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This study explored the use of the α2C‐adrenoceptor PET tracer [11C]ORM‐13070 to monitor α2C‐AR occupancy in the human brain. The subtype‐nonselective α2‐AR antagonist atipamezole was administered to eight healthy volunteer subjects to determine its efficacy and potency (Emax and EC50) at inhibiting tracer uptake. We also explored whether the tracer could reveal changes in the synaptic concentrations...
Rationale No validated methods have been available for studying brain noradrenergic neurotransmission in vivo in humans. Positron emission tomography (PET) radiotracers are widely used in clinical drug development targeted to brain receptors and can also in some cases be employed to monitor extracellular (synaptic) neurotransmitter concentrations. Objectives The objective of this study is to test...
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