THE SYSTEMIC EXPOSURE OF ANN-METHYL-d-ASPARTATE RECEPTOR ANTAGONIST IS LIMITED IN MICE BY THE P-GLYCOPROTEIN AND BREAST CANCER RESISTANCE PROTEIN EFFLUX TRANSPORTERS

Autor:	Robert J. Barnaby, Cosette J. Serabjit-Singh, Luigina Bertolotti, Joseph W. Polli, Todd M. Baughman, Joan E. Humphreys, Angela L. Mote, Giovanni Vitulli, Kevin D. Read, Lindsey O. Webster, Kelly H. Jordan
Rok vydání:	2004
Předmět:	Male medicine.medical_specialty Indoles Time Factors Membrane permeability Abcg2 medicine.drug_class Cmax Pharmaceutical Science Receptors N-Methyl-D-Aspartate Mass Spectrometry Cell Line Mice Tetrahydroisoquinolines Internal medicine medicine ATP Binding Cassette Transporter Subfamily G Member 2 Animals Pyrroles ATP Binding Cassette Transporter Subfamily B Member 1 Furans Receptor P-glycoprotein Mice Knockout Pharmacology Sulfonamides biology Antagonist Receptor antagonist Endocrinology biology.protein Acridines ATP-Binding Cassette Transporters Carbamates Efflux Chromatography Liquid
Zdroj:	Drug Metabolism and Disposition. 32:722-726
ISSN:	1521-009X 0090-9556
DOI:	10.1124/dmd.32.7.722
Popis:	This article is available online at http://dmd.aspetjournals.org ABSTRACT: GV196771 (E-4,6-dichloro-3-(2-oxo-1-phenyl-pyrrolidin-3-glyden- emethyl)-1H-indole-2 carboxylic acid) is a potent antagonist of the modulatory glycine site of the N-methyl-D-aspartate receptor. GV196771 has low oral bioavailability (
Databáze:	OpenAIRE
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