Correlation of analgesia with levels of tilidine and a biologically active metabolite in rat plasma and brain
| Autor: | Myriam D. Melgar, J.Krystyna Karpowicz, Frederick J. Di Carlo, Barry Dubinsky, Malcolm C. Crew |
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| Rok vydání: | 1975 |
| Předmět: |
Male
Chromatography Gas Hot Temperature Time Factors Cyclohexanecarboxylic Acids Metabolite Analgesic Administration Oral Pharmacology Biochemistry chemistry.chemical_compound Oral administration Reflex medicine Animals Brain Chemistry Analgesics Analysis of Variance Chemistry Biological activity Rats Analgesia Tilidine Dimethylamines medicine.drug |
| Zdroj: | Biochemical pharmacology. 24(2) |
| ISSN: | 0006-2952 |
| Popis: | The analgesic ED 50 of tilidine administered orally to rats was 15.4 mg/kg at 15 min and 17.2 mg/kg at 30 min. The drug was metabolized quickly and extensively, and it and its principal metabolite readily crossed the blood-brain barrier. Analgesia after the oral administration of tilidine fumarate to rats was correlated with levels of this metabolite in plasma and brain, and with the tilidine levels in plasma. It appears probable that the conversion of tilidine into its metabolite. which has analgesic properties, is closely related to the analgesic state. |
| Databáze: | OpenAIRE |
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