The mu1, mu2, delta, kappa opioid receptor binding profiles of methadone stereoisomers and morphine
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The mu1, mu2, delta, kappa opioid receptor binding profiles of methadone stereoisomers and morphine. / Kristensen, K; Christensen, C B; Christrup, Lona Louring.
In: Life Sciences, Vol. 56, No. 2, 1995, p. PL45-50.Research output: Contribution to journal › Journal article › Research › peer-review
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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
VL - 56
SP - PL45-50
JO - Life Sciences
JF - Life Sciences
SN - 0024-3205
IS - 2
ER -
ID: 46099584