Journal article Open Access

Identification of the allosteric P2X7 receptor antagonist [11C]SMW139 as a PET tracer of microglial activation.

Janssen, Bieneke; Vugts, Danielle J; Wilkinson, Shane M; Ory, Dieter; Chalon, Sylvie; Hoozemans, Jeroen JM; Schuit, Robert C; Beaino, Wissam; Kooijman, Esther JM; van den Hoek, Johan; Chishty, Mansoor; Doméné, Aurélie; Van der Perren, Anke; Villa, Alessandro; Maggi, Adriana; Molenaar, Ger T; Funke, Uta; Shevchenko, Rostislav V; Baekelandt, Veerle; Bormans, Guy; Lammertsma, Adriaan A; Kassiou, Michael; Windhorst, Albert D


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    <subfield code="a">Identification of the allosteric P2X7 receptor antagonist [11C]SMW139 as a PET tracer of microglial activation.</subfield>
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    <subfield code="a">&lt;p&gt;&lt;strong&gt;Abstract&lt;/strong&gt;&lt;/p&gt;

&lt;p&gt;The P2X&lt;sub&gt;7&lt;/sub&gt; receptor plays a significant role in microglial activation, and as a potential drug target, the P2X&lt;sub&gt;7&lt;/sub&gt; receptor is also an interesting target in positron emission tomography. The current study aimed at the development and evaluation of a potent tracer targeting the P2X&lt;sub&gt;7&lt;/sub&gt; receptor, to which end four adamantanyl benzamide analogues with high affinity for the human P2X&lt;sub&gt;7&lt;/sub&gt; receptor were labelled with carbon-11. All four analogues could be obtained in excellent radiochemical yield and high radiochemical purity and molar activity, and all analogues entered the rat brain. [&lt;sup&gt;11&lt;/sup&gt;C]SMW139 showed the highest metabolic stability in rat plasma, and showed high binding to the hP2X&lt;sub&gt;7&lt;/sub&gt; receptor in vivo in a hP2X&lt;sub&gt;7&lt;/sub&gt; receptor overexpressing rat model. Although no significant difference in binding of [&lt;sup&gt;11&lt;/sup&gt;C]SMW139 was observed between post mortem brain tissue of Alzheimer&amp;#39;s disease patients and that of healthy controls in in vitro autoradiography experiments, [&lt;sup&gt;11&lt;/sup&gt;C]SMW139 could be a promising tracer for P2X&lt;sub&gt;7&lt;/sub&gt; receptor imaging using positron emission tomography, due to high receptor binding in vivo in the hP2X&lt;sub&gt;7&lt;/sub&gt; receptor overexpressing rat model. However, further investigation of both P2X&lt;sub&gt;7&lt;/sub&gt; receptor expression and binding of [&lt;sup&gt;11&lt;/sup&gt;C]SMW139 in other neurological diseases involving microglial activation is warranted.&lt;/p&gt;</subfield>
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