Description: Evaluation of novel tropane analogues in comparison with binding characteristics of [18F]FP-CIT and [131I]beta-CIT

This title appears in the Scientific Report : 2007

Evaluation of novel tropane analogues in comparison with binding characteristics of [18F]FP-CIT and [131I]beta-CIT

This study evaluated novel potential dopamine transporter (DAT) inhibitors as ligands for positron emission tomography. Five new tropane analogs were synthesized and compared with the known ligand 2beta-carbomethoxy-3beta-(4-iodophenyl)tropane (beta-CIT) and the recently characterized ligands N-(3-i...

Personal Name(s):	Sihver, W.
	Drewes, B. / Schulze, A. / Olsson, R. A. / Coenen, H. H.
Contributing Institute:	Nuklearchemie; INB-4
Published in:	Nuclear medicine and biology, 34 (2007) S. 211 - 219
Imprint:	Amsterdam [u.a.] Elsevier 2007
Physical Description:	211 - 219
DOI:	10.1016/j.nucmedbio.2006.11.005
PubMed ID:	17307129
Document Type:	Journal Article
Research Program:	Funktion und Dysfunktion des Nervensystems
Series Title:	Nuclear Medicine and Biology 34
Subject (ZB):	Animals Brain: metabolism Brain: radionuclide imaging Cocaine: analogs & derivatives Cocaine: diagnostic use Cocaine: pharmacokinetics Fluorine Radioisotopes: diagnostic use Fluorine Radioisotopes: pharmacokinetics Iodine Radioisotopes: diagnostic use Iodine Radioisotopes: pharmacokinetics Metabolic Clearance Rate Organ Specificity Protein Binding Radiopharmaceuticals: diagnostic use Radiopharmaceuticals: pharmacokinetics Rats Rats, Wistar Tissue Distribution Tropanes: chemistry Tropanes: diagnostic use Tropanes: pharmacokinetics Fluorine Radioisotopes Iodine Radioisotopes Radiopharmaceuticals Tropanes RTI 55 Cocaine J dopamine transporter tropane derivatives fluorinated radioligand brain imaging
	Publikationsportal JuSER

Please use the identifier: http://dx.doi.org/10.1016/j.nucmedbio.2006.11.005 in citations.

This study evaluated novel potential dopamine transporter (DAT) inhibitors as ligands for positron emission tomography. Five new tropane analogs were synthesized and compared with the known ligand 2beta-carbomethoxy-3beta-(4-iodophenyl)tropane (beta-CIT) and the recently characterized ligands N-(3-iodoprop-2E-enyl)-2beta-carbomethoxy-3beta-(4-methylphenyl)-nortropane (PE2I) and 2beta-carbofluoroethoxy-3beta-(4-methylphenyl)tropane (FETT). Evaluation with autoradiography measured the ability to antagonize the binding of [(131)I]iodine-labeled beta-CIT and [(18)F]fluorine-labeled N-(3-fluoropropyl)-2beta-carbomethoxy-3beta-(4-iodo-phenyl) nortropane in rat and pig brains. The standards for comparison (PE2I and FETT) competed strongly in all regions investigated (striatum, cortex, superior colliculus and cerebellum). Of the new compounds, 2alpha-amido-fluoroethyl-3beta-(4-iodophenyl)tropane (4) and 2beta-amido-fluoroethyl-3beta-(4-iodophenyl)tropane (4a) competed strongly with [(131)I]beta-CIT in DAT-rich striatum, but also in other brain regions suggesting poor DAT selectivity. Because [(131)I]beta-CIT binds unselectively both to DAT and serotonin transporters, no definite conclusion about the selectivity of the new compounds is possible. However, preclinical studies using the compounds and labeled with fluorine-18 or iodine-131 are encouraged.