S4B-3 Targeted to Serotonergic and Adenosine Systems in Parkinsons Disease Drug Development  

作　　者：ZHEN Xue-chu 

机构地区：[1]Jiangsu Key Laboratory of Neuropsychiatric Diseases and College of Pharmaceutical Sciences,Soochow University,Suzhou,215006,China

出　　处：《神经药理学报》2018年第4期72-73,共2页Acta Neuropharmacologica

摘　　要：Parkinson’s disease(PD)is a progressive neurodegenerative disorder.While dopaminergic agents are effective in reliving the motor symptoms,however,chronic dopamine replacement treatment could also induce motor fluctuation and dyskinesia.In addition,there is still a clinical unmet need for novel medications that can treat the non-motor symptoms.Recent evidence suggests that the serotonergic nervous system may be an important target for both motor and non-motor symptoms for PD Meanwhile,adenosine A2A receptors enriched in basal ganglia areas and their antagonistic role towards dopamine receptor stimulation,have positioned A2A receptor antagonists as an a promising target to improve the motor deficits.We have developed a series of dual dopamine receptor and 5-HT1A receptor ligands and A2A receptor antagonists either through natural resource or rational design.We pharmacologically characterized those compounds and provided clear evidences that dual 5-HT/dopamine or A2A receptor antagonist exhibited excellent anti-Parkinsonian effect while it reduced the development of dyskinesia and effectively relieved some of the non-motor symptoms in PD animal models.

关 键 词：NON-MOTOR SYMPTOMS positioned A2A receptor 

分 类 号：R73[医药卫生—肿瘤]