Dopamine transporter imaging agents
AssigneesOrganix, Inc., President and Fellow of Harvard College, The General Hospital Corporation
InventorsPeter C. Meltzer, Paul Blundell, Bertha K. Madras, Alan J. Fischman, Alun G. Jones, Ashfaq Mahmood
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Abstract
Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.
Claims1
A radiopharmaceutical compound which is capable of complexing with 99mTc, said compound having the following structural formula:
- wherein R1 is α or β and is CORa;
- R2 is a and is selected from the group consisting of C6H4X, C6H3XY, C10H7X, and C10H6XY;
- Ra is CH2CH3;
- X and Y are independently selected from the group consisting of Ra, H, Br, Cl, I, F, OH, and OCH3;
- L is —(CH2)n where n is an integer from 1 to 6, or —(CH2)n-(aryl, arylalkyl, ethenyl or ethynyl)-(CH2)m— where m and n are integers and the sum of n plus m is an integer from 1 to 6;
- and
- Ch is a tridentate or tetradentate chelating ligand that forms a neutral complex with technetium or rhenium,
- wherein the compound is N-[2-(3′-N′-Propyl-(1″R-3″α-(4-fluorophenyl)tropane-2″β-(1-propanoyl))((2-((triphenylmethyl)thio)ethyl)amino)acetyl]-S-(triphenyl)-2-aminoethanethiol.
Dependencies are inferred from the claim text.