Abstract：
:Oxymorphazone (at doses of 50-200 mg/kg) was found to be a relatively weak antinociceptive drug in intact frog (Rana esculenta) when acetic acid was used as pain stimulus. Frogs remained analgesic for at least 48 hrs following oxymorphazone (200 mg/kg) administration. The ligand increased the latency of wiping reflex in spinal frogs too. These effects were blocked by naloxone. In equilibrium binding studies (3H)oxymorphazone had high affinity to the opioid receptors of frog brain and spinal cord as well (apparent Kd values were 8.9 and 10.6 nM, respectively). Kinetic experiments show that only 25% of the bound (3H)oxymorphazone is readily dissociable. Preincubation of the membranes with labeled oxymorphazone results in a washing resistant inhibition of the opioid binding sites. At least 70% of the (3H)oxymorphazone specific binding is apparently irreversible after reaction at 5 nM ligand concentration, and this can be enhanced by a higher concentration of tritiated ligand.
journal_name
Life Scijournal_title
Life sciencesauthors
Benyhe S,Hoffmann G,Varga E,Hosztafi S,Toth G,Borsodi A,Wollemann Mdoi
10.1016/0024-3205(89)90302-0subject
Has Abstractpub_date
1989-01-01 00:00:00pages
1847-57issue
24eissn
0024-3205issn
1879-0631pii
0024-3205(89)90302-0journal_volume
44pub_type
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