Instituto de Quimica Medica (CSIC), Spain.
Curr Med Chem. 2014 Apr;21(10):1171-87. doi: 10.2174/0929867321666131228221749.
Phosphodiesterases (PDEs), as key regulators of cyclic nucleotides, and their inhibitors have been emerged as new pharmacological targets and promising drug candidates for many diseases, including central nervous system pathologies. The high level of PDE10A expression in the striatal medium spiny neurons suggests a prominent function role for the isoenzyme. Basal ganglia dysfunction is associated with neuropsychiatric disorders and until recently the development of PDE10A inhibitors has been focused on schizophrenia. Currently, the pharmaceutical research on PDE10A inhibitors is moving to show the modulation of other functions associated with the basal ganglia such the motor control. Thus, PDE10A inhibitors may be important pharmacological agents for neurodegenerative disorders such as Parkinson's and Huntington's diseases. Recent data supporting new clues for PDE10A as therapeutic target together with a concise review of the chemical structures of its inhibitors are provided here. The goal of this manuscript is to provide new ideas for assistant pharmacologist and medicinal chemists in the search for PDE10A inhibitors as new disease modifying drugs for Parkinson's disease.
磷酸二酯酶(PDEs)作为环核苷酸的关键调节剂,及其抑制剂已成为许多疾病(包括中枢神经系统疾病)新的药理学靶点和有前途的药物候选物。纹状体中间神经元中高水平表达的 PDE10A 表明该同工酶具有重要的功能作用。基底神经节功能障碍与神经精神疾病有关,直到最近,PDE10A 抑制剂的开发一直集中在精神分裂症上。目前,对 PDE10A 抑制剂的药物研究正在转向调节与基底神经节相关的其他功能,如运动控制。因此,PDE10A 抑制剂可能是帕金森病和亨廷顿病等神经退行性疾病的重要药物。本文提供了支持 PDE10A 作为治疗靶点的新线索的最新数据,并简要综述了其抑制剂的化学结构。本文的目的是为辅助药理学家和药物化学家提供新思路,寻找 PDE10A 抑制剂作为治疗帕金森病的新型疾病修饰药物。