SPECT imaging of dopamine receptors with [123I]epidepride: characterization of uptake in the human brain.
[123I]Epidepride is a new ligand for single photon emission computerized tomography (SPECT) that specifically labels D2-like dopamine receptors with very high affinity. Here, we report on the regional kinetic uptake of [123I]epidepride in the brain of 4 normal volunteers and 3 patients with choreatic movement disorders. In healthy subjects striatal activity peaked at 2.5 hours after injection of the tracer and decreased slowly thereafter. There were no significant differences between left and right brain hemispheres. Activity above background was also measurable in areas corresponding to the thalamus, temporal cortex and frontal cortex. The striatal to cerebellar ratio was about 14 after 2.5 hours and this ratio steadily increased with time. The striatal to cerebellar ratio was clearly reduced in all 3 patients with choreatic movement disorders (from about 14 in control subjects after 2.5 hours to about 7 in choreatic patients). [123I]Epidepride may be a useful SPECT ligand for studying D2 receptors in the living human brain because of its high target to background ratio, its high affinity and the possibility to investigate extrastriatal D2 receptors.
Kornhuber
J
J
University Clinics for Neurology and Nuclear Medicine, Vienna, Austria.
Brücke
T
T
Angelberger
P
P
Asenbaum
S
S
Podreka
I
I
D000328:Adult; D000368:Aged; D001549:Benzamides / Q000493:pharmacokinetics*; D001921:Brain / Q000378:metabolism*; D002819:Chorea / Q000378:metabolism; D005260:Female; D006801:Humans; D007457:Iodine Radioisotopes; D008297:Male; D008875:Middle Aged; D011759:Pyrrolidines / Q000493:pharmacokinetics*; D011954:Receptors, Dopamine / Q000378:metabolism*; D015899:Tomography, Emission-Computed, Single-Photon
D001549:Benzamides; D007457:Iodine Radioisotopes; D011759:Pyrrolidines; D011954:Receptors, Dopamine; C063525:epidepride