PET measurements of neuroreceptor occupancy by typical and atypical neuroleptics

Peter F. Goyer; Marc S. Berridge; Evan D. Morris; William E. Semple; Beth A. Compton-Toth; S. Charles Schulz; Dean F. Wong; Flora Miraldi; Herbert Y. Meltzer

PET measurements of neuroreceptor occupancy by typical and atypical neuroleptics

Peter F. Goyer, Marc S. Berridge, Evan D. Morris, William E. Semple, Beth A. Compton-Toth, S. Charles Schulz, Dean F. Wong, Flora Miraldi, Herbert Y. Meltzer

School of Medicine

Research output: Contribution to journal › Article › peer-review

37 Scopus citations

Abstract

The goal of this study was to use PET and ¹¹C-N-methylspiperone (¹¹C-NMSP) to measure the differences in relative occupancy of serotonin (5-hydroxytryptamine-2 or 5-HT(2A) and dopamine-2 (D2) neuroreceptors in subjects being treated with typical or atypical antipsychotic drugs. Methods: We used PET and single-dose ¹¹C-NMSP to measure receptor indices and relative receptor occupancy of 5-HT(2A) receptors in frontal cortex and D2 receptors in basal ganglia in five subjects who were neuroleptic free, five subjects who were being treated with typical antipsychotic drugs and five subjects who were being treated with clozapine, an atypical antipsychotic drug. Results: Among the three groups, there were significant differences in 5-HT(2A) indices, D2 indices and the ratio of 5-HT(2A) to D2 indices. With no overlap, the 5-HT(2A) index separated all subjects who received clozapine and the D2 index separated the remaining two groups. Conclusion: Typical antipsychotic and atypical antipsychotic subjects do have differing patterns of 5-HT(2A) and D2 relative receptor occupancy when measured with a single PET scan, single ¹¹C-NMSP radiotracer dose and no separately injected 'cold' pharmaceutical.

Original language	English (US)
Pages (from-to)	1122-1127
Number of pages	6
Journal	Journal of Nuclear Medicine
Volume	37
Issue number	7
State	Published - Jul 1996

Keywords

PET
carbon-11-N-methylspiperone
neuroreceptor occupancy

ASJC Scopus subject areas

Radiology Nuclear Medicine and imaging

Cite this

@article{46d434975e1c41f0ae417da74d624a27,

title = "PET measurements of neuroreceptor occupancy by typical and atypical neuroleptics",

abstract = "The goal of this study was to use PET and 11C-N-methylspiperone (11C-NMSP) to measure the differences in relative occupancy of serotonin (5-hydroxytryptamine-2 or 5-HT(2A) and dopamine-2 (D2) neuroreceptors in subjects being treated with typical or atypical antipsychotic drugs. Methods: We used PET and single-dose 11C-NMSP to measure receptor indices and relative receptor occupancy of 5-HT(2A) receptors in frontal cortex and D2 receptors in basal ganglia in five subjects who were neuroleptic free, five subjects who were being treated with typical antipsychotic drugs and five subjects who were being treated with clozapine, an atypical antipsychotic drug. Results: Among the three groups, there were significant differences in 5-HT(2A) indices, D2 indices and the ratio of 5-HT(2A) to D2 indices. With no overlap, the 5-HT(2A) index separated all subjects who received clozapine and the D2 index separated the remaining two groups. Conclusion: Typical antipsychotic and atypical antipsychotic subjects do have differing patterns of 5-HT(2A) and D2 relative receptor occupancy when measured with a single PET scan, single 11C-NMSP radiotracer dose and no separately injected 'cold' pharmaceutical.",

keywords = "PET, carbon-11-N-methylspiperone, neuroreceptor occupancy",

author = "Goyer, {Peter F.} and Berridge, {Marc S.} and Morris, {Evan D.} and Semple, {William E.} and Compton-Toth, {Beth A.} and Schulz, {S. Charles} and Wong, {Dean F.} and Flora Miraldi and Meltzer, {Herbert Y.}",

year = "1996",

month = jul,

language = "English (US)",

volume = "37",

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publisher = "Society of Nuclear Medicine Inc.",

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T1 - PET measurements of neuroreceptor occupancy by typical and atypical neuroleptics

AU - Goyer, Peter F.

AU - Berridge, Marc S.

AU - Morris, Evan D.

AU - Semple, William E.

AU - Compton-Toth, Beth A.

AU - Schulz, S. Charles

AU - Wong, Dean F.

AU - Miraldi, Flora

AU - Meltzer, Herbert Y.

PY - 1996/7

Y1 - 1996/7

N2 - The goal of this study was to use PET and 11C-N-methylspiperone (11C-NMSP) to measure the differences in relative occupancy of serotonin (5-hydroxytryptamine-2 or 5-HT(2A) and dopamine-2 (D2) neuroreceptors in subjects being treated with typical or atypical antipsychotic drugs. Methods: We used PET and single-dose 11C-NMSP to measure receptor indices and relative receptor occupancy of 5-HT(2A) receptors in frontal cortex and D2 receptors in basal ganglia in five subjects who were neuroleptic free, five subjects who were being treated with typical antipsychotic drugs and five subjects who were being treated with clozapine, an atypical antipsychotic drug. Results: Among the three groups, there were significant differences in 5-HT(2A) indices, D2 indices and the ratio of 5-HT(2A) to D2 indices. With no overlap, the 5-HT(2A) index separated all subjects who received clozapine and the D2 index separated the remaining two groups. Conclusion: Typical antipsychotic and atypical antipsychotic subjects do have differing patterns of 5-HT(2A) and D2 relative receptor occupancy when measured with a single PET scan, single 11C-NMSP radiotracer dose and no separately injected 'cold' pharmaceutical.

AB - The goal of this study was to use PET and 11C-N-methylspiperone (11C-NMSP) to measure the differences in relative occupancy of serotonin (5-hydroxytryptamine-2 or 5-HT(2A) and dopamine-2 (D2) neuroreceptors in subjects being treated with typical or atypical antipsychotic drugs. Methods: We used PET and single-dose 11C-NMSP to measure receptor indices and relative receptor occupancy of 5-HT(2A) receptors in frontal cortex and D2 receptors in basal ganglia in five subjects who were neuroleptic free, five subjects who were being treated with typical antipsychotic drugs and five subjects who were being treated with clozapine, an atypical antipsychotic drug. Results: Among the three groups, there were significant differences in 5-HT(2A) indices, D2 indices and the ratio of 5-HT(2A) to D2 indices. With no overlap, the 5-HT(2A) index separated all subjects who received clozapine and the D2 index separated the remaining two groups. Conclusion: Typical antipsychotic and atypical antipsychotic subjects do have differing patterns of 5-HT(2A) and D2 relative receptor occupancy when measured with a single PET scan, single 11C-NMSP radiotracer dose and no separately injected 'cold' pharmaceutical.

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PET measurements of neuroreceptor occupancy by typical and atypical neuroleptics

Abstract

Keywords

ASJC Scopus subject areas

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