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The DAT Ligand [ 18 F]PR17.MZ Mirrors the in vivo Pharmacokinetic Profile of [ 11 C]Cocaine with Significantly Improved Monoamine Transporter Selectivity
Author(s) -
Riss Patrick J.,
Piel Markus,
Bockhart Vanessa,
Bausbacher Nicole,
Buchholz HansGeorg,
Lueddens Hartmut,
Roesch Frank
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000237
Subject(s) - dopamine transporter , transporter , in vivo , ligand (biochemistry) , pharmacokinetics , selectivity , monoamine neurotransmitter , pharmacology , dopamine , chemistry , norepinephrine transporter , in vitro , psychology , medicine , neuroscience , biochemistry , receptor , gene , biology , genetics , serotonin , catalysis
Better than cocaine for your PET? The radiotracer [ 18 F]PR17.MZ shows high in vitro and in vivo selectivity to the dopamine transporter. Its extraordinarily rapid pharmacokinetic profile is demonstrated in a μPET imaging study. The relatively long half‐life of the fluorine‐18 label is an added advantage over short‐lived (−)‐ N ‐[ 11 C]cocaine PET ligands.