Turk J, Needleman P, Marshall G R
J Med Chem. 1975 Nov;18(11):1139-42. doi: 10.1021/jm00245a019.
Three analogs of bradykinin have been synthesized which bear an alpha-methyl group in the place of an alpha proton at position, 4, 5, or 8. Such analogs possess restricted conformational freedom and are of interest for three reasons. (1) They may provide information about the receptor-bound conformation of the peptide. (2) They may provide a route to antagonists of the native peptide. (3) They may be degraded slowly by proteolytic enzymes. None of the analogs described here antagonized the action of bradykinin, but one exhibited tissue specificity and decreased pulmonary inactivation in the rat.
已合成了三种缓激肽类似物，它们在4位、5位或8位上带有α-甲基取代α-质子。这类类似物具有受限的构象自由度，因其三个原因而备受关注。（1）它们可能提供有关该肽与受体结合构象的信息。（2）它们可能提供一条获得天然肽拮抗剂的途径。（3）它们可能被蛋白水解酶缓慢降解。此处描述的类似物均未拮抗缓激肽的作用，但有一种表现出组织特异性并降低了大鼠肺部的失活作用。
