Antinociceptive effects of azepexole (BHT 933) in mice.
Subcutaneous (s.c.) administration of azepexole (BHT 933) at doses between 4 and 40 mg/kg produced dose-dependent antinociceptive effects in mice as assessed by tail-immersion, tail-pinch and acetic acid writhing tests. The ED16s were 5.6 +/- 0.4, 6.7 +/- 1.2 and 2.96 +/- 0.2 mg/kg respectively. Similarly, morphine produced analgesia in the same tests with ED16s of 0.87 +/- 0.03, 0.47 +/- 0.1 and 0.45 +/- 0.01 mg/kg respectively. In all instances naloxone (0.1 mg/kg s.c.) shifted the dose-response curves to morphine to the right in a parallel manner. Naloxone (0.1 and 1 mg/kg s.c.) partially antagonized the effect of azepexole in the tail-immersion and tail-pinch tests but significantly decreased the slope of the dose-response curve suggesting that a competitive interaction at the level of the opioid receptors did not occur. Naloxone had no effect on the antinociceptive action of azepexole in the acetic acid writhing test.
Vargas
M L
ML
Department of Pharmacology, Murcia University School of Medicine, MurciaSpain Department of Anesthesiology, NYU Medical Center, New York, NY 10016 U.S.A.
Bansinath
M
M
Turndorf
H
H
Puig
M M
MM
D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D001381:Azepines / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004338:Drug Combinations; D008297:Male; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D009270:Naloxone / Q000494:pharmacology; D009619:Nociceptors / Q000187:drug effects / Q000502:physiology*; D010147:Pain Measurement; D011930:Reaction Time / Q000187:drug effects
D000700:Analgesics; D001381:Azepines; D004338:Drug Combinations; D009270:Naloxone; D009020:Morphine; C015603:azepexole