Renuka Sriram1, Robert J. Mather2, Serguei Liachenko1
1BioImaging CoE, Pfizer Inc, Groton, CT, United States; 2Neuroscience, Pfizer Inc, Groton, CT, United States
Neurotransmitter levels of glutamate and glutamine are tightly coupled with modulation of one resulting in a corresponding opposing change in the other. Since glutamate is implicated in a variety of neurological disorders, the observation of an endogenous pool of glutamate (Glu) and glutamine (Gln) and/or its ratio can serve as a strong mechanistic biomarker and measure of efficacy. Flupirtine, a potassium channel opener, has been shown to cause decrease in Glu and a relative increase in Gln in the rat hippocampus.