Quantification of the morphine reversal activity of opioid agonists/antagonists and naloxone by using a rabbit tooth pulp procedure
✍ Scribed by Dr Richard L. Wynn; Stewart A. Bergman
- Book ID
- 102817514
- Publisher
- John Wiley and Sons
- Year
- 1987
- Tongue
- English
- Weight
- 607 KB
- Volume
- 11
- Category
- Article
- ISSN
- 0272-4391
No coin nor oath required. For personal study only.
✦ Synopsis
The rabbit tooth pulp procedure was used to determine the potencies and durations of morphine reversal by naloxone, buprenorphine, nalbuphine, butorphanol, and pentazocine. Cumulative doses (mg/kg) required to double the number of morphine-depressed respirations per minute (RPM) (ED 2 x ) and to reduce morphine-elevated licklchew (UC) volts by one-half (ED 1/2) were determined. These doses were naloxone 0.003, 0.013; buprenorphine 0.030, 0.130; nalbuphine 0.130, 0.520; butorphanol 0.120, 0.630; pentazocine 1 .lo, 0.150. The antinociceptive effects of these compounds were compared by determining the cumulative dose required to achieve the highest percentage maximum possible effect (Yo MPE) as determined by the elevation of licklchew threshold volts from control volts in morphine-free rabbits: naloxone 6% at 0.0005 mglkg; buprenorphine 69% at 0.075 mglkg; nalbuphine 32% at 0.150 mglkg; butorphanol 32% at 0.150 mglkg, and pentazocine 12% at 1.55 mglkg. The durations (min) of reversal of morphine RPM and morphine L/C volts were also determined: naloxone 33, 30; buprenorphine 240, 240; nalbuphine 120, 120; butorphanol90, 45; pentazocine 60, 15. It is suggested that the rabbit tooth pulp assay is a sensitive and reliable assay to evaluate and quantitate compounds for opioid agonist/antagonist activity.