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[强啡肽 I 类似物的合成及构效关系研究]

[Studies on the synthesis and structure-activity relation of deltorphin I analogues].

作者信息

Hu X Y, Wang R, Jia Q, Wang Q

机构信息

Department of Biology, Lanzhou University.

出版信息

Yao Xue Xue Bao. 1995;30(9):679-84.

PMID:8701744
Abstract

Endogenous opioid deltorphin I (DEL I) and its three analogues (progressive, stepwise repositioning of Asp from 5 to 7) were synthesized by solid phase method. DEL I at 10(-14)-10(-10) mol.L-1 in vitro and at 0.5-5 micrograms.kg-1 in vivo was found to increase the percentages of erythrocyte rosette forming cells (E-RFC) and red blood cell C3b receptor garland (RBC-CR1). This augmentative effect of DEL I was antagonized by naloxone. The results indicate that DEL I enhanced the immune function of rats. The order (from strong to weak) of the analgesic and immune activity was shown to be Asp4, Asp7, Asp5, Asp6 and Asp4, Asp7, Asp6, Asp5 respectively.

摘要

采用固相法合成了内源性阿片肽δ-内啡肽I(DEL I)及其三种类似物(天冬氨酸从5位逐步重新定位到7位)。发现在体外10⁻¹⁴ - 10⁻¹⁰ mol·L⁻¹浓度的DEL I以及体内0.5 - 5微克·千克⁻¹剂量时,红细胞玫瑰花结形成细胞(E-RFC)和红细胞C3b受体花环(RBC-CR1)的百分比增加。DEL I的这种增强作用被纳洛酮拮抗。结果表明,DEL I增强了大鼠的免疫功能。镇痛和免疫活性的顺序分别为天冬氨酸4、天冬氨酸7、天冬氨酸5、天冬氨酸6和天冬氨酸4、天冬氨酸7、天冬氨酸6、天冬氨酸5(从强到弱)。

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