SYNTHETIC PEPTIDE DERIVATIVE

摘要

PURPOSE:To provide a synthetic peptide derivative having a specific amino acid sequence, effective for efficiently inhibiting the insulin-secretion suppressing action of galanin and expected to be useful as a galanin-antagonistic substance for the prevention and treatment of Alzheimer's dementia. CONSTITUTION:A peptide fragment expressed by formula I (Bzl is benzyl; Dnp is protecting group) is dissolved in a mixture of dimethylformamide and dimethyl sulfoxide. The solution is incorporated with triethylamine and then a fragment of formula II under stirring and cooling with ice to effect the uniform dissolution and dispersion of the substances. The product is further incorporated with 1-hydroxybenzotriazole and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride as a condensing agent and made to react with each other by stirring for 3hr under ice cooling and for a night at room temperature. The reaction liquid is poured into ice water to separate the reaction product and the protecting group is removed to obtain the objective synthetic peptide derivative expressed by formula III (AA is Ser or D-Thr; Ala-ol is AlaOH).