Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N- [(1-ethyl-2-pyrrolidinyl)methyl]benzamide.
Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N- [(1-ethyl-2-pyrrolidinyl)methyl]benzamide.
复制标题
多巴胺 D-2 受体成像放射性药物：(R)-( )- 和 (S)-(-)-3-碘-2-羟基-6-甲氧基-N- 的合成、放射性标记和体外结合 [(1
DOI：
10.1021/jm00400a027
复制
发表时间：
1988
影响因子：
7.3
通讯作者：
Guo,YZ
中科院分区：
文献类型：
--
作者：
Kung,HF;Kasliwal,R;Pan,SG;Kung,MP;Mach,RH;Guo,YZ
在开发中枢神经系统多巴胺D-2受体显像剂的过程中，合成了3-[125345 I]碘-2-羟基-6-甲氧基-N-[（1-乙基-2-吡咯烷基）甲基]苯甲酰胺（[125 I] IBZM）的R-（+）和S-（-）对映体，并在大鼠纹状体组织标本中评价了它们的体外结合特性。（S）-（-）-[12 T] IBZM显示高特异性多巴胺D-2受体结合（= 0.43 nM，Bmax= 0.48 pmol/mg蛋白）。各种配体对IBZM结合的竞争数据显示以下效力等级顺序：螺哌隆>（S）-（-）-IBZM>（+）-丁他拉莫>（S）-（+）-IBZM>（S）-（-）-BZM>多巴胺>酮色林> SCH 23390>心得安。结果表明，[125 I] IBZM与多巴胺D-2受体特异性结合，具有立体特异性。[123 I] IBZM可能用作研究人类多巴胺D-2受体的成像剂。
In developing central nervous system (CNS) dopamine D-2 receptor imaging agents, enantiomers, R-(+) and S-(-) isomers, of 3-[125 345I] iodo-2-hydroxy-6-methoxy-JV-[(l-ethyl-2-pyrrolidinyl) methyl] benzamide,[125I] IBZM, were syn-thesized, and their in vitro binding characteristics were evaluated in rat striatum tissue preparation. The (S)-(-)-[12T] IBZM showed high specific dopamine D-2 receptorbinding (= 0.43 nM, Bmax= 0.48 pmol/mg of protein). Competition data of various ligands for IBZM binding displayed the following rank order of potency: spiperone>(S)-(-)-IBZM>(+)-butaclamol»(fi)-(+)-IBZM>(S)-(-)-BZM> dopamine> ketanserin> SCH23390» propanolol. The results indicate that [125I] IBZM binds specifically to the dopamine D-2 receptor with stereospecificity. The [123I] IBZM is potentially useful as an imaging agent for the investigation of dopamine D-2 receptors in humans.