Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine.
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.
Hoepping
A
A
Drug Discovery Program, Georgetown University Medical Center, Washington DC 20007-2197, USA.
Babich
J
J
Zubieta
J A
JA
Johnson
K M
KM
Machill
S
S
Kozikowski
A P
AP
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
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