Radiochemical synthesis and biodistribution of a novel maxi-K potassium channel opener

被引：10

作者：

Kiesewetter, DO

Jagoda, EM

Starrett, JE

Gribkoff, VK

Hewawasam, P

Srinivas, N

Salazar, D

Eckelman, WC

机构：

[1] NIH, Ctr Clin, Positron Emiss Tomog Dept, Bethesda, MD 20892 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Lawrenceville, NJ USA

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2002年 / 29卷 / 01期

关键词：

PET; biodistribution; brain; maxi-K; MaxiPost; BMS-204352;

D O I：

10.1016/S0969-8051(01)00281-5

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

The racemate 1, ((+/-)-(5-Chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)- 2H-indol-21-one), is a potent, specific and novel opener of cloned large-conductance, calcium-activated (maxi-K) potassium channels. One of its enantiomers, BMS-204352 (Maxi-Post(TM)), is undergoing clinical evaluation for efficacy in patients with suspected acute stroke. In the current study, we have prepared [F-18]-labeled 1 using a silver assisted nucleophilic substitution to examine its distribution and disposition in the rat, with particular emphasis on the brain. Biodistribution Studies in rats confirm that brain uptake is rapid and occurs at high levels, and indicate that a major fraction of the compound in the brain does not accumulate by a specific, saturable mechanism. (C) 2002 Elsevier Science Inc. All rights reserved.

引用

页码：55 / 59

页数：5

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