Use of Freund's Complete Adjuvant (FCA) in inflammatory pain models: consequences on the metabolism and pharmacokinetics of the non-peptidic delta receptor agonist SNC80 in the rat
| Autor: | Etienne Lessard, J. Ducharme, M P Ducharme, D. Projean |
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| Rok vydání: | 2007 |
| Předmět: |
Agonist
Male medicine.drug_class Health Toxicology and Mutagenesis Freund's Adjuvant Biological Availability Pain Orosomucoid Pharmacology Toxicology Biochemistry Piperazines Rats Sprague-Dawley Pharmacokinetics Cytochrome P-450 Enzyme System In vivo Receptors Opioid delta medicine Animals Humans Glycoproteins Inflammation biology Chemistry Cytochrome P450 General Medicine Blood Proteins Blood proteins Recombinant Proteins Bioavailability Rats Solutions Disease Models Animal Benzamides biology.protein Microsome Microsomes Liver Protein Binding |
| Zdroj: | Xenobiotica; the fate of foreign compounds in biological systems. 37(8) |
| ISSN: | 0049-8254 |
| Popis: | This study was initiated to characterize the metabolism and pharmacokinetics of SNC80 in rats and to evaluate the impact of Freund's complete adjuvant (FCA)-induced inflammation on its body disposition. In vitro, the disappearance and intrinsic clearance (CL(int)) of SNC80 were measured following incubations in recombinant rat CYPs and in phenotyped liver microsomes from naive and 24-h FCA-treated rats. The unbound fraction (f(u)) was assessed by ultrafiltration. Based on the Clint values, in vivo blood clearance of 3.35 and 2.48 L/h/kg were predicted in naive and FCA-treated rats. In vivo, SNC80 was administered to naive and 24-h FCA-treated rats at 10 micromol/kg i.v. and 50 micromol/kg p.o. The naive animals showed high plasma clearance (3.1 L/h/kg), low renal clearance ( |
| Databáze: | OpenAIRE |
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