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Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
Published on: July 29, 2014
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La regulación del tráfico de receptores opioides y la tolerancia a la morfina mediante la oligomerización de los
Li He1, Jamie Fong, Mark von Zastrow
1Ernest Gallo Clinic and Research Center, University of California San Francisco, Emeryville, CA 94608, USA.
Cell
|February 8, 2002
Resumen
La tolerancia a la morfina, un desafío en el manejo del dolor crónico, puede reducirse. La combinación de morfina con DAMGO facilita la endocitosis del receptor opioide mu (MOR), disminuyendo significativamente la tolerancia analgésica en ratas.
Área de la Ciencia:
- Farmacología Farmacología.
- La neurociencia es la neurociencia.
- Manejo del dolor Manejo del dolor.
Sus antecedentes:
- El tratamiento del dolor crónico está limitado por la tolerancia a la morfina.
- La morfina activa los receptores opioides mu (MOR) sin promover la desensibilización o la endocitosis.
- Desarrollar estrategias para superar la tolerancia a los analgésicos es crucial para un manejo eficaz del dolor.
Objetivo del estudio:
- Para investigar si DAMGO puede facilitar la endocitosis MOR inducida por la morfina.
- Para determinar si la administración conjunta de morfina y DAMGO reduce la tolerancia analgésica.
- Explorar el potencial de la endocitosis MOR como objetivo terapéutico para el dolor crónico.
Principales métodos:
- Se utilizó [D-Ala(2)-MePhe(4)-Gly(5)-ol] enkefalina (DAMGO) para atacar el MOR.
- Se administró morfina y DAMGO a ratas para el tratamiento crónico.
- Evaluación de la tolerancia analgésica mediante la comparación de la eficacia del fármaco en el tiempo.
Principales resultados:
- DAMGO facilitó la endocitosis MOR inducida por la morfina.
- Las ratas tratadas con morfina y DAMGO mostraron una tolerancia analgésica reducida en comparación con el tratamiento solo con morfina.
- Se demostró que la endocitosis MOR mitiga el desarrollo de la tolerancia analgésica.
Conclusiones:
- La endocitosis MOR es un mecanismo viable para reducir la tolerancia a los analgésicos opioides.
- La coadministración de agentes de internalización de MOR con morfina ofrece una estrategia potencial para mejorar la terapia del dolor crónico.
- Esta investigación allana el camino para el desarrollo de nuevos análogos de opioides con eficacia analgésica sostenida.
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