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…
75 Citations
d-Methadone blocks morphine tolerance and N-methyl-D-aspartate-induced hyperalgesia.
- Biology, PsychologyThe Journal of pharmacology and experimental therapeutics
- 1999
The results support the conclusion that d-methadone affects the development of morphine tolerance and NMDA-induced hyperalgesia by virtue of its NMDA receptor antagonist activity.
Characterization of the antinociceptive effects of the individual isomers of methadone after acute and chronic administrations
- Biology, MedicineBehavioural pharmacology
- 2011
Findings support the antinociceptive effects of the isomers being opioid receptor mediated with the L-isomer functioning as a full-efficacy agonist, whereas the D-isomers seems to have lower efficacy.
The N-methyl-d-aspartate antagonistic and opioid components of d-methadone antinociception in the rat spinal cord
- BiologyNeuroscience Letters
- 2000
Pharmacology of methadone and its isomers.
- Biology, ChemistryMinerva anestesiologica
- 2005
D-metha-done affects the development of morphine tolerance and NMDA-induced hyperalgesia by virtue of its NMDA receptor antagonist activity, and results support the conclusion that this drug is used as an alternate to morphine and hydromorphone for patients with severe pain.
Characterization of the Antinociceptive and Pronociceptive Effects of Methadone in Rats
- Psychology, BiologyAnesthesiology
- 2007
The current findings with methadone are supportive of previous findings implicating &mgr;-opioid and N-methyl-d-aspartate receptor mechanisms in OIH and may help in choosing the most appropriate opioids for use in the treatment of pain.
Morphine, Oxycodone, Methadone and Its Enantiomers in Different Models of Nociception in the Rat
- Biology, PsychologyAnesthesia and analgesia
- 2006
In nerve injury pain, l-methadone showed the greatest antiallodynic potency in both mechanical and cold allodynia compared with the other opioids, with morphine showing the weakest effect.
Differential antinociception by morphine and methadone in two sub-strains of Sprague–Dawley rats and its potentiation by dextromethorphan
- Biology, PsychologyBrain Research
- 2002
Characterization of methadone as a β-arrestin-biased μ-opioid receptor agonist
- Biology, PsychologyMolecular pain
- 2016
The results suggest that methadone may, at least partly, produce its pharmacological effect as a β-arrestin-biased µ-opioid receptor agonist, similar to fentanyl, and NMDA receptor blockade is not the main contributor to the pharmacological profile of methamphetamine.
Heroin discriminative stimulus effects of methadone, LAAM and other isomers of acetylmethadol in rats
- PsychologyPsychopharmacology
- 2002
Examination of the discriminative stimulus effects of LAAM, the other isomers of acetylmethadol, and methadone in rats trained to discriminate heroin from water found that LAAM elicited heroin-like discriminatives for at least 6 h and generated partial generalization up to 36 h following administration.
References
SHOWING 1-10 OF 35 REFERENCES
The d- and l- isomers of methadone bind to the non-competitive site on the N-methyl-d-aspartate (NMDA) receptor in rat forebrain and spinal cord
- Biology, ChemistryNeuroscience Letters
- 1997
Comparison of the antinociceptive effects of pre- and posttreatment with intrathecal morphine and MK801, an NMDA antagonist, on the formalin test in the rat.
- Biology, PsychologyAnesthesiology
- 1992
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.
- Biology, ChemistryEuropean journal of pharmacology
- 1992
Attenuation and reversal of morphine tolerance by the competitive N-methyl-D-aspartate receptor antagonist, LY274614.
- BiologyThe Journal of pharmacology and experimental therapeutics
- 1993
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.
- BiologyThe Journal of pharmacology and experimental therapeutics
- 1981
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.
Ketobemidone, methadone and pethidine are non-competitive N-methyl-d-aspartate (NMDA) antagonists in the rat cortex and spinal cord
- Biology, ChemistryNeuroscience Letters
- 1995
Dextromethorphan attenuates and reverses analgesic tolerance to morphine
- Biology, MedicinePain
- 1994
The binding of the optical isomers of methadone, alpha-methadol, alpha-acetylmethadol and their N-demethylated derivatives to the opiate receptors of rat brain.
- Chemistry, BiologyResearch communications in chemical pathology and pharmacology
- 1976
The affinities of the methadone isomers and related compounds on the binding of 3H-NLX fall in the presence of Na+.
Evidence for spinalN-methyl-d-aspartate receptor involvement in prolonged chemical nociception in the rat
- BiologyBrain Research
- 1990
Oral administration of dextromethorphan prevents the development of morphine tolerance and dependence in rats
- Biology, PsychologyPain
- 1996