Abstract
Several new amino group and acetylamino group substituted benzamides and their 125I labeled compounds were synthesized. The IC50 of (RS)—2—methoxy—4—amino—5—bromo—N—[(1—ethyl—2—pyrrolidinyl) methyl] benzamide was 0.0164 µmol/L, IC50 of sulpride and haloperidol being 0.0991 µmol/L and 0.0156 µmol/L respectively. It showed high affinity for dopamine D2 receptor in vitro. The ratio of striatum to cerebellum and the ratio of striatum to cortex of [125I]—(RS)—2—methoxy—4—acetylamino—5—iodo—N—[(1—ethyl—2—pyrrolidin yl) methyl] benzamide in rats at 60 min after injection were 6.75 respectively. When labeled with 123I, it may be uesful for imaging brain dopamine D2 receptor.
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References
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© 1992 Springer Science+Business Media Dordrecht
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Chang, F.C. et al. (1992). Studies on Substituted Benzamides as Brain Dopamine Receptor Imaging Agent. In: Schubiger, P.A., Westera, G. (eds) Progress in Radiopharmacy. Developments in Nuclear Medicine, vol 22. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-2584-0_4
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DOI: https://doi.org/10.1007/978-94-011-2584-0_4
Publisher Name: Springer, Dordrecht
Print ISBN: 978-94-010-5140-8
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