the mouse brain δ(NCX) binding sites is similar to the cloned mouse opioid δ receptor: Further evidence for heterogeneity of δ opioid receptors

Heng Xu, Yi Feng Lu, John S. Partilla, Julia Pinto, Sylvia N. Calderon, Dorota Matecka, Kenner C. Rice, Josephine Lai, Frank Porreca, Subramaniam Ananthan, Richard B. Rothman

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Quantitative ligand binding studies resolved two subtypes of the δ opioid receptor, termed δ(ncx1), and δ(ncx2), in mouse brain membranes depleted of μ receptors by pretreatment with the irreversible ligand, BIT. The purpose of the present study was to compare the binding parameters, ligand-selectivity profile and pharmacological properties of the cloned mouse δ receptor (MDOR) stably expressed in a cell line to the δ(ncx) binding sites of mouse brain. [3H][D-Ala2,D-Leu5]enkephalin labeled a single binding site in membranes prepared from MDOR cells under several different assay conditions including BIT-pretreatment. The MDOR had high affinity for δ agonists and antagonists. [3H][D-Ala2,D-Leu5]enkephalin labeled two binding sites in mouse brain membranes depleted of p. receptors by pretreatment with BIT: the δ(ncx1) site (high affinity for DPDPE and deltorphin) and the δ(ncx2) site (low affinity for DPDPE and deltorphin). Some agents were moderately selective for the delta(ncx2) site: [pCl]DPDPE (10.9-fold), JP41 (5.9-fold) and JP45 (3.8-fold). The K(i) values of 12 opioids at the mouse MDOR were determined. These values were highly correlated with their values at the delta(ncx1) site but not the delta(ncx2) site. These data suggest that the delta(ncx2) site may be distinct from the cloned delta opioid receptor.

Original languageEnglish (US)
Pages (from-to)343-350
Number of pages8
JournalPeptides
Volume19
Issue number2
DOIs
StatePublished - Feb 1998

Fingerprint

Peptide Receptors
Opioid Peptides
Opioid Receptors
D-Penicillamine (2,5)-Enkephalin
Brain
Enkephalins
Binding Sites
Ligands
Membranes
delta Opioid Receptor
Opioid Analgesics
Assays
Cells
2-(4-ethoxybenzyl)-1-diethylaminoethyl-5-isothiocyanatobenzimidazole
Pharmacology
Cell Line
deltorphin

Keywords

  • [D-Ala, D-Len]enkephalin
  • Delta receptors
  • Receptor subtypes

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Cellular and Molecular Neuroscience

Cite this

Opioid peptide receptor studies. 8. One of the mouse brain δ(NCX) binding sites is similar to the cloned mouse opioid δ receptor : Further evidence for heterogeneity of δ opioid receptors. / Xu, Heng; Lu, Yi Feng; Partilla, John S.; Pinto, Julia; Calderon, Sylvia N.; Matecka, Dorota; Rice, Kenner C.; Lai, Josephine; Porreca, Frank; Ananthan, Subramaniam; Rothman, Richard B.

In: Peptides, Vol. 19, No. 2, 02.1998, p. 343-350.

Research output: Contribution to journalArticle

Xu, Heng ; Lu, Yi Feng ; Partilla, John S. ; Pinto, Julia ; Calderon, Sylvia N. ; Matecka, Dorota ; Rice, Kenner C. ; Lai, Josephine ; Porreca, Frank ; Ananthan, Subramaniam ; Rothman, Richard B. / Opioid peptide receptor studies. 8. One of the mouse brain δ(NCX) binding sites is similar to the cloned mouse opioid δ receptor : Further evidence for heterogeneity of δ opioid receptors. In: Peptides. 1998 ; Vol. 19, No. 2. pp. 343-350.
@article{bf4780567df949f7a23bf995965d22c5,
title = "Opioid peptide receptor studies. 8. One of the mouse brain δ(NCX) binding sites is similar to the cloned mouse opioid δ receptor: Further evidence for heterogeneity of δ opioid receptors",
abstract = "Quantitative ligand binding studies resolved two subtypes of the δ opioid receptor, termed δ(ncx1), and δ(ncx2), in mouse brain membranes depleted of μ receptors by pretreatment with the irreversible ligand, BIT. The purpose of the present study was to compare the binding parameters, ligand-selectivity profile and pharmacological properties of the cloned mouse δ receptor (MDOR) stably expressed in a cell line to the δ(ncx) binding sites of mouse brain. [3H][D-Ala2,D-Leu5]enkephalin labeled a single binding site in membranes prepared from MDOR cells under several different assay conditions including BIT-pretreatment. The MDOR had high affinity for δ agonists and antagonists. [3H][D-Ala2,D-Leu5]enkephalin labeled two binding sites in mouse brain membranes depleted of p. receptors by pretreatment with BIT: the δ(ncx1) site (high affinity for DPDPE and deltorphin) and the δ(ncx2) site (low affinity for DPDPE and deltorphin). Some agents were moderately selective for the delta(ncx2) site: [pCl]DPDPE (10.9-fold), JP41 (5.9-fold) and JP45 (3.8-fold). The K(i) values of 12 opioids at the mouse MDOR were determined. These values were highly correlated with their values at the delta(ncx1) site but not the delta(ncx2) site. These data suggest that the delta(ncx2) site may be distinct from the cloned delta opioid receptor.",
keywords = "[D-Ala, D-Len]enkephalin, Delta receptors, Receptor subtypes",
author = "Heng Xu and Lu, {Yi Feng} and Partilla, {John S.} and Julia Pinto and Calderon, {Sylvia N.} and Dorota Matecka and Rice, {Kenner C.} and Josephine Lai and Frank Porreca and Subramaniam Ananthan and Rothman, {Richard B.}",
year = "1998",
month = "2",
doi = "10.1016/S0196-9781(97)00294-5",
language = "English (US)",
volume = "19",
pages = "343--350",
journal = "Peptides",
issn = "0196-9781",
publisher = "Elsevier Inc.",
number = "2",

