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Picenadol, a mixed opioid agonist/antagonist without κ opioid agonist activity in the rat urination test
Author(s) -
Leander J. David,
Zimmerman Dennis M.
Publication year - 1983
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430030511
Subject(s) - nalbuphine , butorphanol , agonist , chemistry , antagonist , opioid , diuresis , pharmacology , endocrinology , medicine , receptor , biochemistry , renal function
Picenadol and its (+) and (−) isomers were compared to butorphanol and nalbuphine for their effects on urinary output in the normally hydrated rat. Butorphanol, a partial K agonist, increased urinary output markedly at all doses (0.32–20 mg/kg, s.c.). Nalbuphine (0.32–20 mg/kg, s.c.), picenadol (1.25–40 mg/kg, s.c.) and the two isomers (0.32–20 mg/kg, s.c.) had no tendency to increase urinary output within the 5‐hr test period. Nalbuphine did not affect bremazocine‐induced diuresis, whereas the (−) isomer of picenadol decreased bremazocine‐induced diuresis through a κ‐antagonist action and the (+) isomer of picenadol decreased the bremazocine‐induced diuresis through a μ‐opioid‐like agonist action. These results were interpreted to mean that nalbuphine is a mixed agonist/antagonist without activity at κ receptors. Picenadol is a mixed agonist/antagonist with potent μ‐opioid action in the (+) isomer and weak μ‐and κ‐antagonist action in the (−) isomer.