The role of agonistic/antagonistic activity in the development of psychotropic effects of antipsychotics
The development of psychotic symptoms is traditionally linked to the increase of the functional activity of endogenous dopaminergic system. Antipsychotic effect of existing medications is associated with direct blockade of postsynaptic dopamine receptors. However, direct antagonistic activity is «al...
| Main Authors: | , , |
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| Format: | Article |
| Language: | Russian |
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Federal State Budget Scientific Institution National Medical Research Center for Psychiatry and Neurology n.a. V.M. Bekhterev Ministry of Health of the Russian Federation
2019-05-01
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| Series: | Обозрение психиатрии и медицинской психологии имени В.М. Бехтерева |
| Subjects: | |
| Online Access: | https://www.bekhterevreview.com/jour/article/view/227 |
| _version_ | 1826573146195492864 |
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| author | V. I. Kozlovskiy D. N. Kosterin M. Yu. Popov |
| author_facet | V. I. Kozlovskiy D. N. Kosterin M. Yu. Popov |
| author_sort | V. I. Kozlovskiy |
| collection | DOAJ |
| description | The development of psychotic symptoms is traditionally linked to the increase of the functional activity of endogenous dopaminergic system. Antipsychotic effect of existing medications is associated with direct blockade of postsynaptic dopamine receptors. However, direct antagonistic activity is «alien» to physiological mechanisms of neurotransmission modulation, and presynaptic autoreceptor blockade mау produce a reverse (agonistic) effect, enhancing neurotransmitter release. On the other hand, anti-dopamine effect can be achieved by indirect antagonistic activity—by presynaptic dopamine depletion, which is consistent with the natural, physiological mechanisms of reducing neurotransmission. It can be assumed that modulation of presynaptic regulation is one of the promising directions for the development of antipsychotic drugs of future generations. |
| first_indexed | 2024-03-12T03:01:39Z |
| format | Article |
| id | doaj.art-f3747441b307495189adcc7827a6f86d |
| institution | Directory Open Access Journal |
| issn | 2313-7053 2713-055X |
| language | Russian |
| last_indexed | 2025-03-14T12:38:16Z |
| publishDate | 2019-05-01 |
| publisher | Federal State Budget Scientific Institution National Medical Research Center for Psychiatry and Neurology n.a. V.M. Bekhterev Ministry of Health of the Russian Federation |
| record_format | Article |
| series | Обозрение психиатрии и медицинской психологии имени В.М. Бехтерева |
| spelling | doaj.art-f3747441b307495189adcc7827a6f86d2025-03-02T09:12:44ZrusFederal State Budget Scientific Institution National Medical Research Center for Psychiatry and Neurology n.a. V.M. Bekhterev Ministry of Health of the Russian FederationОбозрение психиатрии и медицинской психологии имени В.М. Бехтерева2313-70532713-055X2019-05-01013710.31363/2313-7053-2019-1-3-7224The role of agonistic/antagonistic activity in the development of psychotropic effects of antipsychoticsV. I. Kozlovskiy0D. N. Kosterin1M. Yu. Popov2V.M. Bekhterev National Medical Research Centre of Psychiatry and Neurology, St. PetersburgV.M. Bekhterev National Medical Research Centre of Psychiatry and Neurology, St. PetersburgV.M. Bekhterev National Medical Research Centre of Psychiatry and Neurology, St. PetersburgThe development of psychotic symptoms is traditionally linked to the increase of the functional activity of endogenous dopaminergic system. Antipsychotic effect of existing medications is associated with direct blockade of postsynaptic dopamine receptors. However, direct antagonistic activity is «alien» to physiological mechanisms of neurotransmission modulation, and presynaptic autoreceptor blockade mау produce a reverse (agonistic) effect, enhancing neurotransmitter release. On the other hand, anti-dopamine effect can be achieved by indirect antagonistic activity—by presynaptic dopamine depletion, which is consistent with the natural, physiological mechanisms of reducing neurotransmission. It can be assumed that modulation of presynaptic regulation is one of the promising directions for the development of antipsychotic drugs of future generations.https://www.bekhterevreview.com/jour/article/view/227antipsychoticsdirect- and indirectacting antagonistspre- and postsynaptic mechanisms of action |
| spellingShingle | V. I. Kozlovskiy D. N. Kosterin M. Yu. Popov The role of agonistic/antagonistic activity in the development of psychotropic effects of antipsychotics Обозрение психиатрии и медицинской психологии имени В.М. Бехтерева antipsychotics direct- and indirectacting antagonists pre- and postsynaptic mechanisms of action |
| title | The role of agonistic/antagonistic activity in the development of psychotropic effects of antipsychotics |
| title_full | The role of agonistic/antagonistic activity in the development of psychotropic effects of antipsychotics |
| title_fullStr | The role of agonistic/antagonistic activity in the development of psychotropic effects of antipsychotics |
| title_full_unstemmed | The role of agonistic/antagonistic activity in the development of psychotropic effects of antipsychotics |
| title_short | The role of agonistic/antagonistic activity in the development of psychotropic effects of antipsychotics |
| title_sort | role of agonistic antagonistic activity in the development of psychotropic effects of antipsychotics |
| topic | antipsychotics direct- and indirectacting antagonists pre- and postsynaptic mechanisms of action |
| url | https://www.bekhterevreview.com/jour/article/view/227 |
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