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Towards multitargeted ligands as pain therapeutics: Dual ligands of the Cavα2δ-1 subunit of voltage-gated calcium channel and the μ-opioid receptor
ChemMedChem ( IF 3.4 ) Pub Date : 2024-01-17 , DOI: 10.1002/cmdc.202300473
Anita Wegert 1 , Menno Monnee 1 , Wouter de Graaf 1 , Frank van Holst 1 , Giovanni Bolcato 1 , José Luis Díaz 2 , Albert Dordal 2 , Enrique Portillo‐Salido 2 , Raquel F. Reinoso 2 , Sandra Yeste 2 , Antoni Torrens 2 , Carmen Almansa 2
Affiliation  

A series of dual ligands acting on the α2δ-1 subunit of voltage-gated calcium channels and the μ-opioid receptor (MOR) was designed by merging of the two non-structurally related target pharmacophores. The new amino-acidic derivatives are represented by compound 31 (WLB-83038) which exhibits a good drug-like profile and analgesia in several pain models.

中文翻译:

走向多靶点配体作为疼痛治疗:电压门控钙通道的 Cavα2δ-1 亚基和 μ-阿片受体的双配体

通过合并两个非结构相关的目标药效团,设计了一系列作用于电压门控钙通道的α2δ-1亚基和μ阿片受体(MOR)的双配体。新的氨基酸衍生物以化合物31 (WLB-83038) 为代表,在多种疼痛模型中表现出良好的药物样特征和镇痛作用。
更新日期:2024-01-18
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