Increased analgesic potency of morphine and increased brain opioid binding sites in the rat following chronic naltrexone treatment.
Implantation of rats with prolonged-release naltrexone pellets increased both morphine's analgesic potency in the tailflick assay and radiolabeled opioid binding in the brain. The increases in both radiolabeled opioid binding and morphine potency were time-dependent. Implantation for 24 hours did not increase binding, whereas increases of approximately 45% were seen following 8 days of implantation. Similarly, morphine's analgesic potency, measured as ED50 values, was increased by 50% following 8 days of exposure to naltrexone while a 24 hour exposure had no significant effect.
Yoburn
B C
BC
Goodman
R R
RR
Cohen
A H
AH
Pasternak
G W
GW
Inturrisi
C E
CE
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D004343:Drug Implants; D004347:Drug Interactions; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000378:metabolism; D016308:Enkephalin, Leucine-2-Alanine; D008297:Male; D009020:Morphine / Q000378:metabolism / Q000494:pharmacology*; D009270:Naloxone / Q000031:analogs & derivatives*; D009271:Naltrexone / Q000494:pharmacology*; D010146:Pain / Q000503:physiopathology*; D051381:Rats; D011919:Rats, Inbred Strains; D011930:Reaction Time / Q000187:drug effects; D011957:Receptors, Opioid / Q000187:drug effects* / Q000378:metabolism; D013997:Time Factors
D004343:Drug Implants; D011957:Receptors, Opioid; D009270:Naloxone; D004743:Enkephalin, Leucine; D009271:Naltrexone; D016308:Enkephalin, Leucine-2-Alanine; D009020:Morphine