{"title":"A - 5-HT1A激动剂瑞匹诺坦治疗急性缺血性脑卒中。","authors":"Helmi L Lutsep","doi":"10.2174/1568007053544165","DOIUrl":null,"url":null,"abstract":"<p><p>Serotonin agonists can reduce glutamate-induced excitotoxicity in cerebral ischemia. The potent 5-HT1A agonist BAY x 3702, or repinotan, has reduced cortical infarct volume in pre-clinical models even when given 5 hours after injury. Early clinical trials showed that the drug was safe, and displayed primarily serotonergic side effects such as nausea and vomiting. A phase IIb trial in moderate to moderately severe strokes completed enrollment in June 2004.</p>","PeriodicalId":11063,"journal":{"name":"Current drug targets. CNS and neurological disorders","volume":"4 2","pages":"119-20"},"PeriodicalIF":0.0000,"publicationDate":"2005-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1568007053544165","citationCount":"14","resultStr":"{\"title\":\"Repinotan, A 5-HT1A agonist, in the treatment of acute ischemic stroke.\",\"authors\":\"Helmi L Lutsep\",\"doi\":\"10.2174/1568007053544165\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Serotonin agonists can reduce glutamate-induced excitotoxicity in cerebral ischemia. The potent 5-HT1A agonist BAY x 3702, or repinotan, has reduced cortical infarct volume in pre-clinical models even when given 5 hours after injury. Early clinical trials showed that the drug was safe, and displayed primarily serotonergic side effects such as nausea and vomiting. A phase IIb trial in moderate to moderately severe strokes completed enrollment in June 2004.</p>\",\"PeriodicalId\":11063,\"journal\":{\"name\":\"Current drug targets. CNS and neurological disorders\",\"volume\":\"4 2\",\"pages\":\"119-20\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2005-04-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.2174/1568007053544165\",\"citationCount\":\"14\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current drug targets. CNS and neurological disorders\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1568007053544165\",\"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 drug targets. CNS and neurological disorders","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1568007053544165","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 14
摘要
5 -羟色胺激动剂可减轻脑缺血时谷氨酸引起的兴奋毒性。在临床前模型中，强效5- ht1a激动剂BAY x 3702或瑞匹诺坦即使在损伤后5小时给予，也能减少皮质梗死体积。早期临床试验表明，该药是安全的，主要表现为血清素能副作用，如恶心和呕吐。2004年6月，一项针对中度至中度重度中风的IIb期试验完成了入组。
Repinotan, A 5-HT1A agonist, in the treatment of acute ischemic stroke.
Serotonin agonists can reduce glutamate-induced excitotoxicity in cerebral ischemia. The potent 5-HT1A agonist BAY x 3702, or repinotan, has reduced cortical infarct volume in pre-clinical models even when given 5 hours after injury. Early clinical trials showed that the drug was safe, and displayed primarily serotonergic side effects such as nausea and vomiting. A phase IIb trial in moderate to moderately severe strokes completed enrollment in June 2004.
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