RADIOPHARMACOLOGY 

The Quarterly Journal of Nuclear Medicine 2001 June;45(2):139-52

Copyright © 2009 EDIZIONI MINERVA MEDICA

language: English

Brain radioligands - State of the art and new trends

Halldin C., Gulyás B., Langer O., Farde L.

From the Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, Stockholm, Sweden

Non-inva­sive radio­ligand ­imaging ­methods for ­brain ­receptor ­studies use ­either ­short-­lived posi­tron-emit­ting radio­nu­clides ­such as 11C and 18F for posi­tron emis­sion tomog­raphy (PET) or ­single ­photon-emit­ting radio­nu­clides ­such as 123I for ­single ­photon emis­sion com­puted tomog­raphy (­SPECT). PET and ­SPECT use radio­lig­ands ­which are ­injected intra­ve­nously ­into experi­mental ani­mals, ­human vol­un­teers or ­patients. The ­main appli­ca­tions of radio­lig­ands in ­brain ­research con­cern ­human neu­ro­psy­cho­phar­ma­cology and the dis­covery and devel­op­ment of ­novel ­drugs to be ­used in the ­therapy of neu­ro­log­ical and psy­chi­atric dis­or­ders. A ­basic ­problem in PET and ­SPECT ­brain ­receptor ­studies is the ­lack of ­useful radio­lig­ands ­with appro­priate ­binding char­ac­ter­is­tics. Pre­req­ui­site cri­teria ­need to be sat­is­fied for a radio­ligand to ­reveal ­target ­binding ­sites in ­vivo. ­This sec­tion ­will dis­cuss ­these impor­tant cri­teria and ­also ­review ­recent exam­ples in neu­ro­re­ceptor radio­ligand devel­op­ment ­such as selec­tive radio­lig­ands for ­brain mono­amine trans­porters.