Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, via Mangiagalli 25, I-20133 Milano, Italy.
J Med Chem. 2023 Nov 9;66(21):14494-14496. doi: 10.1021/acs.jmedchem.3c01817. Epub 2023 Oct 18.
In the striatum, presynaptic α6-containig nicotinic receptors are crucially involved in the modulation of dopamine release. CVN417, a novel selective antagonist at this receptor subtype, attenuates motor dysfunction in a Parkinson's disease-relevant animal model, suggesting, for this pathology, a therapeutic strategy that could greatly profit from the restricted localization of α6* nicotinic receptors in the brain.
在纹状体中,包含α6 的突触前烟碱型乙酰胆碱受体对于调节多巴胺释放至关重要。新型选择性 α6 烟碱型乙酰胆碱受体拮抗剂 CVN417 可减轻与帕金森病相关的动物模型中的运动功能障碍,这表明对于这种病理,一种治疗策略可以从大脑中α6*烟碱型乙酰胆碱受体的受限定位中获益匪浅。