Measurement of binding potential of [C11]WIN 35,428 for dopamine re-uptake site in normal human brain: Comparison of graphical and non-linear least-squares analytic method
- Johns Hopkins Medical Institutions, Baltimore, MD (United States); and others
(C11)WIN 35,428 was evaluated as a specific radioligand for the dopamine re-uptake site in brain by PET scanning. Twenty mCi of [C11]WIN 35,428 was administered IV to 8 normal volunteers (19-81 y.o.). Fifty dynamic PET scan images were acquired with blood sampling, for 90 min after [C11]WIN 35,428 injection. Four different kinetic modeling procedures were used to estimate the binding potential, k3/k4. The k3 and k4 parameters reflect the rate constants for binding to and dissociation from receptors, respectively. The first model is a three-compartment model which is a standard non-linear least-squares analysis with constraint of the k1/k2 ratio. This consists of a plasma, ligand free and a specifically bound compartment. The k1/k2 ratio was estimated with a two-compartment model using plasma and cerebellar data. The other three models are two-compartment models. This consists of a plasma and a brain (cerebellum or striatum) compartment. The second model is a two-compartment graphical method of Gjedde. The distribution volume of [C11]WIN in striatum and cerebellum was plotted as an intercept. The third model approach is the graphical method of Logan, which was a modification of the Gjedde approach. The distribution volume of [C11]WIN in striatum and cerebellum was plotted as a slope. The fourth model consisted of a direct fit a f cerebellum and striatum without plasma input. The mean value and standard deviation of k3/k4 in each model was 4.38 {plus_minus} 0.81, 3.93 {plus_minus} 0.98, 4.15 {plus_minus} 0.83, and 6.90 {plus_minus} 2.19, respectively. There is a significant difference between k3/k4 values of the constraint method and that of the last method. There is no significant difference between the k3/k4 values of the constraint method and the other two methods.
- OSTI ID:
- 198043
- Report Number(s):
- CONF-940605-; ISSN 0161-5505; CNN: Grant MH 42821; Grant NS 15080; TRN: 95:007029-0186
- Journal Information:
- Journal of Nuclear Medicine, Vol. 35, Issue Suppl.5; Conference: 41. annual meeting of the Society of Nuclear Medicine, Orlando, FL (United States), 5-8 Jun 1994; Other Information: PBD: May 1994
- Country of Publication:
- United States
- Language:
- English
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