Synthesis and evaluation of [I-123]-Iodo-PK11195 for mapping peripheral-type benzodiazepine receptors (omega(3)) in heart

被引：35

作者：

Gildersleeve, DL

VanDort, ME

Johnson, JW

Sherman, PS

Wieland, DM

机构：

[1] Division of Nuclear Medicine, Department of Internal Medicine, Univ. of Michigan Medical Center, Ann Arbor

[2] Division of Nuclear Medicine, 3480 Kresge Bldg. III, Univ. of Michigan Medical School, Ann Arbor

[3] College of Human Medicine, Michigan State University, East Lansing

来源：

NUCLEAR MEDICINE AND BIOLOGY | 1996年 / 23卷 / 01期

关键词：

mitochondrial benzodiazepine receptor; isoquinolines; rat; dog; iodine radioisotopes; emission-computed tomography;

D O I：

10.1016/0969-8051(95)02007-1

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：

An iodinated analog of PK11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)isoquinoline-3-carboxamide, a specific antagonist of the peripheral-type benzodiazepine receptor (omega(3)), has been synthesized in three steps with an overall chemical yield of 40%. Both [I-123]- and [I-125]-Iodo-PK11195 have been synthesized by solid-state isotopic exchange in >60% isolated radiochemical yield and specific activity of 233-348 mCi/mmol. Tissue distribution studies in rats indicate a high uptake of radioactivity in adrenal glands, heart, lung and kidneys, which was blocked 63-87% by preadministration of cold PK11195. Single photon emission computer tomography (SPECT) imaging of the canine heart has been accomplished with [I-123]PK11195. These results suggest that [I-123]PK11195 has potential as a SPECT radiotracer for studying the omega(3) receptor in humans.

引用

页码：23 / 28

页数：6

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