Laboratoire de Radiotoxicologie, Commissariat a l'Energie Atomique, Ctr. d'Etudes de Bruyeres-le-Chatel, BP 12, F-91680 Bruyeres-le-Chatel, France
Service Hospitalier Frederic Joliot, Commissariat a l'Energie Atomique, Orsay, France.
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Carson, R. E., Breier, A., De Bartolomeis, A., Saunders, R. C., Su, T. P., Schmall, B., Der, M. G., Eckelman, W. C., Quantification of amphetamine-induced changes in [11C] raclopride binding with continuous infusion (1997) J Cereb Blood Flow Metab, 17, pp. 437-447
Dewey, S. L., Smith, G. S., Logan, J., Brodie, J., Yu, D. W., Ferrieri, R., King, P., Meller, E., Gabaergic inhibition of endogeneous dopamine release measured in vivo with 11C-raclopride and positron emission tomography (1992) Neuroscience, 12, pp. 3773-3780
Endres, C. J., Kolachana, B. S., Saunders, R. C., Su, T., Weinberger, D., Breier, A., Eckelman, W. C., Carson, R. E., Kinetic modeling of [11C] raclopride: Combined PET-microdialysis studies (1997) J Cereb Blood Flow Metab, 17, pp. 932-942
Fisher, R. E., Morris, E. D., Alpert, N., Fischman, A. J., In vivo imaging of neuromodulatory synaptic transmission using PET: A review of relevant neurophysiology (1995) Human Brain Mapping, 3, pp. 24-34
Garris, P. A., Wightman, R. M., Different kinetics govern dopaminergic transmission in amygdala, prefrontal cortex and striatum: An in vivo voltammetric study (1994) J Neurosci, 14, pp. 442-450
Huang, S. C., Barrio, J. R., Phelps, M. E., Neuroreceptor assay with positron emission tomography: Equilibrium versus dynamic approach (1986) J Cereb Blood Flow Metab, 6, pp. 515-521
Kawagoe, K. T., Garris, P. A., Wiedemann, D. J., Wightman, R. M., Regulation of transient dopamine concentration gradients in the microenvironment surrounding nerve terminals in the rat striatum (1992) Neuroscience, 51, pp. 55-64
Koepp, M. J., Gunn, R. N., Lawrence, A. D., Cunningham, V. J., Dagher, A., Jones, T., Brooks, D. J., Grasby, P. M., Evidence for striatal dopamine release during a video game (1998) Nature, 393, pp. 266-268
Millet, P. H., Delforge, J., Maugui re, F., Pappata, S., Cinotti, L., Frouin, V., Samson, Y., Syrota, A., Parametric images of benzodiazepine receptor concentration in human brain: Comparison with the distribution volume approach (1995) J Nucl Med, 36, pp. 1462-1471
Mintun, M. A., Raichle, M. E., Kilbourn, M. R., Wooten, G. F., Welch, M. J., A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography (1984) Ann Neurol, 15, pp. 217-227
Morris, E. D., Fisher, R. E., Alpert, N. M., Rauch, S. L., Fischman, A. J., In vivo imaging of neuromodulation using positron emission tomography: Optimal ligand characteristics and task length for detection of activation (1995) Hum Brain Mapp, 3, pp. 35-55
Price, J. C., Mason, N. S., Lopresti, B., Holt, D., Simpson, N. R., Drevets, W., Smith, G. S., Mathis, C. A., PET measurement of endogenous neurotransmitter activity using high and low affinity radiotracers (1998) Quantitative functional brain imaging with positron emission tomography, pp. 441-448. , (Carson RE, Daube-Witherspoon M, Herscovitch P, eds), San Diego: Academic Press
Ross, S. B., Jackson, D. M., Kinetic properties of the in vivo accumulation of 3H- (-) -N-n-propylnorapomorphine in mouse brain (1989) Naunyn Schmiedebergs Arch Pharmacol, 340, pp. 6-12
Ross, S. B., Synaptic concentration of dopamine in the mouse striatum in relationship to the kinetic properties of the dopamine receptors and uptake mechanism (1991) J Neurochem, 56, pp. 22-29
Swahn, C. -G., Halldin, C., Farde, L., Sedvall, G., Metabolism of the PET ligand [11C] SCH 23390. Identification of two radiolabeled metabolites with HPLC (1994) Human Psychopharmacology, 9, pp. 25-31
Volkow, N. D., Wang, G. -J., Fowler, J., Logan, J., Schlyer, D., Hitzemann, R., Lieberman, J., Wolf, A., Imaging endogenous dopamine competition with 11C raclopride in the human brain (1994) Synapse, 16, pp. 255-262
Volkow, N. D., Fowler, J. S., Gatley, S. J., Logan, J., Wang, G. W., Ding, Y. S., Dewey, S., PET evaluation of the dopamine system of the human brain (1996) J Nucl Med, 37, pp. 1242-1256
Absolute quantification by positron emission tomography of the endogenous ligand
The results of several recent papers have shown a significant influence of the endogenous neurotransmitters on the exogenous ligand kinetics measured by positron emission tomography. For example, several groups found that the percentage of D2 receptor sites occupied by the endogenous dopamine ranged from 25% to 40% at basal level. An obvious consequence of this significant occupancy is that the ligand-receptor model parameters, usually estimated by a model that does not take into account the endogenous ligand (EL) kinetics, can be significantly biased. In the current work, the authors studied the biases obtained by using the multiinjection approach. The results showed that in the classical ligand-receptor model, the receptor concentration is correctly estimated and that only the apparent affinity is biased by not taking the EL into account. At present, all absolute quantifications of the EL have been obtained through pharmacologic manipulation of the endogenous transmitter concentration, which is often too invasive a method to be used in patients. A theoretical reasoning showed that a noninvasive approach is necessarily based on both the apparent affinity measurement and on a multiregion approach. The correlation between the receptor concentration and the apparent affinity, previously observed with some ligands, verifies these two conditions; thus, the authors suggest that this correlation could be the result of the EL effect. To test this assumption experimentally, the effect of reserpine-induced dopamine depletion on the interactions between the D2 receptor sites and the FLB 457 is studied. With untreated baboons, the apparent FLB 457 affinity was smaller in the receptor-rich regions (striatum) than in the receptor-poor regions. This discrepancy disappeared after dopamine depletion, strongly suggesting that this affinity difference was related to the EL effect. Therefore, the purpose of the current study was to test the ability to quantify the EL based on the observed correlation between the receptor concentration and the apparent affinity. This approach offers a method for estimating the percentage of receptor sites occupied by the EL and, if its affinity is known, the free EL concentration. From the data obtained using FLB 457 with baboons, the authors found that approximately 53% of the D2 receptor sites are occupied by dopamine in the striatum and that the free dopamine concentration is approximately 120 nmol/L at basal level. This approach is transferable to patients, because the experimental data are obtained without pharmacologically induced modification of the EL.
Absolute quantification by positron emission tomography of the endogenous ligand
No results.
Absolute quantification by positron emission tomography of the endogenous ligand