title: A functional model for feline P-glycoprotein.
abstract: P-gp (ABCB1) belongs to the group of export transporters that is expressed in various species at biological barriers. Inhibition of P-gp can lead to changes in pharmacokinetics of drugs (drug-drug interactions), which can lead to toxicity and adverse side effects. This study aimed to establish a functional assay to measure the inhibitory potential of veterinary drugs on feline P-gp by means of fluorescence-associated flow cytometry of feline lymphoma cells. In this model, PSC833 and ivermectin potently inhibited P-gp function; cyclosporine and verapamil moderately inhibited P-gp function, whereas ketoconazole, itraconazole, diazepam, and its metabolites had no effect on P-gp function. This model can be used for testing the inhibitory potency of (new) drugs on feline P-gp.
authors.affiliation: Faculty of Veterinary Medicine, Institute for Risk Assessment Sciences, Veterinary Pharmacology, Pharmacotherapy and Toxicology, Utrecht, The Netherlands.
authors.forename: C D
authors.initials: CD
authors.lastname: van Beusekom
authors.affiliation: Faculty of Veterinary Medicine, Institute for Risk Assessment Sciences, Veterinary Pharmacology, Pharmacotherapy and Toxicology, Utrecht, The Netherlands.
authors.forename: R
authors.initials: R
authors.lastname: Lange
authors.affiliation: Faculty of Veterinary Medicine, Institute for Risk Assessment Sciences, Veterinary Pharmacology, Pharmacotherapy and Toxicology, Utrecht, The Netherlands.
authors.forename: J A
authors.initials: JA
authors.lastname: Schrickx
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism*; D000818:Animals; D002371:Cat Diseases / Q000378:metabolism*; D002415:Cats; D045744:Cell Line, Tumor; D005786:Gene Expression Regulation / Q000187:drug effects*; D008223:Lymphoma / Q000378:metabolism / Q000662:veterinary*; D013953:Thymus Neoplasms / Q000378:metabolism / Q000662:veterinary*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1