Nucl Med Mol Imaging.  2007 Apr;41(2):118-131.

Radiopharmaceuticals for Neurotransmitter Imaging

• Oh SJ

Abstract

Neurotransmitter imaging with radiopharmaceuticals plays major role for understanding of neurological and psychiatric disorders such as Parkinson's disease and depression. Radiopharmaceuticals for neurotransmitter imaging can be divided to dopamine transporter imaging radiopharmaceuticals and serotonin trnasporter imaging radiopharmaceuticals. Many kinds of new dopamine transporter imaging radiopharmcaeuticals has a tropane ring and they showed different biological properties according to the substituted functional group on tropane ring. After the first clinical trials with [123I]beta-CIT, alkyl chain substituent introduced to tropane ring amine to decrease time for imaging acquisition and to increase selectivity. From these results, [123I]PE2I, [18F]FE-CNT, [123I]FP-CIT and [18F]FP-CIT were developed and they showed high uptake on the dopamine transporter rich regions and fast peak uptake equilibrium time within 4 hours after injection. [11C]McN 5652 was developed for serotonin trnasporter imaging but this compound showed slow kinetics and high background radioactivity. To overcome these problems, new diarylsulfide backbone derivatives such as ADAM, ODAM, AFM, and DASB were developed. In these candidates, [11C]AFM and [11C]DASB showed high binding affinity to serotonin transporter and fast in vivo kinetics. This paper gives an overview of current status on dopamine and serotonin transporter imaging radiopharmaceuitcals and the development of new lead compounds as potential radiopharmaceuticals by medicinal chemistry.

Keyword

PET; SPECT; radiopharmaceuticals; dopamine transporter; serotonin transporter

MeSH Terms

Chemistry, Pharmaceutical
Depression
Dopamine
Dopamine Plasma Membrane Transport Proteins
Kinetics
Neurotransmitter Agents*
Parkinson Disease
Radioactivity
Radiopharmaceuticals*
Serotonin
Serotonin Plasma Membrane Transport Proteins
Tomography, Emission-Computed, Single-Photon
Dopamine
Dopamine Plasma Membrane Transport Proteins
Neurotransmitter Agents
Radiopharmaceuticals
Serotonin
Serotonin Plasma Membrane Transport Proteins