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THE QUARTERLY JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Rivista di Medicina Nucleare e Imaging Molecolare


A Journal on Nuclear Medicine and Molecular Imaging
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  RADIOPHARMACOLOGY


The Quarterly Journal of Nuclear Medicine 2001 June;45(2):124-38

lingua: Inglese

Vulnerability of Positron Emission Tomography radiotracers to endogeneous competition. New insights

Laruelle M., Huang Y.

From the Depart­ments of Psy­chi­atry and ­Radiology, ­Columbia Uni­ver­sity Col­lege of Phy­si­cians and Sur­geons, and New ­York ­State Psy­chi­atric Insti­tute, New ­York, NY, USA


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PET and ­SPECT neu­ro­re­ceptor ­imaging tech­niques com­bined ­with phar­mac­o­log­ical chal­lenges ­have ­been intro­duced to ­measure ­acute fluc­tu­a­tions of syn­aptic dop­a­mine (DA) con­cen­tra­tions in the ­living ­human ­brain. ­Changes in the in ­vivo ­binding of radio­lig­ands fol­lowing manip­u­la­tion of trans­mitter ­levels are gen­er­ally ­believed to be ­driven by ­binding com­pe­ti­tion ­between the radio­ligand and neu­ro­trans­mitter. ­This ­imaging ­modality has ­been ­very suc­cessful in the ­study of DA trans­mis­sion at D2 recep­tors. Yet, the exten­sion of ­this tech­nique to the ­study of ­other neu­ro­trans­mitter ­systems has ­proven dif­fi­cult. ­This ­paper ­reviews ­recent evi­dence sug­gesting ­that ­simple ­binding com­pe­ti­tion ­might not be the ­only phe­nom­enon reg­u­lating trans­mitter-radio­ligand inter­ac­tions in ­vivo, and exam­ines ­emerging ­data indi­cating ­that ­receptor traf­ficking ­might ­also be ­involved. A ­better under­standing of the mech­a­nisms under­lying ­these inter­ac­tions ­should facil­i­tate the devel­op­ment of PET and ­SPECT radio­tracers suit­able for the ­reporting of syn­aptic trans­mitter ­levels.

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