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Physical dependence liability of TR5379, a novel narcotic antagonist analgesic
Author(s) -
Howes John F.,
Bousquet Ann R.
Publication year - 1982
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.430020408
Subject(s) - butorphanol , physical dependence , antagonist , analgesic , morphine , pharmacology , narcotic antagonists , potency , narcotic , anesthesia , medicine , chemistry , receptor , (+) naloxone , in vitro , biochemistry
Abstract TR5379 is a novel morphinan with potent antinociceptive activity in the mouse abdominal constriction procedure. It is a narcotic antagonist with a potency similar to that of butorphanol. In rats and monkeys, TR5379 does not appear to induce any physical dependence. Following a 6‐day chronic administration of TR5379 to rats, no indications of withdrawal were observed. TR5379 did not substitute for morphine in either the physically dependent rat or the physically dependent monkey. In the chronically morphinized rat, an acute dose of TR5379 caused the rapid onset of a marked withdrawal syndrome.