| Autor: |
Hirani, E., Gillies, J., Karasawa, A., Shimada, J., Kase, H., Opacka‐Juffry, J., Osman, S., Luthra, S.K., Hume, S.P., Brooks, D.J. |
| Zdroj: |
Synapse; December 2001, Vol. 42 Issue: 3 p164-176, 13p |
| Abstrakt: |
KW‐6002, a xanthine‐based adenosine A2Aantagonist, was labelled with the positron emitter carbon‐11 by O‐methylation of its precursor, KF23325, using [11C]iodomethane and was evaluated in rats as a putative in vivo radioligand for positron emission tomography (PET). Following intravenous injection of [11C]KW‐6002, radioactivity was measured in blood, plasma, peripheral tissues, and in discrete brain tissues over a 2‐h time period commensurate with PET scanning. In brain, [11C]KW‐6002 showed highest retention in striata, with evidence of saturable binding, and lowest retention in frontal cortex (a tissue low in adenosine A2Areceptors). PET scanning with [11C]KW‐6002 demonstrated a specific signal in the striata which could be described using compartmental modelling. Specific binding was, however, also detected in extrastriatal regions, including brain areas reported to have low adenosine A2Areceptor density. Blocking studies with the A1selective antagonist KF15372 and the non xanthine‐type A2Aantagonist ZM 241385 failed to elucidate the nature of this binding. Thus, although [11C]KW‐6002 shows some potential for development as a PET ligand for quantifying striatal adenosine A2Areceptor function, its in vivo selectivity requires further investigation. Synapse 42:164–176, 2001. © 2001 Wiley‐Liss, Inc. |
| Databáze: |
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