Measurement of Methylphenidate-Induced Change in Extrastriatal Dopamine Concentration using [11C]FLB 457 PET
Measurement of Methylphenidate-Induced Change in Extrastriatal Dopamine Concentration using [11C]FLB 457 PET
复制标题
使用 [11C]FLB 457 PET 测量哌甲酯引起的纹状体外多巴胺浓度变化
DOI：
--
复制
发表时间：
2007
影响因子：
6.3
通讯作者：
P. Grasby
中科院分区：
文献类型：
--
作者：
A. Montgomery;M. Asselin;L. Farde;P. Grasby
[11 C]FLB 457是一种非常高亲和力的放射性示踪剂，可以测量密度非常低的大脑区域（如大脑皮层）中多巴胺D2/3受体的可用性。尚不清楚[11 C]FLB 457结合是否对人体内源性多巴胺浓度敏感，其方式与纹状体中的[11 C]雷氯必利和[123 I]IBZM类似。为了测试这种可能性，在基线和口服40至60 mg精神兴奋剂哌甲酯（MP）后，在12名健康志愿者中使用正电子发射断层扫描（PET）以平衡顺序，双盲设计测量纹状体外[11 C]FLB 457结合。使用具有代谢物校正动脉血浆输入函数的两组织室模型对动态PET数据进行量化。两名志愿者因头部过度运动而被排除。在其余部分中，MP导致颞叶和额叶皮质区和丘脑的分布容积（VD）显著降低，表明[11 C]FLB 457结合对内源性多巴胺浓度敏感。此外，在评估的所有区域中，MP给药后[11 C]FLB 457结合率的变化与MP剂量（mg/kg体重）相关。我们的结论是，在治疗注意缺陷多动障碍的治疗范围内的剂量的MP引起纹状体外区域的多巴胺浓度增加，[11 C]FLB 457 PET可能是一个有用的工具，用于评估人类这些区域的多巴胺浓度变化。
[11C]FLB 457 is a very high-affinity radiotracer that allows the measurement of dopamine D2/3 receptor availability in regions of the brain where densities are very low, such as the cerebral cortex. It is not known if [11C]FLB 457 binding is sensitive to the concentration of endogenous dopamine in humans in a manner analogous to [11C]raclopride and [123I]IBZM in the striatum. To test this possibility, extrastriatal [11C]FLB 457 binding was measured at baseline and after the oral administration of 40 to 60 mg of the psychostimulant methylphenidate (MP) in 12 healthy volunteers using positron emission tomography (PET) in a balanced-order, double-blind design. The dynamic PET data were quantified using a two-tissue compartment model with a metabolite-corrected arterial plasma input function. Two volunteers were excluded because of excessive head movement. In the remainder, MP caused significant reductions in the volume of distribution (VD) in temporal and frontal cortical regions and thalamus, suggesting that [11C]FLB 457 binding is sensitive to endogenous dopamine concentration. Moreover, the change in [11C]FLB 457 binding after MP correlated with the dose of MP (in mg/kg body weight) in all regions assessed. We conclude that MP in doses within the therapeutic range for the treatment of attention deficit hyperactivity disorder causes increases in dopamine concentrations in extrastriatal regions and that [11C]FLB 457 PET may be a useful tool for the assessment of change in dopamine concentration in these areas in humans.
登录
查看更多内容
DOI：
--
发表时间：
2000-12
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Gregg D. Stanwood;Roman Artymyshyn;M. Kung;H. Kung;I. Lucki;P. Mcgonigle
通讯作者：
Gregg D. Stanwood;Roman Artymyshyn;M. Kung;H. Kung;I. Lucki;P. Mcgonigle
大鼠皮质中多巴胺转运蛋白的细胞和亚细胞定位。
DOI：
10.1016/s1054-3589(08)60720-6
发表时间：
1998
期刊：
Advances in pharmacology (San Diego, Calif.)
影响因子：
--
作者：
Sesack,SR;Hawrylak,VA;Guido,MA;Levey,AI
通讯作者：
Levey,AI
DOI：
10.1073/pnas.93.17.9235
发表时间：
1996-08-20
影响因子：
11.1
作者：
Laruelle, M;Abi-Dargham, A;Innis, RB
通讯作者：
Innis, RB
哌醋甲酯在人、大鼠和猴体内的药代动力学。
DOI：
--
发表时间：
1983
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Wargin,W;Patrick,K;Kilts,C;Gualtieri,CT;Ellington,K;Mueller,RA;Kraemer,G;Breese,GR
通讯作者：
Breese,GR
影响因子：
6.1
作者：
Wang,GJ;Volkow,ND;Fowler,JS;Ferrieri,R;Schlyer,DJ;Alexoff,D;Pappas,N;Lieberman,J;King,P;Warner,D
通讯作者：
Warner,D