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

Authors :: Quelch D
De Santis V
Strege A
Myers J
Wells L
Nutt D
Lingford-Hughes A
Parker C
Tyacke R
Source :: Synapse (New York, N.Y.) [Synapse] 2015 Jan; Vol. 69 (1), pp. 60-5. Date of Electronic Publication: 2014 Sep 19.
Publication Year :: 2015
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.<br /> (© 2014 Wiley Periodicals, Inc.)

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