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Analgesic and side effects of intravenous recombinant Phα1ß.
Rigo, Flavia Karine; Rossato, Mateus Fortes; Borges, Vanessa; da Silva, Juliana Figueira; Pereira, Elizete Maria Rita; de Ávila, Ricardo Andrez Machado; Trevisan, Gabriela; Dos Santos, Duana Carvalho; Diniz, Danuza Montijo; Silva, Marco Aurélio Romano; de Castro, Célio José; Cunha, Thiago Mattar; Ferreira, Juliano; Gomez, Marcus Vinicius.
Afiliación
  • Rigo FK; Graduate Program in Health Sciences, University of the Extreme South of Santa Catarina (UNESC), Criciúma, SC, Brazil.
  • Rossato MF; Department of Pharmacology, Ribeirão Preto Medical School, University of São Paulo (USP), Ribeirão Preto, SP, Brazil.
  • Borges V; Department of Pharmacology, Ribeirão Preto Medical School, University of São Paulo (USP), Ribeirão Preto, SP, Brazil.
  • da Silva JF; Institute of Education and Research of Santa Casa Belo Horizonte, Santa Casa of Belo Horizonte Group, Belo Horizonte, MG, Brazil.
  • Pereira EMR; Institute of Education and Research of Santa Casa Belo Horizonte, Santa Casa of Belo Horizonte Group, Belo Horizonte, MG, Brazil.
  • de Ávila RAM; Graduate Program in Health Sciences, University of the Extreme South of Santa Catarina (UNESC), Criciúma, SC, Brazil.
  • Trevisan G; Graduate Program in Health Sciences, University of the Extreme South of Santa Catarina (UNESC), Criciúma, SC, Brazil.
  • Dos Santos DC; Institute of Education and Research of Santa Casa Belo Horizonte, Santa Casa of Belo Horizonte Group, Belo Horizonte, MG, Brazil.
  • Diniz DM; Institute of Education and Research of Santa Casa Belo Horizonte, Santa Casa of Belo Horizonte Group, Belo Horizonte, MG, Brazil.
  • Silva MAR; Department of Neurosciences, School of Medicine, Federal University of Minas Gerais (UFMG), Belo Horizonte, MG, Brazil.
  • de Castro CJ; Institute of Education and Research of Santa Casa Belo Horizonte, Santa Casa of Belo Horizonte Group, Belo Horizonte, MG, Brazil.
  • Cunha TM; Department of Pharmacology, Ribeirão Preto Medical School, University of São Paulo (USP), Ribeirão Preto, SP, Brazil.
  • Ferreira J; Department of Pharmacology, Federal University of Santa Catarina, Florianópolis, SC, Brazil.
  • Gomez MV; Institute of Education and Research of Santa Casa Belo Horizonte, Santa Casa of Belo Horizonte Group, Belo Horizonte, MG, Brazil.
J Venom Anim Toxins Incl Trop Dis ; 26: e20190070, 2020 Apr 17.
Article en En | MEDLINE | ID: mdl-32362927
BACKGROUND: Intrathecal injection of voltage-sensitive calcium channel blocker peptide toxins exerts analgesic effect in several animal models of pain. Upon intrathecal administration, recombinant Phα1ß exerts the same analgesic effects as the those of the native toxin. However, from a clinical perspective, the intrathecal administration limits the use of anesthetic drugs in patients. Therefore, this study aimed to investigate the possible antinociceptive effect of intravenous recombinant Phα1ß in rat models of neuropathic pain, as well as its side effects on motor, cardiac (heart rate and blood pressure), and biochemical parameters. METHODS: Male Wistar rats and male Balb-C mice were used in this study. Giotto Biotech® synthesized the recombinant version of Phα1ß using Escherichia coli expression. In rats, neuropathic pain was induced by chronic constriction of the sciatic nerve and paclitaxel-induced acute and chronic pain. Mechanical sensitivity was evaluated using von Frey filaments. A radiotelemeter transmitter (TA11PA-C10; Data Sciences, St. Paul, MN, USA) was placed on the left carotid of mice for investigation of cardiovascular side effects. Locomotor activity data were evaluated using the open-field paradigm, and serum CKMB, TGO, TGP, LDH, lactate, creatinine, and urea levels were examined. RESULTS: Intravenous administration of recombinant Phα1ß toxin induced analgesia for up to 4 h, with ED50 of 0.02 (0.01-0.03) mg/kg, and reached the maximal effect (Emax = 100% antinociception) at a dose of 0.2 mg/kg. No significant changes were observed in any of the evaluated motor, cardiac or biochemical parameters. CONCLUSION: Our data suggest that intravenous administration of recombinant Phα1ß may be feasible for drug-induced analgesia, without causing any severe side effects.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: J Venom Anim Toxins Incl Trop Dis Año: 2020 Tipo del documento: Article País de afiliación: Brasil Pais de publicación: Brasil

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: J Venom Anim Toxins Incl Trop Dis Año: 2020 Tipo del documento: Article País de afiliación: Brasil Pais de publicación: Brasil