{"title":"酮色林对亚二氧基甲基苯丙胺对小鼠体温影响的影响","authors":"J. R. Docherty, S. Bexis","doi":"10.1111/aap.12009","DOIUrl":null,"url":null,"abstract":"<div>\n \n <p>\n \n </p><ol>\n \n \n <li>We have investigated the ability of the 5HT<sub>2</sub>-receptor antagonist ketanserin to affect the hyperthermia produced by methylenedioxymethamphetamine (MDMA) in conscious mice and examined whether α<sub>1</sub>-adrenoceptor antagonist actions are involved.</li>\n \n \n <li>Mice were implanted with intra-abdominal temperature probes under anaesthesia and allowed 2 weeks recovery. MDMA (20 mg kg<sup>−1</sup>) was administered subcutaneously 30 min after vehicle or test antagonist and effects on body temperature monitored by telemetry.</li>\n \n \n <li>Following vehicle, MDMA produced a slowly developing hyperthermia, reaching a maximum increase of 1.24 °C at 150 min postinjection. Ketanserin (0.5 mg kg<sup>−1</sup>) revealed a significant and marked early hypothermia to MDMA, an effect that is mimicked by the α<sub>1</sub>-adrenoceptor antagonist prazosin (0.1 mg kg<sup>−1</sup>).</li>\n \n \n <li>Functional studies revealed antagonist actions of ketanserin at α<sub>1</sub>-adrenoceptors in rat aorta and rat vas deferens <i>in vitro</i> indicative of α<sub>1</sub>-adrenoceptor antagonist actions at the concentration used <i>in vivo</i>.</li>\n \n \n <li>In conclusion, ketanserin (0.5 mg kg<sup>−1</sup>) modulates the hyperthermic actions of MDMA in mice. Although we cannot rule out additional actions at 5HT<sub>2</sub>-receptors, the actions of ketanserin are consistent with α<sub>1</sub>-adrenoceptor antagonism. There is no clear evidence from this study that 5HT<sub>2</sub>-receptors mediate the hyperthermic response to MDMA.</li>\n </ol>\n \n </div>","PeriodicalId":100151,"journal":{"name":"Autonomic and Autacoid Pharmacology","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2013-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/aap.12009","citationCount":"9","resultStr":"{\"title\":\"Influence of ketanserin on the effects of methylenedioxymethamphetamine on body temperature in the mouse\",\"authors\":\"J. R. Docherty, S. 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Ketanserin (0.5 mg kg<sup>−1</sup>) revealed a significant and marked early hypothermia to MDMA, an effect that is mimicked by the α<sub>1</sub>-adrenoceptor antagonist prazosin (0.1 mg kg<sup>−1</sup>).</li>\\n \\n \\n <li>Functional studies revealed antagonist actions of ketanserin at α<sub>1</sub>-adrenoceptors in rat aorta and rat vas deferens <i>in vitro</i> indicative of α<sub>1</sub>-adrenoceptor antagonist actions at the concentration used <i>in vivo</i>.</li>\\n \\n \\n <li>In conclusion, ketanserin (0.5 mg kg<sup>−1</sup>) modulates the hyperthermic actions of MDMA in mice. Although we cannot rule out additional actions at 5HT<sub>2</sub>-receptors, the actions of ketanserin are consistent with α<sub>1</sub>-adrenoceptor antagonism. There is no clear evidence from this study that 5HT<sub>2</sub>-receptors mediate the hyperthermic response to MDMA.</li>\\n </ol>\\n \\n </div>\",\"PeriodicalId\":100151,\"journal\":{\"name\":\"Autonomic and Autacoid Pharmacology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2013-08-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1111/aap.12009\",\"citationCount\":\"9\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Autonomic and Autacoid Pharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1111/aap.12009\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Autonomic and Autacoid Pharmacology","FirstCategoryId":"1085","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1111/aap.12009","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 9
摘要
我们研究了5ht2受体拮抗剂酮色林在清醒小鼠中影响亚甲基二氧基甲基苯丙胺(MDMA)产生的高温的能力，并研究了α1肾上腺素受体拮抗剂的作用是否参与其中。小鼠在麻醉状态下植入腹腔温度探头，恢复2周。MDMA (20mg kg−1)在给药或试验拮抗剂后30分钟皮下注射，并通过遥测监测对体温的影响。载药后，MDMA产生缓慢发展的热疗，在注射后150分钟最大升高1.24°C。酮色林(0.5 mg kg - 1)对MDMA表现出明显的早期低体温，α - 1肾上腺素受体拮抗剂吡唑嗪(0.1 mg kg - 1)也有类似的效果。功能研究显示，酮色林在体外对大鼠主动脉和输精管α1-肾上腺素受体有拮抗作用，表明其在体内具有拮抗α1-肾上腺素受体的作用。综上所述，酮色林(0.5 mg kg−1)可调节MDMA在小鼠体内的高热作用。虽然我们不能排除对5ht2受体的其他作用，但酮色林的作用与α1-肾上腺素受体的拮抗作用是一致的。本研究没有明确的证据表明5ht2受体介导MDMA的高温反应。
Influence of ketanserin on the effects of methylenedioxymethamphetamine on body temperature in the mouse
We have investigated the ability of the 5HT2-receptor antagonist ketanserin to affect the hyperthermia produced by methylenedioxymethamphetamine (MDMA) in conscious mice and examined whether α1-adrenoceptor antagonist actions are involved.
Mice were implanted with intra-abdominal temperature probes under anaesthesia and allowed 2 weeks recovery. MDMA (20 mg kg−1) was administered subcutaneously 30 min after vehicle or test antagonist and effects on body temperature monitored by telemetry.
Following vehicle, MDMA produced a slowly developing hyperthermia, reaching a maximum increase of 1.24 °C at 150 min postinjection. Ketanserin (0.5 mg kg−1) revealed a significant and marked early hypothermia to MDMA, an effect that is mimicked by the α1-adrenoceptor antagonist prazosin (0.1 mg kg−1).
Functional studies revealed antagonist actions of ketanserin at α1-adrenoceptors in rat aorta and rat vas deferens in vitro indicative of α1-adrenoceptor antagonist actions at the concentration used in vivo.
In conclusion, ketanserin (0.5 mg kg−1) modulates the hyperthermic actions of MDMA in mice. Although we cannot rule out additional actions at 5HT2-receptors, the actions of ketanserin are consistent with α1-adrenoceptor antagonism. There is no clear evidence from this study that 5HT2-receptors mediate the hyperthermic response to MDMA.
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