Mapping adenosine A1 receptors in the cat brain by positron emission tomography with [11C]MPDX

Abstract We evaluated the potential of [ 11 C]MPDX as a radioligand for mapping adenosine A 1 receptors in comparison with previously proposed [ 11 C]KF15372 in cat brain by PET. Two tracers showed the same brain distribution. Brain uptake of [ 11 C]MPDX (Ki = 4.2 nM) was much higher and washed out faster than that of [ 11 C]KF15372 (Ki = 3.0 nM), and was blocked by carrier-loading or displaced with an A 1 antagonist. The regional A 1 receptor distribution evaluated with kinetic analysis is consistent with that previously measured in vitro. [ 11 C]MPDX PET has a potential for mapping adenosine A 1 receptors in brain.

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