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1. Influence of agonist induced internalization on [3H]Ro15-4513 binding-an application to imaging fluctuations in endogenous GABA with positron emission tomography.

Author

Quelch D, De Santis V, Strege A, Myers J, Wells L, Nutt D, Lingford-Hughes A, Parker C, and Tyacke R

Subjects
Animals, Binding, Competitive, Carbon Radioisotopes pharmacokinetics, Cell Membrane diagnostic imaging, Cell Membrane drug effects, Cell Membrane metabolism, Hippocampus drug effects, Hippocampus metabolism, Male, Positron-Emission Tomography, Rats, Sprague-Dawley, Receptors, GABA-A metabolism, Tiagabine, Tritium pharmacokinetics, Azides pharmacokinetics, Benzodiazepines pharmacokinetics, GABA-A Receptor Antagonists pharmacology, Hippocampus diagnostic imaging, Nipecotic Acids pharmacology, Radiopharmaceuticals pharmacokinetics, gamma-Aminobutyric Acid metabolism
Abstract

Low affinity α1/α2 containing GABAA receptors are significantly less able to bind [(11) C]/[(3) H]Ro15-4513 following translocation to the endosomal environment. The alterations in [(11) C]Ro15-4513 binding observed in vivo following perturbations in endogenous GABA are likely driven by both alterations in receptor binding parameters following agonist induced internalisation and the GABA Shift., (© 2014 Wiley Periodicals, Inc.)

Published
2015
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