Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET.

Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET. Research Abstract Details 

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Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET. Abstract Text:

Masahiro Mishina,Kiichi Ishiwata,Yuichi Kimura,Mika Naganawa,Keiichi Oda,Shiro Kobayashi,Yasuo Katayama,Kenji Ishii,

Adenosine A(2A) receptor (A2AR) is thought to interact with dopamine D(2) receptor. Selective A2AR antagonists have attracted attention as the treatment of Parkinson's disease. In this study, we investigated the distribution of the A2ARs in the living human brain using positron emission tomography (PET) and [7-methyl-(11)C]-(E)-8-(3,4,5-trimethoxystyryl)-1,3,7-trimethylxanthine ([(11)C]TMSX). We recruited five normal male subjects. A dynamic series of PET scans was performed for 60 min, and the arterial blood was sampled during the scan to measure radioactivity of the parent compound and labeled metabolites. Circular regions of interest of 10-mm diameter were placed in the PET images over the cerebellum, brainstem, thalamus, head of caudate nucleus, anterior and posterior putamen, frontal lobe, temporal lobe, parietal lobe, occipital lobe, and posterior cingulate gyrus for each subject. A two-tissue, three-compartment model was used to estimate K(1), k(2), k(3), and k(4) between metabolite-corrected plasma and tissue time activity of [(11)C]TMSX. The binding potential (BP) was the largest in the anterior (1.25) and posterior putamen (1.20), was next largest in the head of caudate nucleus (1.05) and thalamus (1.03), and was small in the cerebral cortex, especially frontal lobe (0.46). [(11)C]TMSX PET showed the largest BP in the striatum in which A2ARs were enriched as in postmortem and nonhuman studies reported, but that the binding of [(11)C]TMSX was relatively larger in the thalamus to compare with other mammals. To date, [(11)C]TMSX is the only promising PET ligand, which is available to clinical use for mapping the A2ARs in the living human brain.

Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET. Publishing Authors By Initials

M Mishina,K Ishiwata,Y Kimura,M Naganawa,K Oda,S Kobayashi,Y Katayama,K Ishii,

For similar heterocyclic compounds: alkaloids: xanthines research abstracts see: heterocyclic compounds: alkaloids: xanthines research

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Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Synapse (New York, N.Y.)

VOLUME: 61

Page Numbers: 778-84

Journal Abbreviation: Synapse

ISSN: 0887-4476

DAY: 29

MONTH: Sep

YEAR: 2007

Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET. Information

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LANGUAGE: eng

NlmUniqueID: 8806914

Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET. Keywords Mesh Terms:

KEYWORDS: Xanthines

MESH TERMS: pharmacokinetics

Chemical & Substance for Abstract: Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET. Information

Substance Name: Xanthines

Registry Number: 0

Grant and Affiliation Information for Evaluation of distribution of adenosine A2A receptors in normal human brain measured with [11C]TMSX PET.

AFFILIATION: Neurological Institute, Nippon Medical School Chiba-Hokusoh Hospital, Imba-gun, Chiba-ken 270-1694, Japan.

Country: United States

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MEDLINETA: Synapse

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