【摘要】 用液相合成方法合成了具有镇痛作用的μ阿片受体的内源性配体——内吗啡肽 - 1(endomorphin- 1 ) ,该四肽为 Tyr- Pro- Trp- Phe NH2 .液相合成法是在氨基酸的 N端用 Boc(叔丁氧羰酰基 )作保护基 ,C端用 HOSu(N-羟基琥珀酰亚胺 )活化 ,与未加保护基的氨基酸在碱性条件下接肽 .先分别合成 C端二肽和 N端二肽 ,再缩合为四肽 ,产物的保护基用盐酸脱帽去除 .中间产物用薄层层析和熔点鉴定其纯度 ,最终得到了高纯度的四肽 .小白鼠脑室注射 (i.c.v)测定表明 ,8.2 5nmol剂量给药 ,其镇痛活性为 87% ,明显高于吗啡 (morphine) .更多还原

【Abstract】 Endomorphin 1(Tyr Pro Trp Phe NH 2,EM 1)has been identified as a novel opiate peptide in mammalian brain recently,which has the highest affinity and specificity for the μ opiate receptor found so far.The synthesis of the endomorphin 1 was described by the liquid phase condensation.C terminal dipeptide and N terminal dipeptide have been synthesized firstly using the liquid phase condensation and then coupled successively.Pure endomorphin 1 was obtained finally.Test of mouse ventricle show that synthetic endomorphin 1 has 87% effect of analgesia in dose of 8.25 nmol,which is much more effective than morphine.更多还原