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PEI6,大鼠腹膜肥大细胞中的一种新型碱性促分泌素:聚乙烯亚胺PEI6的特性与化合物48/80相似。

PEI6, a new basic secretagogue in rat peritoneal mast cells: characteristics of polyethylenimine PEI6 resemble those of compound 48/80.

作者信息

Suzuki-Nishimura T, Oku N, Nango M, Uchida M K

机构信息

Department of Molecular Pharmacology, Meiji College of Pharmacy, Tokyo, Japan.

出版信息

Gen Pharmacol. 1995 Oct;26(6):1171-8. doi: 10.1016/0306-3623(95)99001-x.

Abstract
  1. Polyethylenimine with a molecular weight of 600 (PEI6) was the simplest and the most useful to investigate mast cell-activating mechanisms via pertussis toxin (IAP)-sensitive G protein pathway. 2. IAP, lidocaine, or dibutyryl cyclic AMP were inhibitors of the histamine release induced by PEI6, but anti-allergic drug DSCG, the calcium antagonist, D-600, kinase inhibitors, H-7 and K252a, or the calmodulin inhibitor, W-7 were not. 3. The additive effects of compound 48/80 and PEI6 suggested that the action sites for PEI6 overlapped the binding sites of compound 48/80. 4. Mast cell activation induced by PEI6 was sugar-specifically inhibited by N-acetylglucosamine(Glc-NAc)-specific lectins and/or by sialic acid (Sia)-specific lectins, suggesting that the action sites for PEI6 were glycoproteins having GlcNAc and/or Sia residues. 5. Four glycoproteins seemed to be involved in histamine release, including the IAP-sensitive G-protein pathway.
摘要
  1. 分子量为600的聚乙烯亚胺(PEI6)是通过百日咳毒素(IAP)敏感的G蛋白途径研究肥大细胞激活机制时最简单且最有用的物质。2. IAP、利多卡因或二丁酰环磷腺苷是PEI6诱导的组胺释放的抑制剂,但抗过敏药物色甘酸钠、钙拮抗剂D-600、激酶抑制剂H-7和K252a或钙调蛋白抑制剂W-7则不是。3. 化合物48/80和PEI6的相加作用表明,PEI6的作用位点与化合物48/80的结合位点重叠。4. PEI6诱导的肥大细胞激活被N-乙酰葡糖胺(Glc-NAc)特异性凝集素和/或唾液酸(Sia)特异性凝集素糖特异性抑制,这表明PEI6的作用位点是具有GlcNAc和/或Sia残基的糖蛋白。5. 四种糖蛋白似乎参与了组胺释放,包括IAP敏感的G蛋白途径。

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