Serial [18F]N-methylspiroperidol PET studies to measure changes in antipsychotic drug D-2 receptor occupancy in schizophrenic patients

Smith, Michael; Wolf, Alfred P.; Brodie, Jonathan D.; Arnett, Carroll D.; Barouche, Faouzia; Shiue, Chyng‐Yann; Fowler, Joanna S.; Russell, Jerome A. G.; MacGregor, Robert; Wolkin, Adam; Angrist, Burt; Rotrosen, John; Peselow, Eric D.

doi:10.1016/0006-3223(88)90048-0

Cited by 134 publications

(28 citation statements)

References 22 publications

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“…This effect can be attributed to the action of benzodiazepines reducing monoamine catabolism (Siegel et al, 1981) and thus the number of free dopamine receptors. Therefore, a possible application of spiperone binding studies is the quantitative measurement of D 2 receptor blocking during and following neuroleptic treatment (Farde et al, 1987b;Smith et al, 1988). For this purpose, it may be sufficient to restrict the measurement to one of those parameters which do not require blood sampling with correction for metabolites, e.g., the caudate-to-cerebellum ratio or the total accumulated activity relative to the injected dose.…”

Section: Discussionmentioning

confidence: 98%

PET studies of dopamine receptor distribution using [18F]fluoroethylspiperone: findings in disorders related to the dopaminergic system

Wienhard¹,

Coenen

Pawlik³

et al. 1990

J. Neural Transmission

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PET studies of dopamine D2-receptor binding were performed in thirty patients with various disorders related to the dopaminergic system and in six healthy controls. Uptake of [18F]fluoroethylspiperone in caudate over three hours was analyzed in terms of several indices of receptor binding:caudate-to-cerebellum activity ratio, concentration of ligand as percentage of injected dose, caudate-to-blood radioactivity ratio, slope of tracer uptake curves, binding potential, kinetic constants of a three compartment model. In 14 patients brain glucose metabolism was also measured. Data on medicated patients demonstrate that the average values of most of the above parameters indicate the decreased number of available D2-receptors whereby, besides an age dependent decline, the caudate-to-cerebellum ratio affords the relatively best distinction among diagnostic groups. In individual cases, large variability among subjects permits only the classification of severe pathologies. Morphological damage and neuronal loss in the striatum may also cause abnormal low values both for the indices of receptor binding and for glucose consumption, thus providing a possible pathogenetic link between receptor dysfunction and impaired energy metabolism.

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Section: Discussionmentioning

confidence: 98%

PET studies of dopamine receptor distribution using [18F]fluoroethylspiperone: findings in disorders related to the dopaminergic system

Wienhard¹,

Coenen

Pawlik³

et al. 1990

J. Neural Transmission

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“…Positron emission tomography (PET) and radiolabelled ligands are now used by several centres to determine central DZdopamine receptor occupancy in neuroleptic drug-treated schizophrenic patients (Farde et al, 1985Maziere et al, 1985;Smith et al, 1988). Of clinical importance is the potential of this technique to examine relationships between drug-induced central receptor occupancy and pharmacological effects in patients.…”

Section: Discussionmentioning

confidence: 98%

“…The ratio of radioactivity in the striatum to that in the cerebellum is widely used as an index for specific receptor binding and for quantification of the central dopamine receptor occupancy induced by neuroleptic drugs (Farde et al, 1985Marzikre et al, 1985;Smith et al, 1988). So far, no study has been reported regarding the reliability of such ratios.…”

Section: Introductionmentioning

confidence: 97%

PET analysis of central [¹¹ C]raclopride binding in healthy young adults and schizophrenic patients—reliability and age effects

Nordström

Farde

Pauli

et al. 1992

Human Psychopharmacology

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Central D2-dopamine receptor occupancy determined by positron emission tomography (PET) during neuroleptic drug treatment may be a useful measure for optimal dose finding in schizophrenic patients. The clinical benefit is dependent on the reliability of such determinations. The ratio of radioactivity in the striatum to that of the cerebellum 1s widely used for calculation of D2-receptor occupancy and as an index of D2-dopamine receptor density. To test the reliability of such ratios a test-retest analysis was performed in a series of healthy subjects.The reliability was very high, both when experiments were repeated on the same day and after time intervals of months to years. A group of subjects were examined twice using PET camera systems with different resolution.The strialuni to cerebellum ratios obtained from the high-resolution PET camera system were significantly higher than ratios from the camera with lower resolution. The age effect on the striatum to cerebellum ratio was examined in 25 healthy young adults and in 18 neuroleptic-naive schizophrenic patients. A statistically significant decline was found both in the healthy controls and in the schizophrenic patients. The results do not support the view that there is a lack of age effect on the D2-dopamine receptor density in schizophrenia.

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“…Potential effective therapeutic doses of a given drug may be determined based on its in vivo D 2 receptor occupancy (Smith et al 1988;Farde et al 1988;Bench et al 1993;Kapur et al 1996;Hirschowitz et al 1997). In this, positron emission tomography (PET) study, we used [ 11 C]raclopride ([ 11 C]RAC) to measure the D 2 receptor occupancy of aripiprazole in the corpus striatum in fifteen normal male control subjects.…”

mentioning

confidence: 99%

Dopamine D2 and D3 Receptor Occupancy in Normal Humans Treated with the Antipsychotic Drug Aripiprazole (OPC 14597) A Study Using Positron Emission Tomography and [11C]Raclopride

Yokoi

2002

Neuropsychopharmacology

279

147

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Serial [18F]N-methylspiroperidol PET studies to measure changes in antipsychotic drug D-2 receptor occupancy in schizophrenic patients

Cited by 134 publications

References 22 publications

PET studies of dopamine receptor distribution using [18F]fluoroethylspiperone: findings in disorders related to the dopaminergic system

PET studies of dopamine receptor distribution using [18F]fluoroethylspiperone: findings in disorders related to the dopaminergic system

PET analysis of central [¹¹ C]raclopride binding in healthy young adults and schizophrenic patients—reliability and age effects

Dopamine D2 and D3 Receptor Occupancy in Normal Humans Treated with the Antipsychotic Drug Aripiprazole (OPC 14597) A Study Using Positron Emission Tomography and [11C]Raclopride

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Serial [18F]N-methylspiroperidol PET studies to measure changes in antipsychotic drug D-2 receptor occupancy in schizophrenic patients

Cited by 134 publications

References 22 publications

PET studies of dopamine receptor distribution using [18F]fluoroethylspiperone: findings in disorders related to the dopaminergic system

PET studies of dopamine receptor distribution using [18F]fluoroethylspiperone: findings in disorders related to the dopaminergic system

PET analysis of central [11 C]raclopride binding in healthy young adults and schizophrenic patients—reliability and age effects

Dopamine D2 and D3 Receptor Occupancy in Normal Humans Treated with the Antipsychotic Drug Aripiprazole (OPC 14597) A Study Using Positron Emission Tomography and [11C]Raclopride

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PET analysis of central [¹¹ C]raclopride binding in healthy young adults and schizophrenic patients—reliability and age effects