Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain

Mark S. Yamamura; Robert Horvath; Geza Toth; Ferenc Otvos; Ewa Malatynska; Richard J. Knapp; Frank Porreca; Victor J. Hruby; Henry I. Yamamura

doi:10.1016/0024-3205(92)90464-Z

Characterization of [³H]naltrindole binding to delta opioid receptors in rat brain

Mark S. Yamamura
, Robert Horvath
, Geza Toth
, Ferenc Otvos
, Ewa Malatynska
, Richard J. Knapp
, Frank Porreca
, Victor J. Hruby
, Henry I. Yamamura

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

56 Scopus citations

Abstract

[³H]Naltrindole binding characteristics were determined using homogenized rat brain tissue. Saturation binding studies at 25°C measured an equilibrium dissociation constant (K_d) value of 37.0 ± 3.0 pM and a receptor density (B_max) value of 63.4 ± 2.0 fmol/mg protein. Association binding studies showed that equilibrium was reached within 90 min at a radioligand concentration of 30 pM. Naltrindole, as well as the ligands selective for delta (δ) opioid receptors, such as pCI-DPDPE and Deltorphin II inhibited [³H]naltrindole binding with nanomolar IC₅₀ values. Ligands selective for mu (μ) and kappa (κ) opioid receptors were only effective inhibiting [³H]naltrindole binding at micromolar concentrations. From these data, we conclude that [³H]naltrindole is a high affinity, selective radioligand for delta opioid receptors.

Original language	English (US)
Pages (from-to)	PL119-PL124
Journal	Life Sciences
Volume	50
Issue number	16
DOIs	https://doi.org/10.1016/0024-3205(92)90464-Z
State	Published - 1992

ASJC Scopus subject areas

General Biochemistry, Genetics and Molecular Biology
General Pharmacology, Toxicology and Pharmaceutics

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10.1016/0024-3205(92)90464-Z

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@article{d8a761a4cfbe431480e06f81646cec51,

title = "Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain",

abstract = "[3H]Naltrindole binding characteristics were determined using homogenized rat brain tissue. Saturation binding studies at 25°C measured an equilibrium dissociation constant (Kd) value of 37.0 ± 3.0 pM and a receptor density (Bmax) value of 63.4 ± 2.0 fmol/mg protein. Association binding studies showed that equilibrium was reached within 90 min at a radioligand concentration of 30 pM. Naltrindole, as well as the ligands selective for delta (δ) opioid receptors, such as pCI-DPDPE and Deltorphin II inhibited [3H]naltrindole binding with nanomolar IC50 values. Ligands selective for mu (μ) and kappa (κ) opioid receptors were only effective inhibiting [3H]naltrindole binding at micromolar concentrations. From these data, we conclude that [3H]naltrindole is a high affinity, selective radioligand for delta opioid receptors.",

author = "Yamamura, \{Mark S.\} and Robert Horvath and Geza Toth and Ferenc Otvos and Ewa Malatynska and Knapp, \{Richard J.\} and Frank Porreca and Hruby, \{Victor J.\} and Yamamura, \{Henry I.\}",

note = "Funding Information: Portions of this research was supported by U.S. Public Health Service grants DA 06284, NS 19972, T35HI07479 Short-Term Training: Students in Health Professional Schools and by the Hungarian National Committee for Technological Development, No. 3540/91.",

year = "1992",

doi = "10.1016/0024-3205(92)90464-Z",

language = "English (US)",

volume = "50",

pages = "PL119--PL124",

journal = "Life Sciences",

issn = "0024-3205",

publisher = "Elsevier Inc.",

number = "16",

}

TY - JOUR

T1 - Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain

AU - Yamamura, Mark S.

AU - Horvath, Robert

AU - Toth, Geza

AU - Otvos, Ferenc

AU - Malatynska, Ewa

AU - Knapp, Richard J.

AU - Porreca, Frank

AU - Hruby, Victor J.

AU - Yamamura, Henry I.

N1 - Funding Information: Portions of this research was supported by U.S. Public Health Service grants DA 06284, NS 19972, T35HI07479 Short-Term Training: Students in Health Professional Schools and by the Hungarian National Committee for Technological Development, No. 3540/91.

PY - 1992

Y1 - 1992

N2 - [3H]Naltrindole binding characteristics were determined using homogenized rat brain tissue. Saturation binding studies at 25°C measured an equilibrium dissociation constant (Kd) value of 37.0 ± 3.0 pM and a receptor density (Bmax) value of 63.4 ± 2.0 fmol/mg protein. Association binding studies showed that equilibrium was reached within 90 min at a radioligand concentration of 30 pM. Naltrindole, as well as the ligands selective for delta (δ) opioid receptors, such as pCI-DPDPE and Deltorphin II inhibited [3H]naltrindole binding with nanomolar IC50 values. Ligands selective for mu (μ) and kappa (κ) opioid receptors were only effective inhibiting [3H]naltrindole binding at micromolar concentrations. From these data, we conclude that [3H]naltrindole is a high affinity, selective radioligand for delta opioid receptors.

AB - [3H]Naltrindole binding characteristics were determined using homogenized rat brain tissue. Saturation binding studies at 25°C measured an equilibrium dissociation constant (Kd) value of 37.0 ± 3.0 pM and a receptor density (Bmax) value of 63.4 ± 2.0 fmol/mg protein. Association binding studies showed that equilibrium was reached within 90 min at a radioligand concentration of 30 pM. Naltrindole, as well as the ligands selective for delta (δ) opioid receptors, such as pCI-DPDPE and Deltorphin II inhibited [3H]naltrindole binding with nanomolar IC50 values. Ligands selective for mu (μ) and kappa (κ) opioid receptors were only effective inhibiting [3H]naltrindole binding at micromolar concentrations. From these data, we conclude that [3H]naltrindole is a high affinity, selective radioligand for delta opioid receptors.

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UR - https://www.scopus.com/pages/publications/0026468732#tab=citedBy

U2 - 10.1016/0024-3205(92)90464-Z

DO - 10.1016/0024-3205(92)90464-Z

M3 - Article

C2 - 1313133

SN - 0024-3205

VL - 50

SP - PL119-PL124

JO - Life Sciences

JF - Life Sciences

IS - 16

ER -

Characterization of [³H]naltrindole binding to delta opioid receptors in rat brain

Abstract

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