Drew D. D'Angelo , Takayuki Terasawa , Steven J. Carlisle , Gerald W. Dorn II , Kevin R. Lynch
{"title":"大鼠肾血栓素A2受体的表征:对激动剂配体I-BOP的高亲和力","authors":"Drew D. D'Angelo , Takayuki Terasawa , Steven J. Carlisle , Gerald W. Dorn II , Kevin R. Lynch","doi":"10.1016/S0090-6980(96)00091-3","DOIUrl":null,"url":null,"abstract":"<div><p>We have cloned a rat kidney thromboxane A2 receptor (TP) cDNA. This receptor was shown to be functional in that the thromboxane A<sub>2</sub> mimetics, U46619 and 1-BOP, elicited calcium transients in Xenopus oocytes and HEK293 cells expressing the TP receptor, respectively. Comparison of the affinities of the rat and human TP sites for the agonist radioligand [<sup>125</sup>I]BOP showed that the rat TP site has about a ten-fold higher affinity for this drug (K<sub>D</sub> = 0.5 vs. 4.4 nM) while the affinities of the two sites for other compound (U46619, I-PTH-OH) were the same. Our results are significant in that they identify a cloned TP as having a picomolar affinity for [<sup>125</sup>I]BOP.</p></div>","PeriodicalId":20653,"journal":{"name":"Prostaglandins","volume":"52 4","pages":"Pages 303-316"},"PeriodicalIF":0.0000,"publicationDate":"1996-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0090-6980(96)00091-3","citationCount":"12","resultStr":"{\"title\":\"Characterization of a rat kidney thromboxane A2 receptor: High affinity for the agonist ligand I-BOP\",\"authors\":\"Drew D. D'Angelo , Takayuki Terasawa , Steven J. Carlisle , Gerald W. Dorn II , Kevin R. Lynch\",\"doi\":\"10.1016/S0090-6980(96)00091-3\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>We have cloned a rat kidney thromboxane A2 receptor (TP) cDNA. This receptor was shown to be functional in that the thromboxane A<sub>2</sub> mimetics, U46619 and 1-BOP, elicited calcium transients in Xenopus oocytes and HEK293 cells expressing the TP receptor, respectively. Comparison of the affinities of the rat and human TP sites for the agonist radioligand [<sup>125</sup>I]BOP showed that the rat TP site has about a ten-fold higher affinity for this drug (K<sub>D</sub> = 0.5 vs. 4.4 nM) while the affinities of the two sites for other compound (U46619, I-PTH-OH) were the same. Our results are significant in that they identify a cloned TP as having a picomolar affinity for [<sup>125</sup>I]BOP.</p></div>\",\"PeriodicalId\":20653,\"journal\":{\"name\":\"Prostaglandins\",\"volume\":\"52 4\",\"pages\":\"Pages 303-316\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1996-10-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/S0090-6980(96)00091-3\",\"citationCount\":\"12\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Prostaglandins\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0090698096000913\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Prostaglandins","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0090698096000913","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 12
摘要
我们克隆了一个大鼠肾血栓素A2受体(TP) cDNA。该受体被证明是功能性的，因为血栓素A2模拟物U46619和1-BOP分别在表达TP受体的爪蟾卵母细胞和HEK293细胞中引起钙瞬变。比较大鼠和人TP位点对激动剂放射性配体[125I]BOP的亲和力，发现大鼠TP位点对该药物的亲和力高约10倍(KD = 0.5 vs. 4.4 nM)，而对其他化合物(U46619, I-PTH-OH)的亲和力相同。我们的结果很重要，因为他们鉴定出克隆的TP对[125I]BOP具有皮摩尔亲和力。
Characterization of a rat kidney thromboxane A2 receptor: High affinity for the agonist ligand I-BOP
We have cloned a rat kidney thromboxane A2 receptor (TP) cDNA. This receptor was shown to be functional in that the thromboxane A2 mimetics, U46619 and 1-BOP, elicited calcium transients in Xenopus oocytes and HEK293 cells expressing the TP receptor, respectively. Comparison of the affinities of the rat and human TP sites for the agonist radioligand [125I]BOP showed that the rat TP site has about a ten-fold higher affinity for this drug (KD = 0.5 vs. 4.4 nM) while the affinities of the two sites for other compound (U46619, I-PTH-OH) were the same. Our results are significant in that they identify a cloned TP as having a picomolar affinity for [125I]BOP.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
