Graphical, Kinetic, and Equilibrium Analyses of in vivo [123I]β-CIT Binding to Dopamine Transporters in Healthy Human Subjects
Graphical, Kinetic, and Equilibrium Analyses of in vivo [123I]β-CIT Binding to Dopamine Transporters in Healthy Human Subjects
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健康人类受试者体内 [123I]β-CIT 与多巴胺转运蛋白结合的图形、动力学和平衡分析
DOI：
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发表时间：
1994
影响因子：
6.3
通讯作者：
R. Innis
中科院分区：
文献类型：
--
作者：
M. Laruelle;E. Wallace;J. Seibyl;R. Baldwin;Y. Zea‐Ponce;S. Zoghbi;J. Neumeyer;D. Charney;P. Hoffer;R. Innis
The in vivo kinetics of the dopamine (DA) transporter probe 123I-labeled 2β-carboxymethoxy-3β-(4-iodophenyl)tropane ([123I]β-CIT) in striatum was investigated with single-photon emission computerized tomography (SPECT) in five healthy human subjects. The aim of this study was to derive an adequate measure of the DA transporter density that would not be affected by regional cerebral blood flow or peripheral clearance of the tracer. SPECT data were acquired on the day of injection (day 1) from 0 to 7 h and on the following day (day 2) from 19 to 25 h. Arterial sampling on day 1 was used to measure the input function. Graphical, kinetic, and equilibrium analyses were evaluated. Graphical analysis of day 1 data, with the assumption of negligible dissociation of the tracer–receptor complex (k4 = 0), was found to be blood flow-dependent. A three-compartment kinetic analysis of day 1 data were performed using a three (k4 = 0)- and a four (k4 > 0)-parameter model. The three-parameter model estimated the konBmax product at 0.886 ± 0.087 min−1. The four-parameter model gave a binding potential (BP) of 476 ml g−1, a value consistent with in vitro measurements. The stability of the regional uptake on day 2 allowed direct measurement of the specific to nonspecific equilibrium partition coefficient (V3″ = k3/k4 = 6.66 ± 1.54). Results of day 1 kinetic analysis and day 2 equilibrium analysis were well correlated among subjects. Simulations indicated that the error associated with the day 2 equilibrium analysis was acceptable for plasma tracer terminal half-lives >10 h. We propose the equilibrium analysis on day 2 as the method of choice for clinical studies since it does not require multiple scans or the measurement of the arterial plasma tracer concentrations.
可卡因和相关药物对非人类灵长类动物的影响。
DOI：
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发表时间：
1989
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Madras,BK;Fahey,MA;Bergman,J;Canfield,DR;Spealman,RD
通讯作者：
Spealman,RD
由 [3H]2 β-甲甲氧基-3 β-(4-氟苯基)托烷标记的可卡因受体。
影响因子：
3.6
作者：
Madras,BK;Spealman,RD;Fahey,MA;Neumeyer,JL;Saha,JK;Milius,RA
通讯作者：
Milius,RA
[123I]-2 beta-甲甲氧基-3 beta-(4-碘苯基)托烷：大脑中单胺再摄取位点的高亲和力 SPECT 放射性示踪剂。
影响因子：
7.3
作者：
Neumeyer,JL;Wang,SY;Milius,RA;Baldwin,RM;Zea-Ponce,Y;Hoffer,PB;Sybirska,E;al-Tikriti,M;Charney,DS;Malison,RT
通讯作者：
Malison,RT