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

Authors: Zhang, Ao¹; Kula, Nora S.¹; Zhang, Kehong¹; Baldessarini, Ross J.¹; Kaufman, Marc J.¹; Renshaw, Perry F.¹; Neumeyer, John L.¹

Source: Letters in Drug Design & Discovery, Volume 2, Number 4, June 2005 , pp. 302-306(5)

Publisher: Bentham Science Publishers

Key:

- Free Content

- New Content

- Subscribed Content

- Free Trial Content

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 mgr

M 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.

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

Document Type: Review article

DOI: 10.2174/1570180054038332

Affiliations: 1: Medicinal Chemistry Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478-9106, USA.

Your trusted access to this article has expired.

The full text electronic article is available for purchase. You will be able to download the full text electronic article after payment.

$55.10 plus tax Refund Policy