Tomomi Shimizu, Toshiyuki Kimura, Tatsuya Funahashi, Kazuhito Watanabe, Ing Kang Ho, Ikuo Yamamoto
{"title":"N3-(2'，5'-二甲氧基苯酰基)阿拉伯糖脲嘧啶对大鼠脑内阿片受体结合配体的置换作用。","authors":"Tomomi Shimizu, Toshiyuki Kimura, Tatsuya Funahashi, Kazuhito Watanabe, Ing Kang Ho, Ikuo Yamamoto","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>N3-(2',5 '-Dimethoxyphenacyl)arabinofuranosyluracil (N3-(2',5 '-DiMeOPhAc)AraU) is a pyrimidine nucleoside derivative which possesses antinociceptive effect by intracerebroventricular (i.c.v.) administration to mice. The compound (100 microM) significantly decreased the specific binding of [3H]D-Ala2, N-Me-Phe4, Gly5-ol-enkephalin (DAMGO) and [3H]D-Pen2, D-Pen5-enkephalin (DPDPE) at the mu- and delta-opioid receptor, respectively, but has no effect on the binding of [3H]U-69,593 at the kappa-opioid receptor of rat brain slices. The autoradiographic studies also demonstrated that [3H]DAMGO and [3H]DPDPE bindings on the rat brain slice were displaced by N3-(2',5'-DiMeOPhAc)AraU. These results indicate that N3-(2',5'-DiMeOPhAc)AraU interacts with mu- and delta-opioid receptors.</p>","PeriodicalId":21045,"journal":{"name":"Research communications in molecular pathology and pharmacology","volume":"117-118 ","pages":"105-13"},"PeriodicalIF":0.0000,"publicationDate":"2005-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Displacement of opioid receptor binding ligands from the rat brain by N3-(2',5'-dimethoxyphenacyl) arabinofuranosyluracil.\",\"authors\":\"Tomomi Shimizu, Toshiyuki Kimura, Tatsuya Funahashi, Kazuhito Watanabe, Ing Kang Ho, Ikuo Yamamoto\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>N3-(2',5 '-Dimethoxyphenacyl)arabinofuranosyluracil (N3-(2',5 '-DiMeOPhAc)AraU) is a pyrimidine nucleoside derivative which possesses antinociceptive effect by intracerebroventricular (i.c.v.) administration to mice. The compound (100 microM) significantly decreased the specific binding of [3H]D-Ala2, N-Me-Phe4, Gly5-ol-enkephalin (DAMGO) and [3H]D-Pen2, D-Pen5-enkephalin (DPDPE) at the mu- and delta-opioid receptor, respectively, but has no effect on the binding of [3H]U-69,593 at the kappa-opioid receptor of rat brain slices. The autoradiographic studies also demonstrated that [3H]DAMGO and [3H]DPDPE bindings on the rat brain slice were displaced by N3-(2',5'-DiMeOPhAc)AraU. These results indicate that N3-(2',5'-DiMeOPhAc)AraU interacts with mu- and delta-opioid receptors.</p>\",\"PeriodicalId\":21045,\"journal\":{\"name\":\"Research communications in molecular pathology and pharmacology\",\"volume\":\"117-118 \",\"pages\":\"105-13\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2005-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Research communications in molecular pathology and pharmacology\",\"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":"Research communications in molecular pathology and pharmacology","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Displacement of opioid receptor binding ligands from the rat brain by N3-(2',5'-dimethoxyphenacyl) arabinofuranosyluracil.
N3-(2',5 '-Dimethoxyphenacyl)arabinofuranosyluracil (N3-(2',5 '-DiMeOPhAc)AraU) is a pyrimidine nucleoside derivative which possesses antinociceptive effect by intracerebroventricular (i.c.v.) administration to mice. The compound (100 microM) significantly decreased the specific binding of [3H]D-Ala2, N-Me-Phe4, Gly5-ol-enkephalin (DAMGO) and [3H]D-Pen2, D-Pen5-enkephalin (DPDPE) at the mu- and delta-opioid receptor, respectively, but has no effect on the binding of [3H]U-69,593 at the kappa-opioid receptor of rat brain slices. The autoradiographic studies also demonstrated that [3H]DAMGO and [3H]DPDPE bindings on the rat brain slice were displaced by N3-(2',5'-DiMeOPhAc)AraU. These results indicate that N3-(2',5'-DiMeOPhAc)AraU interacts with mu- and delta-opioid receptors.
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