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腺苷 A 受体拮抗剂治疗帕金森病的药理学潜力。

The Pharmacological Potential of Adenosine A Receptor Antagonists for Treating Parkinson's Disease.

机构信息

Kyowa Kirin Co., Ltd., Tokyo 100-0004, Japan.

Molecular Neuropharmacology Laboratory, Wenzhou Medical University, Wenzhou 325015, China.

出版信息

Molecules. 2022 Apr 6;27(7):2366. doi: 10.3390/molecules27072366.

DOI:10.3390/molecules27072366
PMID:35408767
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9000505/
Abstract

The adenosine A receptor subtype is recognized as a non-dopaminergic pharmacological target for the treatment of neurodegenerative disorders, notably Parkinson's disease (PD). The selective A receptor antagonist istradefylline is approved in the US and Japan as an adjunctive treatment to levodopa/decarboxylase inhibitors in adults with PD experiencing OFF episodes or a wearing-off phenomenon; however, the full potential of this drug class remains to be explored. In this article, we review the pharmacology of adenosine A receptor antagonists from the perspective of the treatment of both motor and non-motor symptoms of PD and their potential for disease modification.

摘要

腺苷 A 受体亚型被认为是治疗神经退行性疾病(尤其是帕金森病)的非多巴胺能药物靶点。选择性 A 受体拮抗剂伊曲茶碱在美国和日本被批准作为左旋多巴/脱羧酶抑制剂的辅助治疗药物,用于治疗出现“OFF”发作或“关期”现象的成年帕金森病患者;然而,这类药物的全部潜力仍有待探索。本文从治疗帕金森病的运动和非运动症状及其对疾病修饰的潜在作用的角度,综述了腺苷 A 受体拮抗剂的药理学。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1294/9000505/acd9e0f41f46/molecules-27-02366-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1294/9000505/7f7f0a5da6c0/molecules-27-02366-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1294/9000505/acd9e0f41f46/molecules-27-02366-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1294/9000505/7f7f0a5da6c0/molecules-27-02366-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1294/9000505/acd9e0f41f46/molecules-27-02366-g002.jpg

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Pharmacol Rev. 2022 Apr;74(2):340-372. doi: 10.1124/pharmrev.121.000445.
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An Update on Nondopaminergic Treatments for Motor and Non-motor Symptoms of Parkinson's Disease.帕金森病运动和非运动症状的非多巴胺能治疗方法的最新进展。
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Discovery of novel AR antagonist via 3D-QSAR pharmacophore modeling: neuroprotective effects in 6-OHDA-induced SH-SY5Y cells and haloperidol-induced Parkinsonism in C57 bl/6 mice.通过3D-QSAR药效团模型发现新型雄激素受体拮抗剂:对6-羟基多巴胺诱导的SH-SY5Y细胞的神经保护作用以及对C57BL/6小鼠氟哌啶醇诱导的帕金森病的影响
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