| 新皮啡肽I(DELI)类似物的合成及构效关系研究 |
| |
| 引用本文： | 胡晓愚,王锐,嘉庆,王勤.新皮啡肽I(DELI)类似物的合成及构效关系研究[J].药学学报,1995,30(9):679-684. |
| |
| 作者姓名： | 胡晓愚 王锐 嘉庆 王勤 |
| |
| 作者单位： | 兰州大学生物系，兰州应用有机化学国家重点实验室 |
| |
| 基金项目： | 国家自然科学基金、国家教委资助优秀年轻教师基金，博士点专项基金 |
| |
| 摘 要： | 用固相多肽合成法合成了类阿片肽新皮啡肽I(DELI)及其三个类似物(将Asp4从5位到7位逐一后移)。实验发现DELI在离体条件(浓度范围10-14～10mol·L-1)和在体条件(剂量范围0.5～5μg·kg-1)下能提高红细胞玫瑰花环形成细胞百分率(E-RFC)和红细胞C3b受体花环百分率(RBC-CR1),且可被纳洛酮阻断。这些结果表明DELI能提高大鼠免疫功能。实验还发现DELI及其类似物的镇痛和免疫活性次序(由大到小)分别是Asp4,Asp7,Asp5,Asp6和Asp4,Asp7,Asp6,Asp5。
|
| 关 键 词： | 新皮啡肽I 固相多肽合成 红细胞免疫功能 纳洛酮 镇痛 |
| 收稿时间： | 1994-10-05 |
STUDIES ON THE SYNTHESIS AND STRUCTURE-ACTIVITY RELATION OF DELTORPHIN I ANALOGUES |
| |
| XY Hu,R Wang,Q Jia and Q Wang.STUDIES ON THE SYNTHESIS AND STRUCTURE-ACTIVITY RELATION OF DELTORPHIN I ANALOGUES[J].Acta Pharmaceutica Sinica,1995,30(9):679-684. |
| |
| Authors: | XY Hu R Wang Q Jia and Q Wang |
| |
| Abstract: | Endogenous opioid deltorphin I(DEL I)and its three analogues(progressive,stepwise repositioning of Asp from 5 to 7)were synthesized solid phase method. DEL I at 10-14～10-10 mol·L-1 in vitro and at 0.5～5μg·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).Thisaugmentative effect of DEL I was antagonized by naloxone. The results indicate that DEL I enhancedthe immune function of rats. The order(from strong to weak)of the analgesic and immune activitywas shown to be Asp4, Asp7, Asp5,Asp6 and Asp4,asp7,Asp6,Asp5 respectively. |
| |
| Keywords: | Deltorphin I Solid phase peptide synthesis Red cell immune function Naloxone Analgesia |
| 本文献已被 CNKI 等数据库收录！ |
| 点击此处可从《药学学报》浏览原始摘要信息 |
| 点击此处可从《药学学报》下载免费的PDF全文 |
|
