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

Darren Quelch; Vittorio De Santis; Annette Strege; James Myers; Lisa Wells; David Nutt; Anne Lingford-Hughes; Christine A. Parker; Robin J. Tyacke

doi:10.1002/syn.21780

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

Darren Quelch, Vittorio De Santis, Annette Strege, James Myers, Lisa Wells, David Nutt, Anne Lingford-Hughes, Christine A. Parker, Robin J. Tyacke

Research output: Contribution to journal › Article › peer-review

Abstract

Low affinity α1/α2 containing GABAA receptors are significantly less able to bind [11C]/[3H]Ro15-4513 following translocation to the endosomal environment. The alterations in [11C]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.

Original language	English
Pages (from-to)	60-65
Number of pages	6
Journal	Synapse
Volume	69
Issue number	1
DOIs	https://doi.org/10.1002/syn.21780
Publication status	Published - 1 Jan 2015
Externally published	Yes

Keywords

GABAA
Internalization
Neurotransmitters
PET
[11C]Ro15-4513
agonist
environment
imaging
internalization (cell)
parameters
positron emission tomography
receptor binding
4 aminobutyric acid
8 azido 5,6 dihydro 5 methyl 6 oxo 4h imidazo[1,5 a][1,4]benzodiazepine 3 carboxylic acid ethyl ester
carbon 11
neurotransmitter
receptor

Access to Document

10.1002/syn.21780

Cite this

@article{f656cb667f4f46bbaba3bd46f1163c4a,

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

abstract = "Low affinity α1/α2 containing GABAA receptors are significantly less able to bind [11C]/[3H]Ro15-4513 following translocation to the endosomal environment. The alterations in [11C]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.",

keywords = "GABAA, Internalization, Neurotransmitters, PET, [11C]Ro15-4513, agonist, environment, imaging, internalization (cell), parameters, positron emission tomography, receptor binding, 4 aminobutyric acid, 8 azido 5,6 dihydro 5 methyl 6 oxo 4h imidazo[1,5 a][1,4]benzodiazepine 3 carboxylic acid ethyl ester, carbon 11, neurotransmitter, receptor",

author = "Darren Quelch and {De Santis}, Vittorio and Annette Strege and James Myers and Lisa Wells and David Nutt and Anne Lingford-Hughes and Parker, {Christine A.} and Tyacke, {Robin J.}",

year = "2015",

month = jan,

day = "1",

doi = "10.1002/syn.21780",

language = "English",

volume = "69",

pages = "60--65",

journal = "Synapse",

issn = "0887-4476",

publisher = "Wiley",

number = "1",

}

TY - JOUR

T1 - Influence of agonist induced internalization on [3H]Ro15-4513 binding-an application to imaging fluctuations in endogenous GABA with positron emission tomography

AU - Quelch, Darren

AU - De Santis, Vittorio

AU - Strege, Annette

AU - Myers, James

AU - Wells, Lisa

AU - Nutt, David

AU - Lingford-Hughes, Anne

AU - Parker, Christine A.

AU - Tyacke, Robin J.

PY - 2015/1/1

Y1 - 2015/1/1

N2 - Low affinity α1/α2 containing GABAA receptors are significantly less able to bind [11C]/[3H]Ro15-4513 following translocation to the endosomal environment. The alterations in [11C]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.

AB - Low affinity α1/α2 containing GABAA receptors are significantly less able to bind [11C]/[3H]Ro15-4513 following translocation to the endosomal environment. The alterations in [11C]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.

KW - GABAA

KW - Internalization

KW - Neurotransmitters

KW - PET

KW - [11C]Ro15-4513

KW - agonist

KW - environment

KW - imaging

KW - internalization (cell)

KW - parameters

KW - positron emission tomography

KW - receptor binding

KW - 4 aminobutyric acid

KW - 8 azido 5,6 dihydro 5 methyl 6 oxo 4h imidazo[1,5 a][1,4]benzodiazepine 3 carboxylic acid ethyl ester

KW - carbon 11

KW - neurotransmitter

KW - receptor

U2 - 10.1002/syn.21780

DO - 10.1002/syn.21780

M3 - Article

SN - 0887-4476

VL - 69

SP - 60

EP - 65

JO - Synapse

JF - Synapse

IS - 1

ER -

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

Abstract

Keywords

Access to Document

Fingerprint

Cite this