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In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D2-like dopamine receptors

Authors
Journal
Bioorganic & Medicinal Chemistry
0968-0896
Publisher
Elsevier
Publication Date
Volume
15
Issue
21
Identifiers
DOI: 10.1016/j.bmc.2007.07.017
Keywords
  • Benzamides
  • Dopamine Receptors
  • In Vitro Affinities
Disciplines
  • Medicine

Abstract

Abstract Benzamide derivatives as radiotracers have played an important role in diagnosing malfunction in dopaminergic neurotransmission. A variety of halogenated and two unsubstituted benzamide derivatives were synthesised and their in vitro affinities to dopaminergic, serotonergic and adrenergic receptors and their lipophilicities were determined. As references IBZM ( 3), raclopride ( 4) and FLB457 ( 5) were tested as well. The two iodinated compounds NAE ( 27) and NADE ( 28) displayed K i values of 0.68 and 14 nM for the D 2 receptor. The well-established radiotracers FP ( 1) and DMFP ( 2) showed affinities in the same range as did the brominated compounds NABrE ( 29) and NABrDE ( 30). The log D 7.4 values of 2.91 for NAE ( 27) and of 2.81 for NADE ( 28) are in the range of those found for IBZM ( 3), FP ( 1) and DMFP ( 2). These facts allow to expect good properties for the two iodinated compounds NAE ( 27) and NADE ( 28) regarding in vivo imaging with SPECT.

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