I am a
Home I AM A Search Login

Papers of the Week

Papers: 3 Jul 2021 - 9 Jul 2021

Animal Studies, Pharmacology/Drug Development

2021 Jul 08

J Med Chem

Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σ Receptor Antagonists for the Treatment of Pain.


García M, Llorente V, Garriga L, Christmann U, Rodríguez-Escrich S, Virgili M, Fernández B, Bordas M, Ayet E, Burgueño J, Pujol M, Dordal A, Portillo-Salido E, Gris G, Vela J M, Almansa C
J Med Chem. 2021 Jul 08.
PMID: 34236190.


A new series of propionamide derivatives was developed as dual μ-opioid receptor agonists and σ receptor antagonists. Modification of a high-throughput screening hit originated a series of piperazinylcycloalkylmethyl propionamides, which were explored to overcome the challenge of achieving balanced dual activity and convenient drug-like properties. The lead compound identified, , showed good analgesic effects in several animal models of both acute (paw pressure) and chronic (partial sciatic nerve ligation) pain, with reduced gastrointestinal effects in comparison with oxycodone.