A PET-study of [11C]FLB 457 binding to extrastriatal D2-dopamine receptors in healthy subjects and antipsychotic drug-treated patients
A PET-study of [11C]FLB 457 binding to extrastriatal D2-dopamine receptors in healthy subjects and antipsychotic drug-treated patients
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健康受试者和接受抗精神病药物治疗的患者中 [11C]FLB 457 与纹状体外 D2-多巴胺受体结合的 PET 研究
作者：
L. Farde;T. Suhara;S. Nyberg;P. Karlsson;Y. Nakashima;J. Hietala;C. Halldin
[11 C]FLB 457是一种取代苯甲酰胺，在体外对D2-多巴胺受体具有20 pM的亲和力。本探索性研究的目的是检查[11 C]FLB 457结合在人脑中的解剖分布，并确定抗精神病药物治疗患者的纹状体外D2受体占有率。[11 C]雷氯必利用于获得壳核中D2-多巴胺受体占有率的参考值。静脉注射[11 C]FLB 457后，不仅在尾壳核中，而且在丘脑和颞叶皮质中均存在高浓度放射性。额叶皮质、黑质和丘的放射性浓度略高于小脑。用氟哌啶醇和氟奋乃静预处理表明，[11 C]FLB 457在纹状体外区域的高度结合代表了与D2-多巴胺受体的特异性结合。抗精神病药物治疗患者的丘脑和颞叶皮质中的D2-占用率与[11 C]雷氯必利在壳核中测定的水平相同。该研究表明，[11 C]FLB 457具有对人体D2-多巴胺受体进行定量PET检查的潜力。
Abstract We recently developed [11C]FLB 457 a substituted benzamide with the very high affinity of 20 pM for D2-dopamine receptors in vitro. The aim of the present exploratory study was to examine the anatomical distribution of [11C]FLB 457 binding in the human brain and to determine extrastriatal D2-receptor occupancy in antipsychotic drug-treated patients. [11C]raclopride was used to obtain reference values for D2-dopamine receptor occupancy in the putamen. After IV injection of [11C]FLB 457 there was a high concentration of radioactivity, not only in the caudate putamen but also in the thalamus and the temporal cortex. The concentration of radioactivity in the frontal cortex, the substantia nigra and the colliculi was slightly higher than in the cerebellum. Pretreatment with haloperidol and fluphenazine indicated that [11C]FLB 457 binding in extrastriatal regions to a high degree represents specific binding to D2-dopamine receptors. The D2-occupancy in antipsychotic drug-treated patients was on the same level in the thalamus and the temporal cortex as that determined with [11C]raclopride in the putamen. The study shows that [11C]FLB 457 has potential for quantitative PET-examination of D2-dopamine receptors in man.
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影响因子：
--
作者：
L. Farde;A. Nordström;F. Wiesel;S. Pauli;C. Halldin;G. Sedvall
通讯作者：
L. Farde;A. Nordström;F. Wiesel;S. Pauli;C. Halldin;G. Sedvall
DOI：
10.1073/pnas.91.23.11271
发表时间：
1994-11-08
影响因子：
11.1
作者：
MURRAY, AM;RYOO, HL;JOYCE, JN
通讯作者：
JOYCE, JN
纹状体外多巴胺 D2 受体：氯氮平的分布、药理学特征和区域特异性调节。
DOI：
--
发表时间：
1992
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Janowsky,A;Neve,KA;Kinzie,JM;Taylor,B;dePaulis,T;Belknap,JK
通讯作者：
Belknap,JK
螺哌酮烷基化和非烷基化衍生物在大鼠脑中延长 D2 抗多巴胺能活性。
影响因子：
3.6
作者：
Baldessarini,RJ;Kula,NS;Campbell,A;Bakthavachalam,V;Yuan,J;Neumeyer,JL
通讯作者：
Neumeyer,JL