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Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one
There is a need for novel antiepileptic agents whose modes of action differ from those of current antiepileptic drugs. The objective of this study was to determine whether 1-diethylamino-3-phenylprop-2-en-1-one (2) could prevent or at least diminish convulsions caused by different mechanisms. This a...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10535378/ https://www.ncbi.nlm.nih.gov/pubmed/37755244 http://dx.doi.org/10.3390/medicines10090054 |
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author | Das, Swagatika Roayapalley, Praveen K. Vashishtha, Sarvesh C. Das, Umashankar Dimmock, Jonathan R. |
author_facet | Das, Swagatika Roayapalley, Praveen K. Vashishtha, Sarvesh C. Das, Umashankar Dimmock, Jonathan R. |
author_sort | Das, Swagatika |
collection | PubMed |
description | There is a need for novel antiepileptic agents whose modes of action differ from those of current antiepileptic drugs. The objective of this study was to determine whether 1-diethylamino-3-phenylprop-2-en-1-one (2) could prevent or at least diminish convulsions caused by different mechanisms. This amide afforded protection in the maximal electroshock and subcutaneous pentylenetetrazole screens when given intraperitoneally to both mice and rats. A number of specialized tests in mice were conducted and are explained in the text. They revealed (2) to have efficacy in the 6 Hz psychomotor seizure test, the corneal kindling model, the mouse temporal epilepsy screen and a peripheral neuronal transmission test using formalin. Three screens in rats were undertaken, which revealed that (2) blocked chloride channels, inhibited peripheral neuronal transmission (tested using sciatic ligation and von Frey fibres) and afforded protection in the lamotrigine-resistant kindled rat model. The biodata generated reveal that (2) is an important lead molecule in the quest for novel structures to combat epilepsy. |
format | Online Article Text |
id | pubmed-10535378 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-105353782023-09-29 Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one Das, Swagatika Roayapalley, Praveen K. Vashishtha, Sarvesh C. Das, Umashankar Dimmock, Jonathan R. Medicines (Basel) Brief Report There is a need for novel antiepileptic agents whose modes of action differ from those of current antiepileptic drugs. The objective of this study was to determine whether 1-diethylamino-3-phenylprop-2-en-1-one (2) could prevent or at least diminish convulsions caused by different mechanisms. This amide afforded protection in the maximal electroshock and subcutaneous pentylenetetrazole screens when given intraperitoneally to both mice and rats. A number of specialized tests in mice were conducted and are explained in the text. They revealed (2) to have efficacy in the 6 Hz psychomotor seizure test, the corneal kindling model, the mouse temporal epilepsy screen and a peripheral neuronal transmission test using formalin. Three screens in rats were undertaken, which revealed that (2) blocked chloride channels, inhibited peripheral neuronal transmission (tested using sciatic ligation and von Frey fibres) and afforded protection in the lamotrigine-resistant kindled rat model. The biodata generated reveal that (2) is an important lead molecule in the quest for novel structures to combat epilepsy. MDPI 2023-09-08 /pmc/articles/PMC10535378/ /pubmed/37755244 http://dx.doi.org/10.3390/medicines10090054 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Brief Report Das, Swagatika Roayapalley, Praveen K. Vashishtha, Sarvesh C. Das, Umashankar Dimmock, Jonathan R. Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one |
title | Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one |
title_full | Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one |
title_fullStr | Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one |
title_full_unstemmed | Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one |
title_short | Anticonvulsant Properties of 1-Diethylamino-3-phenylprop-2-en-1-one |
title_sort | anticonvulsant properties of 1-diethylamino-3-phenylprop-2-en-1-one |
topic | Brief Report |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10535378/ https://www.ncbi.nlm.nih.gov/pubmed/37755244 http://dx.doi.org/10.3390/medicines10090054 |
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