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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) .
The endomorphic ligand 1 (endomorphin-1) of mu opioid receptor with analgesic activity was synthesized by a liquid phase method and the tetrapeptide was Tyr-Pro-Trp-Phe NH2. Synthetic method is the N-terminal amino acid with Boc (tert-butoxycarbonyl) as a protective group, C terminal HOSu (N-hydroxysuccinimide) activation, and the unprotected amino acids in alkaline conditions peptide First, the C-terminal dipeptide and the N-terminal dipeptide were respectively synthesized and then condensed into the tetrapeptide, the protective group of the product was removed by removing the cap with hydrochloric acid, the purity of the intermediate was identified by TLC and melting point, finally the high-purity tetrapeptide The intracerebroventricular (icv) injection in mice showed that the analgesic activity of 8.2 5 nmol was 87%, which was significantly higher than that of morphine.