Research reportInhibition of opiate tolerance by non-competitive N-d-aspartate receptor antagonists
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2020, BurnsCitation Excerpt :However, it may be better tolerated in some patients, and is therefore utilized as an alternative to morphine. Methadone has numerous advantages including long duration of action, low abuse potential, and antagonist activity at the N-methyl-d-aspartate (NMDA) receptor, a mechanism which has been demonstrated to block the development of opioid analgesic tolerance [11,12] as well as producing direct analgesia [13]. For these reasons, NMDA receptor antagonism has been utilized for pain relief both on its own [14] as well as in combination with opioids [15].
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2020, Drug and Alcohol DependenceCitation Excerpt :NMDAR plays a significant role in the process that implicates both the acute and chronic exposure to opioids to induce a variety of neurobiological changes such as sensitization and tolerance as adaptive mechanisms of the addicted brain. Several biological mechanisms may explain this process (Trujillo and Akil, 1991, 1994; Trujillo, 2000, 2002). Bishop et al. (2010) demonstrated that intra- prelimbic cortex (PLC) NMDAR transmission could play a "critical modulatory role" during the encoding of "associative opioid reward learning."
Ketamine and norketamine attenuate oxycodone tolerance markedly less than that of morphine: from behaviour to drug availability
2018, British Journal of Anaesthesia
Preliminary reports of this work have been presented [45–47].