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碘-125 4-碘代喹核酯和氚-3喹核酯在体内和体外的特性。

The characteristics of I-125 4-IQNB and H-3 QNB in vivo and in vitro.

作者信息

Gibson R E, Weckstein D J, Jagoda E M, Rzeszotarski W J, Reba R C, Eckelman W C

出版信息

J Nucl Med. 1984 Feb;25(2):214-22.

PMID:6726431
Abstract

The accumulation of (R)-(H-3)-3-quinuclidinyl benzilate (H-3 QNB) and (R,S)-1-azabicyclo(2.2.2)oct-3-yl (R,S)-alpha-hydroxy-(4-[I-125]iodophenyl) benzeneacetate (I-125 4- IQNB ) in heart, caudate/putamen, and cerebellum of rats was determined at intervals from 15 min to 4 hr after injection. The behavior of the two radiotracers in the heart is consistent with in vitro results with respect to affinities and specificities. In the brain, however, the compounds differ in tissue selectivity. At high specific activity, neither compound provides localization that is consistent with the concentration of receptor in the tissues. The results of this study do not indicate quantification of receptor concentration by means of single external images.

摘要

在注射后15分钟至4小时的不同时间间隔,测定了大鼠心脏、尾状核/壳核和小脑中(R)-(H-3)-3-喹核醇基苯甲酸酯(H-3 QNB)和(R,S)-1-氮杂双环(2.2.2)辛-3-基(R,S)-α-羟基-(4-[I-125]碘苯基)苯乙酸酯(I-125 4-IQNB)的蓄积情况。两种放射性示踪剂在心脏中的行为在亲和力和特异性方面与体外结果一致。然而,在大脑中,这两种化合物在组织选择性上有所不同。在高比活度下,两种化合物都不能提供与组织中受体浓度一致的定位。本研究结果并未表明可通过单次外部图像对受体浓度进行定量。

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