d -Methadone Blocks Morphine Tolerance and N -Methyl-d-Aspartate-Induced Hyperalgesia
作者： Charles E. Inturrisi , Antonia M. Davis
DOI:
关键词: Morphine 、 NMDA receptor 、 Methadone 、 In vivo 、 Hyperalgesia 、 Receptor antagonist activity 、 Analgesic 、 Chemistry 、 Pharmacology 、 ED50
摘要: Previous in vitro and vivo studies have determined that the d isomer of methadone has N -methyl-d-aspartate (NMDA) receptor antagonist activity. The present examined ability -methadone to attenuate development morphine tolerance mice rats modify NMDA-induced hyperalgesia rats. A decrease percentage analgesic (tail-flick response) after 5 days once-daily (7 mg/kg s.c.) was completely blocked by coadministration d-methadone given s.c. at 10 mg/kg. Morphine on an escalating three times per day dosing schedule resulted a nearly 3-fold increase tail-flick ED50 dose which prevented coadministered 15 In rats, intrathecal (i.t.) produced 38-fold ED50, i.t. 160 μg/rat. thermal paw withdrawal latency induced administration 1.64 μg/rat NMDA pretreatment with -methadone. Thus, systemically prevents mice, attenuates -methadone, same modulates tolerance, blocks hyperalgesia. These results support conclusion affects virtue its
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