title: Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine.
abstract: Two new technetium complexes containing a piperidine template have been synthesized and evaluated as possible leads for the development of dopamine transporter (DAT) imaging agents. Binding data for the corresponding rhenium complexes containing either a monoaminomonoamide (MAMA') or a diaminodithiol (DADT) chelating unit exhibited significant affinity for the DAT. Initial biodistribution studies in rats revealed only a low brain uptake.
authors.affiliation: Drug Discovery Program, Georgetown University Medical Center, Washington DC 20007-2197, USA.
authors.forename: A
authors.initials: A
authors.lastname: Hoepping
authors.forename: J
authors.initials: J
authors.lastname: Babich
authors.forename: J A
authors.initials: JA
authors.lastname: Zubieta
authors.forename: K M
authors.initials: KM
authors.lastname: Johnson
authors.forename: S
authors.initials: S
authors.lastname: Machill
authors.forename: A P
authors.initials: AP
authors.lastname: Kozikowski
mesh_terms: D000818:Animals; D002352:Carrier Proteins / Q000378:metabolism*; D003042:Cocaine / Q000737:chemistry*; D050483:Dopamine Plasma Membrane Transport Proteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D010880:Piperidines / Q000737:chemistry*; D011485:Protein Binding; D011869:Radioligand Assay; D051381:Rats; D014018:Tissue Distribution
chemical_list: D002352:Carrier Proteins; D050483:Dopamine Plasma Membrane Transport Proteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D009942:Organometallic Compounds; D015609:Organotechnetium Compounds; D010880:Piperidines; C493216:Slc6a3 protein, rat; C112051:technetium Tc 99m diaminedithiol; C401743:technetium Tc 99m-monoaminomonoamide; D003042:Cocaine