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January 24, 2010 | History

Pre-clinical evaluation of [carbon-11]-(+)-PHNO as an agonist positron emission tomography (PET) radiotracer for imaging of the high-affinity state of the dopamine D2 receptor 1 edition

Pre-clinical evaluation of [carbon-11]-(+)-PHNO as an agonist positron ...
Patrick Neil McCormick

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Pre-clinical evaluation of [carbon-11]-(+)-PHNO as an agonist positron emission tomography (PET) radiotracer for imaging of the high-affinity state of the dopamine D2 receptor.

Published 2006 .
Written in English.

About the Book

In vivo imaging of the D2 receptor with agonist radiotracers could provide important information on the high-affinity, functional state of the D2 receptor in schizophrenia and Parkinson's disease. Here the D2 agonist [11C]-(+)-PHNO was evaluated for use as an agonist PET radiotracer. In vitro, (+)-PHNO was shown, through competitive binding experiments and functional assays for D2 agonism, to be a potent full agonist at the D2 receptor. Ex vivo in rats, [11C]-(+)-PHNO readily crossed the blood-brain barrier and accumulated preferentially in the D2-rich striatum. [11C]-(+)-PHNO pharmacokinetics were rapid, with peak accumulation 5 min after tail-vein injection. The striatal binding of [11C]-(+)-PHNO was highly stereo selective, saturable, had pharmacology appropriate for D2 receptor binding and was sensitive to both increases and decreases in the concentration of endogenous dopamine. These characteristics make [11C]-(+)-PHNO a promising candidate for in vivo imaging of the high-affinity, functional state of the D2 receptor in humans using PET.

Edition Notes

Source: Masters Abstracts International, Volume: 44-06, page: 2775.

Thesis (M.Sc.)--University of Toronto, 2006.

Electronic version licensed for access by U. of T. users.

ROBARTS MICROTEXT copy on microfiche.

The Physical Object

Pagination
75 leaves.
Number of pages
75

ID Numbers

Open Library
OL19215879M
ISBN 13
9780494163764

History Created December 11, 2009 · 2 revisions Download catalog record: RDF / JSON

January 24, 2010 Edited by WorkBot add more information to works
December 11, 2009 Created by WorkBot add works page