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

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

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@article{64d783bf56f74625ad857f58761df2da,

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",

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

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

M3 - Article

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AN - SCOPUS:0026468732

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

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