D2拮抗剂和激动剂对体内125I标记的3-碘苯甲酰胺（IBZM）与多巴胺受体结合的阻断作用。

Blockade of in vivo binding of 125I-labeled 3-iodobenzamide (IBZM) to dopamine receptors by D2 antagonist and agonist.

作者信息

Singhaniyom W, Tsai Y F, Brücke T, McLellan C A, Cohen R M, Kung H F, Chiueh C C

机构信息

Section on Clinical Brain Imaging, National Institute of Mental Health, Bethesda, MD 20892-1000.

出版信息

Brain Res. 1988 Jun 21;453(1-2):393-6. doi: 10.1016/0006-8993(88)90186-2.

DOI:10.1016/0006-8993(88)90186-2

PMID:2969766

Abstract

The in vivo binding of [125I]3-iodobenzamide (IBZM), a substituted benzamide, to DA receptor binding sites in the caudate nucleus, nucleus accumbens, and olfactory tubercle was investigated by using ex vivo autoradiography. The in vivo binding of IBZM seems to be selective to D2 dopamine receptors, since the binding was blocked by pretreatment of animals with D2 agonist LY-171555 or antagonist YM-09151-2. Furthermore, in vitro binding assays in striatal membranes confirmed that IBZM binding was highly selective to D2 sites. Thus, IBZM, when labeled with 123I (T1/2: 13h; 159 kev), could be a potential ligand for imaging D2 dopamine receptors by single photon emission computerized tomography procedures.

摘要

通过体外放射自显影法研究了[125I]3-碘苯甲酰胺（IBZM），一种取代苯甲酰胺，在体内与尾状核、伏隔核和嗅结节中多巴胺（DA）受体结合位点的结合情况。IBZM在体内的结合似乎对D2多巴胺受体具有选择性，因为用D2激动剂LY-171555或拮抗剂YM-09151-2预处理动物可阻断这种结合。此外，纹状体膜的体外结合试验证实，IBZM的结合对D2位点具有高度选择性。因此，当用123I（半衰期：13小时；159千电子伏特）标记时，IBZM可能是一种通过单光子发射计算机断层扫描程序对D2多巴胺受体进行成像的潜在配体。