{"title":"GABAA受体γ - 2亚基亚型反义寡核苷酸诱导的苯二氮卓类药物在大鼠脑内结合适度降低","authors":"Jesper Karle, Mogens Nielsen","doi":"10.1016/0922-4106(95)90088-8","DOIUrl":null,"url":null,"abstract":"<div><p>The GABA<sub>A</sub> (γ-aminobutyric acid-A) receptor <em>γ</em><sub>2</sub> subunit subtype is functionally integral part of the benzodiazepine binding site of the GABA<sub>A</sub> receptor complex, important for benzodiazepine pharmacology. We have evaluated the possibility of specifically reducing benzodiazepine receptor binding properties in vivo using phosphorothioate antisense oligodeoxynucleotides to inhibit the expression of GABA<sub>A</sub> receptor <em>γ</em><sub>2</sub> subinit subtype. Intracerebroventricular infusions of an antisense oligonucleotide reduced benzodiazepine receptor radioligand binding by 9–15% in specific rat brain regions.</p></div>","PeriodicalId":100502,"journal":{"name":"European Journal of Pharmacology: Molecular Pharmacology","volume":"291 3","pages":"Pages 439-441"},"PeriodicalIF":0.0000,"publicationDate":"1995-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0922-4106(95)90088-8","citationCount":"14","resultStr":"{\"title\":\"Modest reduction of benzodiazepine binding in rat brain in vivo induced by antisense oligonucleotide to GABAA receptor γ2 subunit subtype\",\"authors\":\"Jesper Karle, Mogens Nielsen\",\"doi\":\"10.1016/0922-4106(95)90088-8\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The GABA<sub>A</sub> (γ-aminobutyric acid-A) receptor <em>γ</em><sub>2</sub> subunit subtype is functionally integral part of the benzodiazepine binding site of the GABA<sub>A</sub> receptor complex, important for benzodiazepine pharmacology. We have evaluated the possibility of specifically reducing benzodiazepine receptor binding properties in vivo using phosphorothioate antisense oligodeoxynucleotides to inhibit the expression of GABA<sub>A</sub> receptor <em>γ</em><sub>2</sub> subinit subtype. Intracerebroventricular infusions of an antisense oligonucleotide reduced benzodiazepine receptor radioligand binding by 9–15% in specific rat brain regions.</p></div>\",\"PeriodicalId\":100502,\"journal\":{\"name\":\"European Journal of Pharmacology: Molecular Pharmacology\",\"volume\":\"291 3\",\"pages\":\"Pages 439-441\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1995-11-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0922-4106(95)90088-8\",\"citationCount\":\"14\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Pharmacology: Molecular Pharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/0922410695900888\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Pharmacology: Molecular Pharmacology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/0922410695900888","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Modest reduction of benzodiazepine binding in rat brain in vivo induced by antisense oligonucleotide to GABAA receptor γ2 subunit subtype
The GABAA (γ-aminobutyric acid-A) receptor γ2 subunit subtype is functionally integral part of the benzodiazepine binding site of the GABAA receptor complex, important for benzodiazepine pharmacology. We have evaluated the possibility of specifically reducing benzodiazepine receptor binding properties in vivo using phosphorothioate antisense oligodeoxynucleotides to inhibit the expression of GABAA receptor γ2 subinit subtype. Intracerebroventricular infusions of an antisense oligonucleotide reduced benzodiazepine receptor radioligand binding by 9–15% in specific rat brain regions.
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