The mu1, mu2, delta, kappa opioid receptor binding profiles of methadone stereoisomers and morphine

K Kristensen; C B Christensen; Lona Louring Christrup

The mu1, mu2, delta, kappa opioid receptor binding profiles of methadone stereoisomers and morphine

K Kristensen, C B Christensen, Lona Louring Christrup

206 Citationer (Scopus)

Abstract

The binding affinities of racemic methadone and its optical isomers R-methadone and S-methadone were evaluated for the opioid receptors mu1, mu2, delta and kappa, in comparison with that of morphine. The analgesic R-methadone had a 10-fold higher affinity for mu1 receptors than S-methadone (IC50 3.0 nM and 26.4 nM, respectively). At the mu2 receptor, the IC50 value of R-methadone was 6.9 nM and 88 nM for S-methadone, respectively. As expected, R-methadone had twice the affinity for mu1 and mu2 receptors than the racemate. All of the compounds tested had low affinity for the delta and kappa receptors. This result suggests that S-methadone does not essentially contribute to opioid effect of racemic methadone. R-methadone has a receptor binding profile which resembles that of morphine.

Originalsprog	Engelsk
Tidsskrift	Life Sciences
Vol/bind	56
Udgave nummer	2
Sider (fra-til)	PL45-50
ISSN	0024-3205
Status	Udgivet - 1995

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http://www.sciencedirect.com/science/article/pii/0024320594009376

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title = "The mu1, mu2, delta, kappa opioid receptor binding profiles of methadone stereoisomers and morphine",

abstract = "The binding affinities of racemic methadone and its optical isomers R-methadone and S-methadone were evaluated for the opioid receptors mu1, mu2, delta and kappa, in comparison with that of morphine. The analgesic R-methadone had a 10-fold higher affinity for mu1 receptors than S-methadone (IC50 3.0 nM and 26.4 nM, respectively). At the mu2 receptor, the IC50 value of R-methadone was 6.9 nM and 88 nM for S-methadone, respectively. As expected, R-methadone had twice the affinity for mu1 and mu2 receptors than the racemate. All of the compounds tested had low affinity for the delta and kappa receptors. This result suggests that S-methadone does not essentially contribute to opioid effect of racemic methadone. R-methadone has a receptor binding profile which resembles that of morphine.",

keywords = "Animals, Binding, Competitive, Cattle, Methadone, Morphine, Protein Binding, Receptors, Opioid, Receptors, Opioid, delta, Receptors, Opioid, kappa, Receptors, Opioid, mu, Reproducibility of Results, Stereoisomerism",

author = "K Kristensen and Christensen, {C B} and Christrup, {Lona Louring}",

year = "1995",

language = "English",

volume = "56",

pages = "PL45--50",

journal = "Life Sciences",

issn = "0024-3205",

publisher = "Elsevier",

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TY - JOUR

T1 - The mu1, mu2, delta, kappa opioid receptor binding profiles of methadone stereoisomers and morphine

AU - Kristensen, K

AU - Christensen, C B

AU - Christrup, Lona Louring

PY - 1995

Y1 - 1995

N2 - The binding affinities of racemic methadone and its optical isomers R-methadone and S-methadone were evaluated for the opioid receptors mu1, mu2, delta and kappa, in comparison with that of morphine. The analgesic R-methadone had a 10-fold higher affinity for mu1 receptors than S-methadone (IC50 3.0 nM and 26.4 nM, respectively). At the mu2 receptor, the IC50 value of R-methadone was 6.9 nM and 88 nM for S-methadone, respectively. As expected, R-methadone had twice the affinity for mu1 and mu2 receptors than the racemate. All of the compounds tested had low affinity for the delta and kappa receptors. This result suggests that S-methadone does not essentially contribute to opioid effect of racemic methadone. R-methadone has a receptor binding profile which resembles that of morphine.

AB - The binding affinities of racemic methadone and its optical isomers R-methadone and S-methadone were evaluated for the opioid receptors mu1, mu2, delta and kappa, in comparison with that of morphine. The analgesic R-methadone had a 10-fold higher affinity for mu1 receptors than S-methadone (IC50 3.0 nM and 26.4 nM, respectively). At the mu2 receptor, the IC50 value of R-methadone was 6.9 nM and 88 nM for S-methadone, respectively. As expected, R-methadone had twice the affinity for mu1 and mu2 receptors than the racemate. All of the compounds tested had low affinity for the delta and kappa receptors. This result suggests that S-methadone does not essentially contribute to opioid effect of racemic methadone. R-methadone has a receptor binding profile which resembles that of morphine.

KW - Animals

KW - Binding, Competitive

KW - Cattle

KW - Methadone

KW - Morphine

KW - Protein Binding

KW - Receptors, Opioid

KW - Receptors, Opioid, delta

KW - Receptors, Opioid, kappa

KW - Receptors, Opioid, mu

KW - Reproducibility of Results

KW - Stereoisomerism

M3 - Journal article

C2 - 7823756

SN - 0024-3205

VL - 56

SP - PL45-50

JO - Life Sciences

JF - Life Sciences

IS - 2

ER -

The mu1, mu2, delta, kappa opioid receptor binding profiles of methadone stereoisomers and morphine

Abstract

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