Abstract:
:Using the hot plate test, the potency and mechanism of the analgesic activity of levonantradol was studied in mice. Levonantradol is 10 to 30 times more potent than morphine; the antinociception can be only partially blocked by naloxone. Similar limited antagonism by cholinergics indicates possible opiodergic mechanism. The role of serotoninergic pathways is unclear; antinociception is partially blocked by 5,7-dihydroxytryptamine, unaffected by p-chlorophenylalanine, and potentiated by cyproheptadine. Levonantradol blocks naloxone-induced signs of abstinence in morphine-dependent mice, being 3000 times more potent than morphine and 300 times more potent than delta 9-tetrahydrocannabinol (THC).
journal_name
J Clin Pharmacoljournal_title
Journal of clinical pharmacologyauthors
Jacob JJ,Ramabadran K,Campos-Medeiros Mdoi
10.1002/j.1552-4604.1981.tb02611.xsubject
Has Abstractpub_date
1981-08-01 00:00:00pages
327S-333Sissue
S1eissn
0091-2700issn
1552-4604journal_volume
21pub_type
杂志文章abstract::The purpose of this analysis was to develop a population pharmacokinetic model for CS-917, an oral hypoglycemic prodrug, and its 3 metabolites. The population pharmacokinetic model was used to predict exposure of the active moiety R-125338 and thus to identify potential CS-917 dosage reduction criteria. The dataset in...
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