Tom Chappie, John Humphrey, Frank Menniti, Chris Schmidt
{"title":"PDE10A抑制剂:对当前中枢神经系统药物发现前景的评估","authors":"Tom Chappie, John Humphrey, Frank Menniti, Chris Schmidt","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>PDE10A is a dual substrate PDE that is highly expressed in medium spiny neurons of the striatal complex. The inhibition of PDE10A produces effects that modulate basal ganglia function in ways that suggest a particular therapeutic utility in the treatment of psychosis in schizophrenia. Significant understanding of PDE10A at the molecular level has helped to guide efforts in inhibitor design, and many different inhibitor classes have now been discovered. At least one PDE10A inhibitor has been advanced into clinical trials to begin to test the hypothesis that such agents may be useful in the treatment of psychosis.</p>","PeriodicalId":10809,"journal":{"name":"Current opinion in drug discovery & development","volume":"12 4","pages":"458-67"},"PeriodicalIF":0.0000,"publicationDate":"2009-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"PDE10A inhibitors: an assessment of the current CNS drug discovery landscape.\",\"authors\":\"Tom Chappie, John Humphrey, Frank Menniti, Chris Schmidt\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>PDE10A is a dual substrate PDE that is highly expressed in medium spiny neurons of the striatal complex. The inhibition of PDE10A produces effects that modulate basal ganglia function in ways that suggest a particular therapeutic utility in the treatment of psychosis in schizophrenia. Significant understanding of PDE10A at the molecular level has helped to guide efforts in inhibitor design, and many different inhibitor classes have now been discovered. At least one PDE10A inhibitor has been advanced into clinical trials to begin to test the hypothesis that such agents may be useful in the treatment of psychosis.</p>\",\"PeriodicalId\":10809,\"journal\":{\"name\":\"Current opinion in drug discovery & development\",\"volume\":\"12 4\",\"pages\":\"458-67\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2009-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current opinion in drug discovery & development\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current opinion in drug discovery & development","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
PDE10A inhibitors: an assessment of the current CNS drug discovery landscape.
PDE10A is a dual substrate PDE that is highly expressed in medium spiny neurons of the striatal complex. The inhibition of PDE10A produces effects that modulate basal ganglia function in ways that suggest a particular therapeutic utility in the treatment of psychosis in schizophrenia. Significant understanding of PDE10A at the molecular level has helped to guide efforts in inhibitor design, and many different inhibitor classes have now been discovered. At least one PDE10A inhibitor has been advanced into clinical trials to begin to test the hypothesis that such agents may be useful in the treatment of psychosis.
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