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Effects of Dopamine D(2) Receptor Partial Agonist Antipsychotic Aripiprazole on Dopamine Synthesis in Human Brain Measured by PET with L-[β-(11)C]DOPA
Dopamine D(2) receptor partial agonist antipsychotic drugs can modulate dopaminergic neurotransmission as functional agonists or functional antagonists. The effects of antipsychotics on presynaptic dopaminergic functions, such as dopamine synthesis capacity, might also be related to their therapeuti...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2012
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3460902/ https://www.ncbi.nlm.nih.gov/pubmed/23029533 http://dx.doi.org/10.1371/journal.pone.0046488 |
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author | Ito, Hiroshi Takano, Harumasa Arakawa, Ryosuke Takahashi, Hidehiko Kodaka, Fumitoshi Takahata, Keisuke Nogami, Tsuyoshi Suzuki, Masayuki Suhara, Tetsuya |
author_facet | Ito, Hiroshi Takano, Harumasa Arakawa, Ryosuke Takahashi, Hidehiko Kodaka, Fumitoshi Takahata, Keisuke Nogami, Tsuyoshi Suzuki, Masayuki Suhara, Tetsuya |
author_sort | Ito, Hiroshi |
collection | PubMed |
description | Dopamine D(2) receptor partial agonist antipsychotic drugs can modulate dopaminergic neurotransmission as functional agonists or functional antagonists. The effects of antipsychotics on presynaptic dopaminergic functions, such as dopamine synthesis capacity, might also be related to their therapeutic efficacy. Positron emission tomography (PET) was used to examine the effects of the partial agonist antipsychotic drug aripiprazole on presynaptic dopamine synthesis in relation to dopamine D(2) receptor occupancy and the resulting changes in dopamine synthesis capacity in healthy men. On separate days, PET studies with [(11)C]raclopride and L-[β-(11)C]DOPA were performed under resting condition and with single doses of aripiprazole given orally. Occupancy of dopamine D(2) receptors corresponded to the doses of aripiprazole, but the changes in dopamine synthesis capacity were not significant, nor was the relation between dopamine D(2) receptor occupancy and these changes. A significant negative correlation was observed between baseline dopamine synthesis capacity and changes in dopamine synthesis capacity by aripiprazole, indicating that this antipsychotic appears to stabilize dopamine synthesis capacity. The therapeutic effects of aripiprazole in schizophrenia might be related to such stabilizing effects on dopaminergic neurotransmission responsivity. |
format | Online Article Text |
id | pubmed-3460902 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2012 |
publisher | Public Library of Science |
record_format | MEDLINE/PubMed |
spelling | pubmed-34609022012-10-01 Effects of Dopamine D(2) Receptor Partial Agonist Antipsychotic Aripiprazole on Dopamine Synthesis in Human Brain Measured by PET with L-[β-(11)C]DOPA Ito, Hiroshi Takano, Harumasa Arakawa, Ryosuke Takahashi, Hidehiko Kodaka, Fumitoshi Takahata, Keisuke Nogami, Tsuyoshi Suzuki, Masayuki Suhara, Tetsuya PLoS One Research Article Dopamine D(2) receptor partial agonist antipsychotic drugs can modulate dopaminergic neurotransmission as functional agonists or functional antagonists. The effects of antipsychotics on presynaptic dopaminergic functions, such as dopamine synthesis capacity, might also be related to their therapeutic efficacy. Positron emission tomography (PET) was used to examine the effects of the partial agonist antipsychotic drug aripiprazole on presynaptic dopamine synthesis in relation to dopamine D(2) receptor occupancy and the resulting changes in dopamine synthesis capacity in healthy men. On separate days, PET studies with [(11)C]raclopride and L-[β-(11)C]DOPA were performed under resting condition and with single doses of aripiprazole given orally. Occupancy of dopamine D(2) receptors corresponded to the doses of aripiprazole, but the changes in dopamine synthesis capacity were not significant, nor was the relation between dopamine D(2) receptor occupancy and these changes. A significant negative correlation was observed between baseline dopamine synthesis capacity and changes in dopamine synthesis capacity by aripiprazole, indicating that this antipsychotic appears to stabilize dopamine synthesis capacity. The therapeutic effects of aripiprazole in schizophrenia might be related to such stabilizing effects on dopaminergic neurotransmission responsivity. Public Library of Science 2012-09-28 /pmc/articles/PMC3460902/ /pubmed/23029533 http://dx.doi.org/10.1371/journal.pone.0046488 Text en © 2012 Ito et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited. |
spellingShingle | Research Article Ito, Hiroshi Takano, Harumasa Arakawa, Ryosuke Takahashi, Hidehiko Kodaka, Fumitoshi Takahata, Keisuke Nogami, Tsuyoshi Suzuki, Masayuki Suhara, Tetsuya Effects of Dopamine D(2) Receptor Partial Agonist Antipsychotic Aripiprazole on Dopamine Synthesis in Human Brain Measured by PET with L-[β-(11)C]DOPA |
title | Effects of Dopamine D(2) Receptor Partial Agonist Antipsychotic Aripiprazole on Dopamine Synthesis in Human Brain Measured by PET with L-[β-(11)C]DOPA |
title_full | Effects of Dopamine D(2) Receptor Partial Agonist Antipsychotic Aripiprazole on Dopamine Synthesis in Human Brain Measured by PET with L-[β-(11)C]DOPA |
title_fullStr | Effects of Dopamine D(2) Receptor Partial Agonist Antipsychotic Aripiprazole on Dopamine Synthesis in Human Brain Measured by PET with L-[β-(11)C]DOPA |
title_full_unstemmed | Effects of Dopamine D(2) Receptor Partial Agonist Antipsychotic Aripiprazole on Dopamine Synthesis in Human Brain Measured by PET with L-[β-(11)C]DOPA |
title_short | Effects of Dopamine D(2) Receptor Partial Agonist Antipsychotic Aripiprazole on Dopamine Synthesis in Human Brain Measured by PET with L-[β-(11)C]DOPA |
title_sort | effects of dopamine d(2) receptor partial agonist antipsychotic aripiprazole on dopamine synthesis in human brain measured by pet with l-[β-(11)c]dopa |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3460902/ https://www.ncbi.nlm.nih.gov/pubmed/23029533 http://dx.doi.org/10.1371/journal.pone.0046488 |
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