Binding characteristics of the 5‐HT2A receptor antagonists altanserin and MDL 100907

To study the 5‐HT2A receptors in the living human brain, using positron emission tomography (PET), two selective radiotracers are currently in use: [18F]altanserin and [11C]MDL 100907. It is, however, currently unknown to what extent data obtained with either tracer are directly comparable. The aim of this study was to compare binding characteristics of these two radiotracers in rat brain with respect to affinity (Kd), receptor binding density (Bmax), binding potential (BP), and nonspecific binding. Further, binding kinetics, sensitivity towards competition with the endogenous transmitter serotonin, and the competitive/noncompetitive interaction between the two radioligands were evaluated. In addition, the selectivity of [18F]altanserin for the 5‐HT2A receptor was assessed.

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