{"title":"胍丁氨酸对阿片受体cAMP信号转导系统适应性的影响。","authors":"J Li, X Li, G Pei, B Y Qin","doi":"","DOIUrl":null,"url":null,"abstract":"<p><strong>Aim: </strong>To observe attenuative effects of agmatine on opiate desensitization and substance dependence.</p><p><strong>Methods: </strong>Guanosine 5'-O-(3-[35S] thiotriphosphate) ([35S]GTTP) binding and cellular cyclic AMP (cAMP) level were determined by radioligand binding assay and radioimmunoassay in NG108-15 cells, respectively.</p><p><strong>Results: </strong>Agmatine increased stimulative action of opioids on [35S]GTTP binding by about 35% and inhibitory effects of opioids on cellular cAMP concentration by about 114.3% in NG108-15 cells pretreated with opioids. On the other hand, it also inhibited cAMP over-shooting by 214.9% of morphine substance dependent cells precipitated by naloxone compared with that of control. These effects of agmatine were antagonized by idazoxan in a concentration-dependent manner.</p><p><strong>Conclusion: </strong>Agmatine reversed the formative process of adaptation in cAMP signal transduction cascade.</p>","PeriodicalId":24002,"journal":{"name":"Zhongguo yao li xue bao = Acta pharmacologica Sinica","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"1999-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Influence of agmatine in adaptation of cAMP signal transduction system of opiate receptors.\",\"authors\":\"J Li, X Li, G Pei, B Y Qin\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Aim: </strong>To observe attenuative effects of agmatine on opiate desensitization and substance dependence.</p><p><strong>Methods: </strong>Guanosine 5'-O-(3-[35S] thiotriphosphate) ([35S]GTTP) binding and cellular cyclic AMP (cAMP) level were determined by radioligand binding assay and radioimmunoassay in NG108-15 cells, respectively.</p><p><strong>Results: </strong>Agmatine increased stimulative action of opioids on [35S]GTTP binding by about 35% and inhibitory effects of opioids on cellular cAMP concentration by about 114.3% in NG108-15 cells pretreated with opioids. On the other hand, it also inhibited cAMP over-shooting by 214.9% of morphine substance dependent cells precipitated by naloxone compared with that of control. These effects of agmatine were antagonized by idazoxan in a concentration-dependent manner.</p><p><strong>Conclusion: </strong>Agmatine reversed the formative process of adaptation in cAMP signal transduction cascade.</p>\",\"PeriodicalId\":24002,\"journal\":{\"name\":\"Zhongguo yao li xue bao = Acta pharmacologica Sinica\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1999-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Zhongguo yao li xue bao = Acta pharmacologica Sinica\",\"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":"Zhongguo yao li xue bao = Acta pharmacologica Sinica","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
摘要
目的:观察胍丁氨酸对阿片脱敏和物质依赖的减弱作用。方法:采用放射配体结合法和放射免疫法分别测定NG108-15细胞中鸟苷5′- o -(3-[35S]硫代三磷酸)([35S]GTTP)结合和细胞环AMP (cAMP)水平。结果:Agmatine使阿片样物质对[35S]GTTP结合的刺激作用增加约35%，阿片样物质对NG108-15细胞cAMP浓度的抑制作用增加约114.3%。另一方面，与对照组相比，纳洛酮对吗啡物质依赖细胞cAMP过冲的抑制作用降低了214.9%。胍丁氨酸的这些作用被咪唑嗪以浓度依赖的方式拮抗。结论:胍丁氨酸逆转了cAMP信号转导级联中的适应形成过程。
Influence of agmatine in adaptation of cAMP signal transduction system of opiate receptors.
Aim: To observe attenuative effects of agmatine on opiate desensitization and substance dependence.
Methods: Guanosine 5'-O-(3-[35S] thiotriphosphate) ([35S]GTTP) binding and cellular cyclic AMP (cAMP) level were determined by radioligand binding assay and radioimmunoassay in NG108-15 cells, respectively.
Results: Agmatine increased stimulative action of opioids on [35S]GTTP binding by about 35% and inhibitory effects of opioids on cellular cAMP concentration by about 114.3% in NG108-15 cells pretreated with opioids. On the other hand, it also inhibited cAMP over-shooting by 214.9% of morphine substance dependent cells precipitated by naloxone compared with that of control. These effects of agmatine were antagonized by idazoxan in a concentration-dependent manner.
Conclusion: Agmatine reversed the formative process of adaptation in cAMP signal transduction cascade.
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