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Inicio Revista Española de Anestesiología y Reanimación (English Edition) Dualism, allosteric modulation, and biased signaling of opioid receptors: Future...
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Vol. 71. Issue 4.
Pages 298-303 (April 2024)
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Vol. 71. Issue 4.
Pages 298-303 (April 2024)
Special article
Dualism, allosteric modulation, and biased signaling of opioid receptors: Future therapeutic potential
Dualismo, modulación alostérica y señalización diferencial en los receptores opiáceos: futuro potencial terapéutico
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3
A.M. González
Corresponding author
, A.G. Jubete
Service of Anesthesiology, Universitary Hospital Marqués de Valdecilla, Santander, Cantabria, Spain
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Tables (3)
Table 1. Main clinical effects of opioid agonists (adapted from12).
Table 2. Opioid allosteric modulators (adapted from22).
Table 3. Biased ligands (adapted from24).
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Abstract

Opioids are still the drugs of choice for the treatment of acute post-surgical pain and chronic cancer pain. Overprescribing of these drugs has given rise to an “opioid crisis” in some countries. In this context, attention has been drawn to the therapeutic potential of various ligands that act as allosteric modulators of orthosteric binding sites and modulate the drug’s activity, affinity, potency, and even efficacy.

Keywords:
Opioids
Future therapeutic potential
Resumen

Los fármacos opioides permanecen como fármacos de elección en el tratamiento del dolor agudo postoperatorio y del dolor crónico oncológico. Su prescripción inadecuada, a dado lugar, en algunos países, a una verdadera "crisis de opioides". En este contexto, puede resultar interesante el potencial terapéutico de algunos ligandos que actúan como moduladores alostéricos de la fijación de los agonistas opioides  y su capacidad de modular su actividad, modificando su afinidad, potencia e incluso eficacia.

Palabras clave:
Fármacos opioides
Dolor
Receptor opioide
Efectos adversos opioides

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