Bispecific sigma-1 receptor antagonism and mu-opioid receptor partial agonism: WLB-73502, an analgesic with improved efficacy and safety profile compared to strong opioids

Bispecific sigma-1 receptor antagonism and mu-opioid receptor partial agonism: WLB-73502, an analgesic with improved efficacy and safety profile compared to strong opioids

Opioids are the most effective painkillers, but their benefit-risk balance often hinder their therapeutic use. WLB-73502 is a dual, bispecific compound that binds sigma-1 (S1R) and mu-opioid (MOR) receptors. WLB-73502 is an antagonist at the S1R. It behaved as a partial MOR agonist at the G-protein...

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Bibliographic Details
Main Authors: Alba Vidal-Torres, Begoña Fernández-Pastor, Mónica García, Eva Ayet, Anna Cabot, Javier Burgueño, Xavier Monroy, Bertrand Aubel, Xavier Codony, Luz Romero, Rosalía Pascual, Maria Teresa Serafini, Gregorio Encina, Carmen Almansa, Daniel Zamanillo, Manuel Merlos, José Miguel Vela
Format: Article
Language:English
Published: Elsevier 2023-01-01
Series:Acta Pharmaceutica Sinica B
Subjects:
WLB-73502
Sigma-1 receptor
Mu-opioid receptor
Biased agonist
Analgesic activity
Chronic pain
Online Access:http://www.sciencedirect.com/science/article/pii/S221138352200404X

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http://www.sciencedirect.com/science/article/pii/S221138352200404X

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