{"title":"大鼠胃底5 -羟色胺2B (5HT 2B)收缩受体四氢β-卡泊碱拮抗剂的定量构效关系研究","authors":"P. Singh, Rajesh Kumar","doi":"10.1080/14756360127570","DOIUrl":null,"url":null,"abstract":"The antagonist actions of three sub-series of tetrahydro- β -carbolines at the serotonin 2B (5HT 2B) contractile receptor in the rat stomach fundus are analyzed in relation to the physicochemical properties of the molecules. Significant correlations are obtained between the 5HT 2B receptor antagonist affinity and the hydrophobic, steric, electronic, hydrogen bond acceptor and some indicator variables of substituents. Based on these findings, the mode of actions of these congeneric series and future strategy to synthesize more potential compounds are discussed.","PeriodicalId":15776,"journal":{"name":"Journal of enzyme inhibition","volume":"1 1","pages":"491 - 497"},"PeriodicalIF":0.0000,"publicationDate":"2001-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"6","resultStr":"{\"title\":\"Quantitative Structure-Activity Relationship Study on Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT 2B) Contractile Receptor in the Rat Stomach Fundus\",\"authors\":\"P. Singh, Rajesh Kumar\",\"doi\":\"10.1080/14756360127570\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The antagonist actions of three sub-series of tetrahydro- β -carbolines at the serotonin 2B (5HT 2B) contractile receptor in the rat stomach fundus are analyzed in relation to the physicochemical properties of the molecules. Significant correlations are obtained between the 5HT 2B receptor antagonist affinity and the hydrophobic, steric, electronic, hydrogen bond acceptor and some indicator variables of substituents. Based on these findings, the mode of actions of these congeneric series and future strategy to synthesize more potential compounds are discussed.\",\"PeriodicalId\":15776,\"journal\":{\"name\":\"Journal of enzyme inhibition\",\"volume\":\"1 1\",\"pages\":\"491 - 497\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2001-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"6\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of enzyme inhibition\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1080/14756360127570\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of enzyme inhibition","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/14756360127570","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Quantitative Structure-Activity Relationship Study on Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT 2B) Contractile Receptor in the Rat Stomach Fundus
The antagonist actions of three sub-series of tetrahydro- β -carbolines at the serotonin 2B (5HT 2B) contractile receptor in the rat stomach fundus are analyzed in relation to the physicochemical properties of the molecules. Significant correlations are obtained between the 5HT 2B receptor antagonist affinity and the hydrophobic, steric, electronic, hydrogen bond acceptor and some indicator variables of substituents. Based on these findings, the mode of actions of these congeneric series and future strategy to synthesize more potential compounds are discussed.
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