Chalcones reverse the anxiety and convulsive behavior of adult zebrafish
Autor: | Maria Kueirislene Amâncio Ferreira, Paulo Nogueira Bandeira, Ketelly Vanessa Barros Sales, Emmanuel Silva Marinho, Joyce do Nascimento Martins Cardoso, Francisco Ernani Alves Magalhães, Emanuelle Machado Marinho, Atilano Lucas dos Santos Moura, Antonio Wlisses da Silva, Jane Eire Silva Alencar de Menezes, Márcia Machado Marinho, Hélcio Silva dos Santos |
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Rok vydání: | 2021 |
Předmět: |
medicine.drug_class
medicine.medical_treatment Anxiety Pharmacology Anxiolytic Open field 03 medical and health sciences Behavioral Neuroscience Chalcones 0302 clinical medicine Seizures medicine Animals 030212 general & internal medicine Zebrafish Benzodiazepine Behavior Animal GABAA receptor Chemistry Antagonist Receptors GABA-A Anticonvulsant Anti-Anxiety Agents Neurology Flumazenil GABAergic Neurology (clinical) 030217 neurology & neurosurgery medicine.drug |
Zdroj: | Epilepsy & Behavior. 117:107881 |
ISSN: | 1525-5050 |
DOI: | 10.1016/j.yebeh.2021.107881 |
Popis: | In the treatment of anxiety and seizures, drugs of the benzodiazepine (BZD) class are used, which act on the Central Nervous System (CNS) through the neurotransmitter gamma-aminobutyric acid (GABA). Flavonoids modulate GABAA receptors. The aim of this study was to evaluate the anxiolytic and anticonvulsant effects of synthetic chalcones and their mechanisms of action via the GABAergic system, using adult zebrafish (ZFa). The animals were treated with chalcones (4.0 or 20 or 40 mg/kg; 20 µL; i.p) and submitted to the open field and 96 h toxicity test. Chalcones that cause locomotor alteration were evaluated in the light and dark anxiolytic test. The same doses of chalcones were evaluated in the anticonvulsant test. The lowest effective dose was chosen to assess the possible involvement in the GABAA receptor by blocking the flumazenil (fmz) antagonist. No chalcone was toxic and altered ZFa’s locomotion. All chalcones had anxiolytic and anticonvulsant effects, mainly chalcones 1, where all doses showed effects in both tests. These effects were blocked by Fmz (antagonist GABAA), where it shows evidence of the performance of these activities of the GABA system. Therefore, this study demonstrated in relation to structure–activity, that the position of the substituents is important in the intensity of activities and that the absence of toxicity and the action of these compounds in the CNS, shows the pharmacological potential of these molecules, and, therefore, the insights are designed for the development of new drugs. |
Databáze: | OpenAIRE |
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