Lammertsma A A, Bench C J, Price G W, Cremer J E, Luthra S K, Turton D, Wood N D, Frackowiak R S
MRC Cyclotron Unit, Hammersmith Hospital, London, U.K.
J Cereb Blood Flow Metab. 1991 Jul;11(4):545-56. doi: 10.1038/jcbfm.1991.103.
A tracer kinetic procedure was developed for the measurement of monoamine oxidase type B (MAO-B) activity using L-[11C]deprenyl and positron emission tomography (PET). The kinetic model consisted of two tissue compartments with irreversible binding to the second compartment (three rate constants). In addition, a blood volume component was included. Special attention was given to the accurate measurement of the plasma and whole blood input functions. The method was applied to the measurement of the dose-response curve of a reversible MAO-B inhibitor (Ro 19-6327). From the results, it followed that the rate constant for irreversible binding (k3) appeared to be a better index of MAO-B activity than the net influx constant Ki. Furthermore, regional analysis demonstrated that Ki, but not k3, was flow dependent. This implies that full kinetic analysis is required for an accurate assessment of MAO-B activity.
开发了一种示踪动力学方法,使用L-[11C]司来吉兰和正电子发射断层扫描(PET)测量单胺氧化酶B型(MAO-B)活性。动力学模型由两个组织隔室组成,与第二个隔室存在不可逆结合(三个速率常数)。此外,还纳入了血容量成分。特别关注血浆和全血输入函数的准确测量。该方法应用于可逆性MAO-B抑制剂(Ro 19-6327)剂量反应曲线的测量。从结果来看,不可逆结合的速率常数(k3)似乎比净流入常数Ki更能作为MAO-B活性的指标。此外,区域分析表明,Ki而非k3与血流有关。这意味着需要进行完整的动力学分析才能准确评估MAO-B活性。