Differential sensitivity of antinociceptive tests to opioid agonists and partial agonists.
1. The antinociceptive activity of a range of opioid agonists and agonist-antagonist analgesics was determined in mice by use of the 55 degrees C hot plate and abdominal constriction assays. 2. Opioid agonists were approximately 10 times more effective in the abdominal constriction assay. 3. The agonist-antagonists produced analgesia only in the abdominal constriction assay, and antagonized the antinociceptive action of opioid agonists in the 55 degrees C hot plate test. 4. These differences were shown to be attributable to the different levels of stimulus employed in the two tests. 5. By comparing the antagonist potencies of the agonist-antagonists in the 55 degrees C hot plate test with their antinociceptive ED50 values in the abdominal constriction assay, an index of intrinsic activity was calculated.
Shaw
J S
JS
Bioscience Department, ICI Pharmaceuticals Division, Macclesfield, Cheshire.
Rourke
J D
JD
Burns
K M
KM
D000005:Abdomen / Q000187:drug effects; D000700:Analgesics; D000818:Animals; D005260:Female; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009292:Narcotic Antagonists / Q000494:pharmacology; D009294:Narcotics / Q000494:pharmacology*; D011930:Reaction Time / Q000187:drug effects; D011957:Receptors, Opioid / Q000502:physiology; D017450:Receptors, Opioid, mu
D000700:Analgesics; D009292:Narcotic Antagonists; D009294:Narcotics; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu