Anticonvulsant and analgesic in neuropathic pain activity in a group of new aminoalkanol derivatives.
Bioorg Med Chem Lett
; 30(16): 127325, 2020 08 15.
Article
em En
| MEDLINE
| ID: mdl-32631530
ABSTRACT
As part of the presented research, thirteen new aminoalkanol derivatives were designed and obtained by chemical synthesis. In vivo studies (mice, i.p.) showed anticonvulsant activity (MES) of nine compounds, and in the case of one compound (R,S-trans-2-((2-(2,3,5-trimethylphenoxy)ethyl)amino)cyclohexan-1-ol, 4) both anticonvulsant (ED50 MES = 15.67 mg/kg, TD50 rotarod = 78.30 mg.kg, PI = 5.00) and analgesic activity (OXA-induced neuropathic pain, active at 15 mg/kg). For selected active compounds additional in vitro studies have been performed, including receptor studies (5-HT1A), evaluation of antioxidant activity (DPPH assay), metabolism studies as well as safety panel (mutagenicity, safety in relation to the gastrointestinal flora, cytotoxicity towards astrocytes as well as impact on their proliferation and cell cycle).
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Amino Álcoois
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Analgésicos
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Anticonvulsivantes
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Neuralgia
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Antioxidantes
Limite:
Animals
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Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article