NOVEL RHENIUM COMPLEXES DERIVED FROM ALPHA-TROPANOL AS POTENTIAL LIGANDS FOR THE DOPAMINE TRANSPORTER

A series of rhenium complexes was synthesized as model compounds for t he corresponding radioactive technetium-99m complexes for preliminary biological investigations. In a '3 + 1' mixed-ligand approach the trop anol molecule was linked with the metal core through a omega-mercaptoe ster group as monodentate ligand. Bis(thioethyl)sulphide was used as t he tridentate dithiol ligand to block the remaining free coordination sites. The omega-mercaptoesters were synthesized via the trityl-protec ted precursors. Binding tests on the cloned human dopamine transporter revealed moderate binding affinities for some of the prepared compoun ds. The complexes were characterised by X-ray and the lipophilicity as well as pK(a) values were determined. (C) 1998 Elsevier Science Ltd. All rights reserved.