【摘要】 用3-N-保护的氨酰基-四氢噻唑-2-硫酮作为新的活泼酰胺合成了保护的促睡眠九肽中的所有片段,最后一步用混合酸酐法合成保护的促睡眠九肽,再经三氟乙酸处理,凝胶柱层析纯化,得到了纯的自由九肽,其物化性质与经典法合成的一致,将其经脑室(5微克/兔)或静脉(50微克/公斤)给家兔注射后引起睡眠,兔脑电图(EEG)均呈现δ及σ波明显增强作用。更多还原

【Abstract】 3-Aminoacyl-tetrahydrothiazole-2-thione (3-Aminoacyl-TTT) was used for the preparation of all the protected fragments of DSIP, which was obtained finally through the coupling of DSIP (1-4) and DSIP (5-9) by the mixed anhydride method. The protected DSIP was deprotected with meicaptoethanol-TFA-CH2Cl2 and then purified on DEAE-sephadex A-25 column. The purified sample was proved to be homogeneous by HPLC, TLC and highvoltage electrophoresis at pH 3.8 and was identical in all respects with that obtained by early method.The physiological activities of the sample were performed on rabbits by using intravenous administration or mesodiencephalic ventricular infusion respectively. Its function of intensifying and waves on rabbits electroencephalog (EEG) was shown clearly. Therefore basic identity between the present sample and those prepared by classical method could be established. It is likely that TTT method will find a useful method for the preparation of biological active peptides.更多还原