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3,3-Dibromoflavanone, a synthetic flavonoid derivative for pain management with antidepressant-like effects and fewer side effects than those of morphine in mice.
Colettis, Natalia; Higgs, Josefina; Wasowski, Cristina; Knez, Damijan; Gobec, Stanislav; Pastore, Valentina; Marder, Mariel.
Afiliação
  • Colettis N; Universidad de Buenos Aires, Consejo Nacional de Investigaciones Científicas y Técnicas, Laboratorio de Neuro-Fito-Farmacología Medicinal, Instituto de Química y Fisicoquímica Biológicas Prof. Dr. Alejandro C. Paladini, Facultad de Farmacia y Bioquímica, Junín 956 (C1113AAD), Buenos Aires, Argentina
  • Higgs J; Universidad de Buenos Aires, Consejo Nacional de Investigaciones Científicas y Técnicas, Laboratorio de Neuro-Fito-Farmacología Medicinal, Instituto de Química y Fisicoquímica Biológicas Prof. Dr. Alejandro C. Paladini, Facultad de Farmacia y Bioquímica, Junín 956 (C1113AAD), Buenos Aires, Argentina
  • Wasowski C; Universidad de Buenos Aires, Consejo Nacional de Investigaciones Científicas y Técnicas, Laboratorio de Neuro-Fito-Farmacología Medicinal, Instituto de Química y Fisicoquímica Biológicas Prof. Dr. Alejandro C. Paladini, Facultad de Farmacia y Bioquímica, Junín 956 (C1113AAD), Buenos Aires, Argentina
  • Knez D; University of Ljubljana, Faculty of Pharmacy, Askerceva 7, SI-1000, Ljubljana, Slovenia. Electronic address: damijan.knez@ffa.uni-lj.si.
  • Gobec S; University of Ljubljana, Faculty of Pharmacy, Askerceva 7, SI-1000, Ljubljana, Slovenia. Electronic address: Stanislav.Gobec@ffa.uni-lj.si.
  • Pastore V; Universidad de Buenos Aires, Consejo Nacional de Investigaciones Científicas y Técnicas, Laboratorio de Neuro-Fito-Farmacología Medicinal, Instituto de Química y Fisicoquímica Biológicas Prof. Dr. Alejandro C. Paladini, Facultad de Farmacia y Bioquímica, Junín 956 (C1113AAD), Buenos Aires, Argentina
  • Marder M; Universidad de Buenos Aires, Consejo Nacional de Investigaciones Científicas y Técnicas, Laboratorio de Neuro-Fito-Farmacología Medicinal, Instituto de Química y Fisicoquímica Biológicas Prof. Dr. Alejandro C. Paladini, Facultad de Farmacia y Bioquímica, Junín 956 (C1113AAD), Buenos Aires, Argentina
Chem Biol Interact ; 402: 111189, 2024 Oct 01.
Article em En | MEDLINE | ID: mdl-39121896
ABSTRACT
In the pursuit of new lead compounds with fewer side effects than opioids, the novel synthetic phytochemical core, 3,3-dibromoflavanone (3,3-DBF), has emerged as a promising candidate for pain management. Acute assays demonstrated dose-dependent central and peripheral antinociceptive activity of 3,3-DBF through the µ-opioid receptor. This study aimed to explore repeated administration effects of 3,3-DBF in mice and compare them with morphine. Mice were treated with 3,3-DBF (30 mg/kg), morphine (6 mg/kg), or vehicle for 10 days, alongside single-treatment groups. Unlike morphine, 3,3-DBF demonstrated antinociceptive effects in the hot plate test without inducing tolerance. Locomotor activity and motor coordination tests (evaluated through the inverted screen and rotarod tests) revealed no significant differences between the 3,3-DBF-treated and control groups. The gastrointestinal transit assay indicated that 3,3-DBF did not induce constipation, in contrast to morphine. Furthermore, withdrawal signs assessed with the Gellert-Holtzman scale were not comparable to morphine. Additionally, 3,3-DBF exhibited antidepressant-like activity, reducing immobility time in the forced swimming and tail suspension tests, akin to imipramine. In summary, 3,3-DBF demonstrated antinociceptive effects without inducing tolerance or dependence and exhibited antidepressant properties. These findings highlight the potential of 3,3-DBF as a promising therapeutic agent for pain management and its comorbidities, offering advantages over morphine by minimizing side effects.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Flavonoides / Analgésicos / Morfina / Antidepressivos Limite: Animals Idioma: En Revista: Chem Biol Interact Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Argentina País de publicação: Irlanda

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Flavonoides / Analgésicos / Morfina / Antidepressivos Limite: Animals Idioma: En Revista: Chem Biol Interact Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Argentina País de publicação: Irlanda