METHADONE INHIBITION OF 3H-5-HYDROXYTRYPTAMINE UPTAKE BY SYNAPTOSOMES

摘要: Synaptosomes were prepared from whole rabbit brain by differential centrifugation and sucrose-Ficoll gradients. Methadone dramatically inhibited 5-hydroxytryptamine uptake synaptosomes. The apparent K 4 for this effect in the present system is 10-9 M. Morphine also (5-HT) synaptosomes but only at relatively high concentrations. morphine 3.9 x 10-4 Naloxone, concentrations above 10-6 M, decreased 5-HT 10-5 partially blocked of methadone not on uptake. Neither nor altered KCl-stimulated release preloaded results suggest that narcotic inhibition nerve terminals involved analgesic mechanisms due to reaction with specific "opiate receptor." However, marked effects may possibly be related compound's actions longlasting vivo.