}

TY - JOUR

T1 - Opioid peptide receptor studies. 8. One of the mouse brain δ(NCX) binding sites is similar to the cloned mouse opioid δ receptor

T2 - Further evidence for heterogeneity of δ opioid receptors

AU - Xu, Heng

AU - Lu, Yi Feng

AU - Partilla, John S.

AU - Pinto, Julia

AU - Calderon, Sylvia N.

AU - Matecka, Dorota

AU - Rice, Kenner C.

AU - Lai, Josephine

AU - Porreca, Frank

AU - Ananthan, Subramaniam

AU - Rothman, Richard B.

PY - 1998/2

Y1 - 1998/2

N2 - Quantitative ligand binding studies resolved two subtypes of the δ opioid receptor, termed δ(ncx1), and δ(ncx2), in mouse brain membranes depleted of μ receptors by pretreatment with the irreversible ligand, BIT. The purpose of the present study was to compare the binding parameters, ligand-selectivity profile and pharmacological properties of the cloned mouse δ receptor (MDOR) stably expressed in a cell line to the δ(ncx) binding sites of mouse brain. [3H][D-Ala2,D-Leu5]enkephalin labeled a single binding site in membranes prepared from MDOR cells under several different assay conditions including BIT-pretreatment. The MDOR had high affinity for δ agonists and antagonists. [3H][D-Ala2,D-Leu5]enkephalin labeled two binding sites in mouse brain membranes depleted of p. receptors by pretreatment with BIT: the δ(ncx1) site (high affinity for DPDPE and deltorphin) and the δ(ncx2) site (low affinity for DPDPE and deltorphin). Some agents were moderately selective for the delta(ncx2) site: [pCl]DPDPE (10.9-fold), JP41 (5.9-fold) and JP45 (3.8-fold). The K(i) values of 12 opioids at the mouse MDOR were determined. These values were highly correlated with their values at the delta(ncx1) site but not the delta(ncx2) site. These data suggest that the delta(ncx2) site may be distinct from the cloned delta opioid receptor.

AB - Quantitative ligand binding studies resolved two subtypes of the δ opioid receptor, termed δ(ncx1), and δ(ncx2), in mouse brain membranes depleted of μ receptors by pretreatment with the irreversible ligand, BIT. The purpose of the present study was to compare the binding parameters, ligand-selectivity profile and pharmacological properties of the cloned mouse δ receptor (MDOR) stably expressed in a cell line to the δ(ncx) binding sites of mouse brain. [3H][D-Ala2,D-Leu5]enkephalin labeled a single binding site in membranes prepared from MDOR cells under several different assay conditions including BIT-pretreatment. The MDOR had high affinity for δ agonists and antagonists. [3H][D-Ala2,D-Leu5]enkephalin labeled two binding sites in mouse brain membranes depleted of p. receptors by pretreatment with BIT: the δ(ncx1) site (high affinity for DPDPE and deltorphin) and the δ(ncx2) site (low affinity for DPDPE and deltorphin). Some agents were moderately selective for the delta(ncx2) site: [pCl]DPDPE (10.9-fold), JP41 (5.9-fold) and JP45 (3.8-fold). The K(i) values of 12 opioids at the mouse MDOR were determined. These values were highly correlated with their values at the delta(ncx1) site but not the delta(ncx2) site. These data suggest that the delta(ncx2) site may be distinct from the cloned delta opioid receptor.

KW - [D-Ala, D-Len]enkephalin

KW - Delta receptors

KW - Receptor subtypes

UR - http://www.scopus.com/inward/record.url?scp=18544404835&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=18544404835&partnerID=8YFLogxK

U2 - 10.1016/S0196-9781(97)00294-5

DO - 10.1016/S0196-9781(97)00294-5

M3 - Article

C2 - 9493867

AN - SCOPUS:18544404835

VL - 19

SP - 343

EP - 350

JO - Peptides

JF - Peptides

SN - 0196-9781

IS - 2

ER -