催产素的构象偏向类似物。

Conformationally biased analogs of oxytocin.

作者信息

Lebl M, Toth G, Slaninová J, Hruby V J

机构信息

Institute of Organic Chemistry and Biochemistry, Czechoslovak Academy of Sciences, Prague.

出版信息

Int J Pept Protein Res. 1992 Aug;40(2):148-51. doi: 10.1111/j.1399-3011.1992.tb01463.x.

DOI:10.1111/j.1399-3011.1992.tb01463.x

PMID:1446971

Abstract

Four diastereomeric analogs of oxytocin containing substituted phenylalanine in position 2 were synthesized. This modified phenylalanine side chain contained one methyl group attached to the beta-carbon and the second one at the 2' position of the aromatic ring. All analogs were found to be inhibitors of uterotonic activity of oxytocin with pA2 values ranging from 6.0 to 8.3; the most potent one (pA2 = 8.3) contained dimethylphenylalanine of the D-erythro configuration.

摘要

合成了4种在2位含有取代苯丙氨酸的催产素非对映体类似物。这种修饰的苯丙氨酸侧链在β-碳上连接有一个甲基，在芳环的2'位连接有第二个甲基。发现所有类似物都是催产素子宫收缩活性的抑制剂，其pA2值范围为6.0至8.3；最有效的一种（pA2 = 8.3）含有D-赤藓糖构型的二甲基苯丙氨酸。