Dopamine transporter imaging ligand

US6358492B1 · kind B1 · utility

Assignee

• Research Triangle Institute · US

Inventors

• Michael J. Kuhar · Baltimore, US
• Frank Ivy Carroll · Durham, US
• John W. Boja · Baltimore, US
• Anita H. Lewin · Chapel Hill, US
• Philip Abraham · Cary, US

Key dates

• Filing date: Oct 7, 1997
• Grant date: Mar 19, 2002
• Expiry date: Oct 7, 2017

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D451/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The 3&agr; isomer of RTI-55, RTI-352, is an effective in vivo binding ligand that reflects greater selectivity for the dopamine transporter than is observed with RTI-55. In addition, there is also a more rapid achievement of apparent equilibrium in the striatal-to-cerebellar ratio (compared to RTI-55) as the ratio peaks at about 30 min and is maintained for about 20 min thereafter. Such apparent equilibrium is useful in developing an approach to measuring the number of dopamine transporters present in tissues. Moreover, these results indicate that the utilization of 3&agr; isomers of a variety of 3&bgr;-(substituted phenyl)tropanes will result in greater selectivity for dopamine transporters and a more rapid of achievement of apparent equilibrium.