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Updated: Apr 24, 2026

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Published on: March 12, 2019
Influence of agonist induced internalization on [3H]Ro15-4513 binding-an application to imaging fluctuations in
Darren Quelch1, Vittorio De Santis, Annette Strege
1Centre for Neuropsychopharmacology, Division of Brain Sciences, Imperial College, London, UK.
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.
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