Evaluation of Pharmacokinetics and Pharmacodynamics of BI 425809, a Novel GlyT1 Inhibitor: Translational Studies

Autor:	Michael Desch, Bernhard Schmid, Riccardo Giovannini, Viktoria Moschetti, Glen Wunderlich, Christina Schlecker, Karl-Heinz Liesenfeld, Sascha Keller, Sophia Goetz, Cornelia Dorner-Ciossek, Sven Wind, Oliver Kleiner, Steven Ramael, Gwenaëlle Fillon, Holger Rosenbrock
Rok vydání:	2018
Předmět:	Adult Male Primary Cell Culture Glycine Cmax Administration Oral Pharmacology Article General Biochemistry Genetics and Molecular Biology Cell Line Young Adult 03 medical and health sciences 0302 clinical medicine Cerebrospinal fluid Pharmacokinetics Alzheimer Disease Glycine Plasma Membrane Transport Proteins Oral administration Animals Humans Organic Chemicals Rats Wistar General Pharmacology Toxicology and Pharmaceutics Nootropic Agents Neurons Dose-Response Relationship Drug biology Chemistry Research General Neuroscience Articles General Medicine Middle Aged Healthy Volunteers Rats 030227 psychiatry Dose–response relationship Area Under Curve Glycine transporter 1 Schizophrenia biology.protein Steady state (chemistry) 030217 neurology & neurosurgery
Zdroj:	Clinical and Translational Science
ISSN:	1752-8054
DOI:	10.1111/cts.12578
Popis:	BI 425809 is a potent and selective glycine transporter 1 (GlyT1) inhibitor being developed for the treatment of cognitive impairment in Alzheimer disease and schizophrenia. Translational studies evaluated the effects of BI 425809 on glycine levels in rat and human cerebrospinal fluid (CSF). Oral administration of BI 425809 in rats induced a dose‐dependent increase of glycine CSF levels from 30% (0.2 mg/kg, not significant) to 78% (2 mg/kg, P
Databáze:	OpenAIRE
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