Comparative analysis of the inibitory effects of phenylpropenes and lidocaine on voltage-gated Na+ channels. (2008)
- Authors:
- Autor USP: CASSOLA, ANTONIO CARLOS - ICB
- Unidade: ICB
- Assunto: FISIOLOGIA (HUMANO)
- Language: Português
- Abstract: Objetivos: Eugenol (EUG, 2-methoxy-4-(2-propenyl)phenol ) is a phenylpropene used in dentistry as an analgesic We have shown a fast, reversible and low affinity (IC50=2.28±0.104mM) blockage of voltage-gated Na+ channels (Nav) by eugenol (EUG). EUG analogues with modifications in the aromatic ring have blocking effects similar to that of EUG. However, modifications in the aliphatic chain, that make it less hidrophobic, reduces the blocking effect. Isoeugenol (ISO) blocks Nav with higher affinity (IC50=1.16±0.211mM). We have undertaken a comparative analysis of the effects of EUG, ISO and lidocaine (LID). Métodos e resultados: Macroscopic Na+ currents were recorded on sensory neurons from rat dorsal root ganglia, by whole-cell patch-clamp technique. All experiments to investigate the blockage mechanism were carried on with IC50 concentrations of the blockers. LID blocks Nav with a IC50 of 1.42±0.169mM. There are quantitative differences between the phenylpropenes and lidocaine in the displacement of the steady-state activation curve to the right and of the steady-state inactivation curve to the left. The more conspicuous differences in the effects, were found in the time course for the recorery from inactivation and in the frequency dependence of the blocking effect. The time constant of exponentials for the recovery from inactivation of Na+ currents were delayed by EUG, ISO and LID by 79.8, 159.59 and 454.3% in relation to control. At pulse frequency of 2Hz the Na+ currents evoked by the twentieth pulse was reduced to 85% of first pulse under LID, to 92% under EUG and to 101% under ISO. At 5Hz, twentieth/first ratio were 56, 82 and 97% for LID, EUG and ISO, respectively. Conclusão: These results strongly suggest that phenylpropenes and LID block Nav binding at different sites.
- Imprenta:
- Publisher: Comissão de Cultura e Extensão Universitária do ICB/USP
- Publisher place: São Paulo
- Date published: 2008
- Source:
- Título do periódico: Resumos
- Conference titles: Congresso do Instituto de Ciências Biomédicas da Universidade de São Paulo
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ABNT
SOUZA, J. L. C. e CASSOLA, Antonio Carlos. Comparative analysis of the inibitory effects of phenylpropenes and lidocaine on voltage-gated Na+ channels. 2008, Anais.. São Paulo: Comissão de Cultura e Extensão Universitária do ICB/USP, 2008. . Acesso em: 26 abr. 2024. -
APA
Souza, J. L. C., & Cassola, A. C. (2008). Comparative analysis of the inibitory effects of phenylpropenes and lidocaine on voltage-gated Na+ channels. In Resumos. São Paulo: Comissão de Cultura e Extensão Universitária do ICB/USP. -
NLM
Souza JLC, Cassola AC. Comparative analysis of the inibitory effects of phenylpropenes and lidocaine on voltage-gated Na+ channels. Resumos. 2008 ;[citado 2024 abr. 26 ] -
Vancouver
Souza JLC, Cassola AC. Comparative analysis of the inibitory effects of phenylpropenes and lidocaine on voltage-gated Na+ channels. Resumos. 2008 ;[citado 2024 abr. 26 ] - Bloqueadores de canais dependentes de voltagem para cátions: terpenóides a peptídios
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