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Motilin-like peptide compound that has a transmucosal absorption susceptibility imparted thereto

机译:赋予胃粘膜吸收敏感性的胃动素样肽化合物

摘要

A compound comprising the sequence represented by the following general formula 1: X1 Val X2 Ile Phe Thr Tyr Gly X3 Leu Gln Arg X4 Gln Glu Lys Glu Arg X5 Lys Pro Gln (formula 1) [in which all linkages between amino acids, except for the X1-Val bond, they are amide bonds; the X1-Val bond is an amide bond or a bond represented by the following formula 2 ** Formula ** X1 is phenylalanine, ß-homophenylglycine or acetylnaphthylalanine; X2 is proline or sarcosine; X3 is glutamic acid or aspartic acid; X4 is methionine or leucine; X5 is asparagine or proline] or a pharmaceutically acceptable salt thereof, in which the compound has a motilin-like activity that stimulates gastrointestinal motility and shows a higher absorption efficiency after transmucosal administration compared to native motilin
机译:包含以下通式所示序列的化合物:X1 Val X2 Ile Phe Thr Tyr Gly X3 Leu Gln Arg X4 Gln Glu Lys Glu Arg X5 Lys Pro Gln(式1)[其中氨基酸之间的所有键合,但X1-Val键,它们是酰胺键; X1-Val键是酰胺键或下式2表示的键。**式** X1是苯丙氨酸,β-高苯基甘氨酸或乙酰基萘丙氨酸; X 2是脯氨酸或肌氨酸; X3是谷氨酸或天冬氨酸; X4是蛋氨酸或亮氨酸; X5是天冬酰胺或脯氨酸]或其药学上可接受的盐,其中所述化合物具有胃动素样活性,与天然胃动素相比,其刺激肠胃蠕动并在经粘膜给药后显示出更高的吸收效率。

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