PMID: 2525621Jul 1, 1989Paper

(+/-)-7-chloro-8-hydroxy-1-(4'-[125I]iodophenyl)-3-methyl-2,3,4,5- tetrahydro-1H-3-benzazepine: a potential CNS D-1 dopamine receptor imaging agent

Journal of Medicinal Chemistry
S ChumpraditS Pan

Abstract

Synthesis, radiolabeling, and in vitro and in vivo properties of an iodinated benzazepine, (+/-)-7-chloro-8-hydroxy-1-(4'-[125I]iodophenyl)-3- methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, [125I]FISCH, as a potential imaging agent for evaluation of central nervous system (CNS) D-1 dopamine receptors in humans, were investigated. After an iv injection, this benzazepine derivative showed good brain uptake in rats (2.27, 1.40, 0.55% dose/whole brain at 2, 15, and 60 min, respectively). The striatum/cerebellum ratio was high (2.47 at 60 min after the injection). The binding affinity of this agent in rat striatum tissue preparation displayed a Kd of 1.43 +/- 0.15 nM. Competition data (in vitro) showed the following rank order of potency: SCH-23390 greater than (+/-)-FISCH greater than (+/-)-IBZP much greater than apomorphine greater than WB 4010 greater than ketanserin approximately spiperone. The preliminary data suggest that the agent is highly selective for the CNS D-1 receptor.

Citations

Jan 1, 1990·European Journal of Nuclear Medicine·B Mazière, M Mazière
Sep 7, 2007·Cancer Biotherapy & Radiopharmaceuticals·Sotiris Missailidis, Alan Perkins
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Kenji ArimitsuHideo Saji
Mar 17, 2012·Chemical Communications : Chem Comm·Bidyut Kumar DindaDipakranjan Mal
Dec 26, 2001·Chemical Reviews·C F Shaw III
Jul 3, 2013·The Journal of Organic Chemistry·Naseem Iqbal, Anne Fiksdahl

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