{"title":"2-(2-氨基乙基)-喹啉(D-1997):一种与偏头痛治疗相关的脑血管5-HT1受体的新型激动剂","authors":"J. Terron","doi":"10.1111/J.1527-3458.2000.TB00152.X","DOIUrl":null,"url":null,"abstract":"The functional pharmacological properties of a group of quinoline-derivatives were screened for agonist activity at 5-HT1-like receptors mediating vasoconstriction. In experimental models predictive of antimigraine activity, 2-(2-aminoethyl) quinoline hydrochloride (D-1997) exhibited higher potency and efficacy at vasoconstrictor 5-HT1-like receptors than quipazine. D-1997 was also found to activate a novel vasoconstrictor mechanism in the carotid circulation. It is suggested D-1997 may represent a useful lead in the search for better acute antimigraine therapies.","PeriodicalId":10499,"journal":{"name":"CNS drug reviews","volume":"14 1","pages":"267-277"},"PeriodicalIF":0.0000,"publicationDate":"2006-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":"{\"title\":\"2-(2-aminoethyl)-quinoline (D-1997): A Novel Agonist at Craniovascular 5-HT1 Receptors Relevant to Migraine Therapy\",\"authors\":\"J. Terron\",\"doi\":\"10.1111/J.1527-3458.2000.TB00152.X\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The functional pharmacological properties of a group of quinoline-derivatives were screened for agonist activity at 5-HT1-like receptors mediating vasoconstriction. In experimental models predictive of antimigraine activity, 2-(2-aminoethyl) quinoline hydrochloride (D-1997) exhibited higher potency and efficacy at vasoconstrictor 5-HT1-like receptors than quipazine. D-1997 was also found to activate a novel vasoconstrictor mechanism in the carotid circulation. It is suggested D-1997 may represent a useful lead in the search for better acute antimigraine therapies.\",\"PeriodicalId\":10499,\"journal\":{\"name\":\"CNS drug reviews\",\"volume\":\"14 1\",\"pages\":\"267-277\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2006-06-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"CNS drug reviews\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1111/J.1527-3458.2000.TB00152.X\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"CNS drug reviews","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1111/J.1527-3458.2000.TB00152.X","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
2-(2-aminoethyl)-quinoline (D-1997): A Novel Agonist at Craniovascular 5-HT1 Receptors Relevant to Migraine Therapy
The functional pharmacological properties of a group of quinoline-derivatives were screened for agonist activity at 5-HT1-like receptors mediating vasoconstriction. In experimental models predictive of antimigraine activity, 2-(2-aminoethyl) quinoline hydrochloride (D-1997) exhibited higher potency and efficacy at vasoconstrictor 5-HT1-like receptors than quipazine. D-1997 was also found to activate a novel vasoconstrictor mechanism in the carotid circulation. It is suggested D-1997 may represent a useful lead in the search for better acute antimigraine therapies.