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Synergistic antinociceptive effect of a calcium channel blocker and a TRPV1 blocker in an acute pain model in mice.
Palhares, Manuella R; Silva, Juliana F; Rezende, Marcio Junior S; Santos, Duana C; Silva-Junior, Cláudio A; Borges, Márcia H; Ferreira, Juliano; Gomez, Marcus V; Castro-Junior, Célio J.
Afiliação
  • Palhares MR; Department of Neurotransmitters, Institute for Education and Research, Hospital Santa Casa, Belo Horizonte, Minas Gerais 30150-240, Brazil.
  • Silva JF; Department of Neurotransmitters, Institute for Education and Research, Hospital Santa Casa, Belo Horizonte, Minas Gerais 30150-240, Brazil.
  • Rezende MJS; Department of Neurotransmitters, Institute for Education and Research, Hospital Santa Casa, Belo Horizonte, Minas Gerais 30150-240, Brazil.
  • Santos DC; Department of Neurotransmitters, Institute for Education and Research, Hospital Santa Casa, Belo Horizonte, Minas Gerais 30150-240, Brazil.
  • Silva-Junior CA; Department of Neurotransmitters, Institute for Education and Research, Hospital Santa Casa, Belo Horizonte, Minas Gerais 30150-240, Brazil.
  • Borges MH; Department of Biochemistry, Ezequiel Dias Foundation, Belo Horizonte, Minas Gerais 30510-010, Brazil.
  • Ferreira J; Department of Pharmacology, Biological Sciences Center, Federal University of Santa Catarina, Florianópolis, Santa Catarina 80040-900, Brazil.
  • Gomez MV; Department of Neurotransmitters, Institute for Education and Research, Hospital Santa Casa, Belo Horizonte, Minas Gerais 30150-240, Brazil.
  • Castro-Junior CJ; Department of Neurotransmitters, Institute for Education and Research, Hospital Santa Casa, Belo Horizonte, Minas Gerais 30150-240, Brazil. Electronic address: celiojcjunior@gmail.com.
Life Sci ; 182: 122-128, 2017 Aug 01.
Article em En | MEDLINE | ID: mdl-28629730
AIMS: Extensive evidence supports a role for voltage-gated calcium channels (VGCC) and TRPV1 receptors in pain transmission and modulation. We investigated the profile of analgesic interaction between Phα1ß toxin (a VGCC blocker) and SB366791 (selective TRPV1 antagonist) in a model of acute pain induced by capsaicin. Changes in body temperature induced by combination regimens were also evaluated. MAIN METHODS: Isobolographic approach with a fixed dose-ratio of combined drugs was used to determine whether antinociceptive interaction of Phα1ß and SB366791 are subadditive, additive or synergic. Body temperature was obtained by thermal infrared imaging. KEY FINDINGS: Phα1ß and SB366791 interact in a synergistic manner to cause antinociception. We found an interaction index (α) of 0.07 for Phα1ß and SB366791 when these drugs were injected together intraplantarly, which indicates that in vivo interaction between these drugs is greater than additive interaction. Synergism also occurred when intraplantar SB366791 was administered simultaneously with intrathecal Phα1ß (interaction index α=0.06) suggesting a 15 fold rise in potency on the analgesic effect of these drugs when they are added together. It was observed no significant alterations in body temperature of animals treated with this combination regimen. SIGNIFICANCE: Our data reveal that Phα1ß toxin potentiates in 15 fold the antinociceptive action of the TRPV1 blocker SB366791. Therefore, lower doses of these drugs are required to achieve antinociceptive effects when these agents are given in combination.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Venenos de Aranha / Cinamatos / Canais de Cátion TRPV / Dor Aguda / Analgésicos / Anilidas Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Life Sci Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Venenos de Aranha / Cinamatos / Canais de Cátion TRPV / Dor Aguda / Analgésicos / Anilidas Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Life Sci Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda