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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...

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Autores principales: Ito, Hiroshi, Takano, Harumasa, Arakawa, Ryosuke, Takahashi, Hidehiko, Kodaka, Fumitoshi, Takahata, Keisuke, Nogami, Tsuyoshi, Suzuki, Masayuki, Suhara, Tetsuya
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2012
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.
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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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