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Journal of Nuclear Medicine Vol. 47 No. 2 302-312
© 2006 by Society of Nuclear Medicine


Continuing Education

Brain Receptor Imaging*

Wolf-Dieter Heiss, MD1 and Karl Herholz, MD2

1 Max-Planck Institute for Neurological Research and Department of Neurology, University of Cologne, Cologne, Germany; and 2 Wolfson Molecular Imaging Centre, University of Manchester, Manchester, United Kingdom

Correspondence: For correspondence or reprints contact: Wolf-Dieter Heiss, MD, Max-Planck Institute for Neurological Research, Gleueler Strasse 50, 50931 Köln, Germany. E-mail: wdh{at}pet.mpin-koeln.mpg.de

Receptors have a prominent role in brain function, as they are the effector sites of neurotransmission at the postsynaptic membrane, have a regulatory role on presynaptic sites for transmitter reuptake and feedback, and are modulating various functions on the cell membrane. Distribution, density, and activity of receptors in the brain can be visualized by radioligands labeled for SPECT and PET, and the receptor binding can be quantified by appropriate tracer kinetic models, which can be modified and simplified for particular application. Selective radioligands are available for the various transmitter systems, by which the distribution of these receptors in the normal brain and changes in receptor binding during various physiologic activities or resulting from pathologic conditions can be visualized. The quantitative imaging for several receptors has gained clinical importance—for example, dopamine (D2) receptors for differential diagnosis of movement disorders and for assessment of receptor occupancy by neuroleptics drugs; serotonin (5-hydroxytryptamine, 5-HT) receptors and the 5-HT transporter in affective disorders and for assessment of activity of antidepressants; nicotinic receptors and acetylcholinesterase as markers of cognitive and memory impairment; central benzodiazepine-binding sites at the {gamma}-aminobutyric acid A (GABAA) receptor complex as markers of neuronal integrity in neurodegenerative disorders, epilepsy, and stroke and as the site of action of benzodiazepines; peripheral benzodiazepine receptors as indicators of inflammatory changes; opioid receptors detecting increased cortical excitability in focal epilepsy but also affected in perception of and emotional response to pain; and several receptor systems affected in drug abuse and craving. Further studies of the various transmitter/receptor systems and their balance and infraction will improve our understanding of complex brain functions and will provide more insight into the pathophysiology of neurologic and psychiatric disease interaction.

Key Words: receptor binding • radioligands • PET • SPECT • dopamine • serotonin • cholinergic receptors • benzodiazepine-binding sites • opioid receptors • adenosine receptors


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