{"title":"三功能配体：一种高亲和力的a1腺苷受体的放射性碘化酰化拮抗剂。","authors":"Kenneth A Jacobson, Mark E Olah, Gary L Stiles","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>A new xanthine (adenosine antagonist) radioligand that binds covalently to A<sub>1-</sub>adenosine receptors was prepared and used as a receptor probe. BH-DITC-XAC was synthesized via a trifunctional aryl diisothiocyanate crosslinker. containing the p-hydroxyphenylpropionyl group for radioiodination. The xanthine competed against agonist or antagonist A<sub>1</sub> receptor radioligands in bovine brain membranes with an IC<sub>50</sub>, of 40nM. <sup>125</sup>I-BH-DITC-XAC, prepared directly by the chloramine T method and purified by HPLC. bound specifically to A<sub>1</sub> receptors. This binding was inhibited in the presence of the adenosine agonists <i>R</i>-PIA, <i>S</i>-PIA. and NECA in a dose dependent manner and with the order of potency characteristic of bovine A<sub>1</sub> receptors. Incubation of affinity purified bovine A<sub>1</sub>-receptors with <sup>125</sup>I-BH-DITC-XAC (0.8 nM) for 2 hours resulted in the specific and clean labelling of a polypeptide band corresponding to MW 36,000, identical to that previously found for the A<sub>1</sub> receptor.</p>","PeriodicalId":90677,"journal":{"name":"Pharmacology communications","volume":"1 2","pages":"145-154"},"PeriodicalIF":0.0000,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4217529/pdf/nihms385194.pdf","citationCount":"0","resultStr":"{\"title\":\"TRIFUNCTIONAL LIGANDS: A RADIOIODINATED HIGH AFFINITY ACYLATING ANTAGONIST FOR THE A<sub>1</sub> ADENOSINE RECEPTOR.\",\"authors\":\"Kenneth A Jacobson, Mark E Olah, Gary L Stiles\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>A new xanthine (adenosine antagonist) radioligand that binds covalently to A<sub>1-</sub>adenosine receptors was prepared and used as a receptor probe. BH-DITC-XAC was synthesized via a trifunctional aryl diisothiocyanate crosslinker. containing the p-hydroxyphenylpropionyl group for radioiodination. The xanthine competed against agonist or antagonist A<sub>1</sub> receptor radioligands in bovine brain membranes with an IC<sub>50</sub>, of 40nM. <sup>125</sup>I-BH-DITC-XAC, prepared directly by the chloramine T method and purified by HPLC. bound specifically to A<sub>1</sub> receptors. This binding was inhibited in the presence of the adenosine agonists <i>R</i>-PIA, <i>S</i>-PIA. and NECA in a dose dependent manner and with the order of potency characteristic of bovine A<sub>1</sub> receptors. Incubation of affinity purified bovine A<sub>1</sub>-receptors with <sup>125</sup>I-BH-DITC-XAC (0.8 nM) for 2 hours resulted in the specific and clean labelling of a polypeptide band corresponding to MW 36,000, identical to that previously found for the A<sub>1</sub> receptor.</p>\",\"PeriodicalId\":90677,\"journal\":{\"name\":\"Pharmacology communications\",\"volume\":\"1 2\",\"pages\":\"145-154\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1992-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4217529/pdf/nihms385194.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmacology communications\",\"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":"Pharmacology communications","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
TRIFUNCTIONAL LIGANDS: A RADIOIODINATED HIGH AFFINITY ACYLATING ANTAGONIST FOR THE A1 ADENOSINE RECEPTOR.
A new xanthine (adenosine antagonist) radioligand that binds covalently to A1-adenosine receptors was prepared and used as a receptor probe. BH-DITC-XAC was synthesized via a trifunctional aryl diisothiocyanate crosslinker. containing the p-hydroxyphenylpropionyl group for radioiodination. The xanthine competed against agonist or antagonist A1 receptor radioligands in bovine brain membranes with an IC50, of 40nM. 125I-BH-DITC-XAC, prepared directly by the chloramine T method and purified by HPLC. bound specifically to A1 receptors. This binding was inhibited in the presence of the adenosine agonists R-PIA, S-PIA. and NECA in a dose dependent manner and with the order of potency characteristic of bovine A1 receptors. Incubation of affinity purified bovine A1-receptors with 125I-BH-DITC-XAC (0.8 nM) for 2 hours resulted in the specific and clean labelling of a polypeptide band corresponding to MW 36,000, identical to that previously found for the A1 receptor.
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