Development of Polyfluorophenyltropanes: Potential Probes for 19F Magnetic Resonance Imaging (MRI) and Spectroscopy (MRS) Assessments of the Dopamine Transporter

Title: Development of Polyfluorophenyltropanes: Potential Probes for 19F Magnetic Resonance Imaging (MRI) and Spectroscopy (MRS) Assessments of the Dopamine Transporter

Volume: 2 Issue: 4

Author(s): Ao Zhang, Nora S. Kula, Kehong Zhang, Ross J. Baldessarini, Marc J. Kaufman, Perry F. Renshaw and John L. Neumeyer

Affiliation:

Keywords: polyfluorophenyltropane, magnetic resonance imaging, magnetic resonance spectroscopy, dopamine transporter

Abstract: A novel series of nonradiolabeled, polyfluorinated phenyltropanes were developed containing three or more 19 F atoms/molecule in a magnetic resonance (MR) equivalent chemical environment to increase coherent MR signal characteristics. Competitive radioreceptor affinity assays of such compounds yielded nM affinity at dopamine (DAT) and serotonin (SERT) transporters in rat brain tissue. Compound 3b (MCL-314) at 50 μM gave a clear magnetic resonance spectroscopy signal, and 9 (MCL-319) yielded very high DAT potency and improved selectivity over SERT. Such compounds might potentially serve as MRI- or MRS-detectable index ligands for the dopamine transporter proteins, and preliminary observations call for further study of additional polyfluorinated phenyltropanes.

Cite this article as:

Zhang Ao, Kula S. Nora, Zhang Kehong, Baldessarini J. Ross, Kaufman J. Marc, Renshaw F. Perry and Neumeyer L. John, Development of Polyfluorophenyltropanes: Potential Probes for 19F Magnetic Resonance Imaging (MRI) and Spectroscopy (MRS) Assessments of the Dopamine Transporter, Letters in Drug Design & Discovery 2005; 2 (4) . https://dx.doi.org/10.2174/1570180054038332