• Corpus ID: 9349173

d-Methadone is antinociceptive in the rat formalin test.

@article{Shimoyama1997dMethadoneIA,
  title={d-Methadone is antinociceptive in the rat formalin test.},
  author={N Shimoyama and M Shimoyama and Kathryn J. Elliott and Charles E Inturrisi},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1997},
  volume={283 2},
  pages={
          648-52
        }
}
The l-isomer of methadone possesses opioid activity, whereas the d-isomer is weak or inactive as an opioid. Both d- and l-methadone have been shown to bind to the N-methyl-D-aspartate (NMDA) receptor. To determine whether d-methadone has functional, in vivo NMDA receptor antagonist activity, the antinociceptive effects of d-methadone were evaluated in the rat tail-flick and formalin tests. Cumulative dose-response analysis in the tail-flick test revealed an ED50 value for intrathecal (spinal) l… 

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References

SHOWING 1-10 OF 35 REFERENCES
Comparison of the antinociceptive effects of pre- and posttreatment with intrathecal morphine and MK801, an NMDA antagonist, on the formalin test in the rat.
TLDR
The effects of pre- and post-treatment of intrathecal morphine and MK801 on the formalin test evaluated the behavioral parallels of this spinal facilitation and an almost complete suppression of formalin-evoked behavior was observed.
Antinociceptive actions of different classes of excitatory amino acid receptor antagonists in mice.
Attenuation and reversal of morphine tolerance by the competitive N-methyl-D-aspartate receptor antagonist, LY274614.
TLDR
The demonstration that LY274614 can prevent and reverse the development of morphine tolerance without reducing the analgesic response suggests that the adaptive system involved in the development and maintenance of tolerance requires a functional N-methyl-D-aspartate receptor.
Pharmacodynamics of subcutaneously administered diacetylmorphine, 6-acetylmorphine and morphine in mice.
TLDR
These pharmacodynamic studies, along with prior dispositional studies, suggest that the ability of DAM and AM to rapidly cross the blood-brain barrier determines their potency and time-action differences from M in centrally mediated bioassays.
Dextromethorphan attenuates and reverses analgesic tolerance to morphine
The binding of the optical isomers of methadone, alpha-methadol, alpha-acetylmethadol and their N-demethylated derivatives to the opiate receptors of rat brain.
TLDR
The affinities of the methadone isomers and related compounds on the binding of 3H-NLX fall in the presence of Na+.
...
1
2
3
4
...