Małgorzata Dukat, Richard A. Glennon, Shawquia Young
{"title":"MD-354:它有什么用?","authors":"Małgorzata Dukat, Richard A. Glennon, Shawquia Young","doi":"10.1111/j.1527-3458.2007.00002.x","DOIUrl":null,"url":null,"abstract":"<p>MD-354 (<i>meta</i>-chlorophenylguanidine) has been identified as a member of a novel class of 5-HT<sub>3</sub> serotonin receptor agonists. MD-354 is a 5-HT<sub>3</sub> receptor partial agonist that has been shown to behave as an agonist in some assays, and as an antagonist in others. MD-354 also binds at α-adrenoceptors (ARs) and displays an affinity for α<sub>2B</sub>-ARs comparable to its affinity for 5-HT<sub>3</sub> receptors. Although devoid of antinociceptive actions following systemic administration alone, MD-354 markedly enhances the antinociceptive actions of clonidine in the mouse tail-flick assay without potentiating the sedative side effects of clonidine. Although studies with MD-354 are still in progress, some pharmacological findings are described here. MD-354-related agents may represent drug adjuvants for the relief of severe pain.</p>","PeriodicalId":94307,"journal":{"name":"CNS drug reviews","volume":"13 1","pages":"1-20"},"PeriodicalIF":0.0000,"publicationDate":"2007-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1527-3458.2007.00002.x","citationCount":"16","resultStr":"{\"title\":\"MD-354: What is It Good For?\",\"authors\":\"Małgorzata Dukat, Richard A. Glennon, Shawquia Young\",\"doi\":\"10.1111/j.1527-3458.2007.00002.x\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>MD-354 (<i>meta</i>-chlorophenylguanidine) has been identified as a member of a novel class of 5-HT<sub>3</sub> serotonin receptor agonists. MD-354 is a 5-HT<sub>3</sub> receptor partial agonist that has been shown to behave as an agonist in some assays, and as an antagonist in others. MD-354 also binds at α-adrenoceptors (ARs) and displays an affinity for α<sub>2B</sub>-ARs comparable to its affinity for 5-HT<sub>3</sub> receptors. Although devoid of antinociceptive actions following systemic administration alone, MD-354 markedly enhances the antinociceptive actions of clonidine in the mouse tail-flick assay without potentiating the sedative side effects of clonidine. Although studies with MD-354 are still in progress, some pharmacological findings are described here. MD-354-related agents may represent drug adjuvants for the relief of severe pain.</p>\",\"PeriodicalId\":94307,\"journal\":{\"name\":\"CNS drug reviews\",\"volume\":\"13 1\",\"pages\":\"1-20\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2007-04-24\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1111/j.1527-3458.2007.00002.x\",\"citationCount\":\"16\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"CNS drug reviews\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2007.00002.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://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2007.00002.x","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
MD-354 (meta-chlorophenylguanidine) has been identified as a member of a novel class of 5-HT3 serotonin receptor agonists. MD-354 is a 5-HT3 receptor partial agonist that has been shown to behave as an agonist in some assays, and as an antagonist in others. MD-354 also binds at α-adrenoceptors (ARs) and displays an affinity for α2B-ARs comparable to its affinity for 5-HT3 receptors. Although devoid of antinociceptive actions following systemic administration alone, MD-354 markedly enhances the antinociceptive actions of clonidine in the mouse tail-flick assay without potentiating the sedative side effects of clonidine. Although studies with MD-354 are still in progress, some pharmacological findings are described here. MD-354-related agents may represent drug adjuvants for the relief of severe pain.