Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Das, Swagatika, Roayapalley, Praveen K., Vashishtha, Sarvesh C., Das, Umashankar, Dimmock, Jonathan R.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
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
_version_ 1785112615448477696
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
work_keys_str_mv AT dasswagatika anticonvulsantpropertiesof1diethylamino3phenylprop2en1one
AT roayapalleypraveenk anticonvulsantpropertiesof1diethylamino3phenylprop2en1one
AT vashishthasarveshc anticonvulsantpropertiesof1diethylamino3phenylprop2en1one
AT dasumashankar anticonvulsantpropertiesof1diethylamino3phenylprop2en1one
AT dimmockjonathanr anticonvulsantpropertiesof1diethylamino3phenylprop2en1one