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

Gildersleeve DL; Van Dort ME; Johnson JW; Sherman PS; Wieland DM

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

机译：（123I）-iodo-PK11195的合成和评估，用于在心脏中定位外周型苯并二氮杂receptor受体（ω3）。

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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 [123I]- and [125I]-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 [123I]PK11195. These results suggest that [123I]PK11195 has potential as a SPECT radiotracer for studying the omega 3 receptor in humans.

机译：PK11195的碘化类似物1-（2-氯苯基）-N-甲基-N-（1-甲基丙基）异喹啉-3-羧酰胺是外周型苯并二氮杂receptor受体（ω3）的特异性拮抗剂。三个步骤，总化学产率为40％。 [123I]-和[125I]-碘-PK11195均已通过固态同位素交换以> 60％的分离放射化学产率和233-348 mCi / mmol的比活合成。在大鼠中进行的组织分布研究表明，肾上腺，心脏，肺和肾脏对放射性的摄取很高，而预先服用冷的PK11195可以阻断63-87％的放射性。 [123I] PK11195已完成犬心脏的单光子发射计算机断层扫描（SPECT）成像。这些结果表明，[123I] PK11195具有作为SPECT放射性示踪剂研究人类欧米伽3受体的潜力。

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《Nuclear Medicine and Biology》 |1996年第1期|共6页
作者
Gildersleeve DL; Van Dort ME; Johnson JW; Sherman PS; Wieland DM;
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正文语种 eng
中图分类特种医学;
关键词
Heart; Isoquinolines; Myocardium; Receptors; GABA-A; 心脏; 异喹啉类; 心肌; 受体; GABA-A;

机译：Heart;Isoquinolines;Myocardium;Receptors;GABA-A;心脏;异喹啉类;心肌;受体;GABA-A;

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1. Synthesis and evaluation of (123I)-iodo-PK11195 for mapping peripheral-type benzodiazepine receptors (omega 3) in heart. [J] . Gildersleeve DL, Van Dort ME, Johnson JW, Nuclear Medicine and Biology . 1996,第1期

机译：（123I）-iodo-PK11195的合成和评估，用于在心脏中定位外周型苯并二氮杂receptor受体（ω3）。
2. Synthesis and evaluation of (123I)labelled analogues of the partial inverse agonist Ro 15-4513 for the study of diazepam-insensitive benzodiazepine receptors. [J] . Katsifis A, Mardon K, McPhee M, Nuclear Medicine and Biology . 1999,第6期

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

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