Synthesis and biological evaluation of analogs of Pro-Leu-Gly-NH2 modified at the leucyl residue
作者:Rodney L. Johnson、Roger J. Bontems、Kaipeen E. Yang、Ram K. Mishra
DOI:10.1021/jm00168a045
日期:1990.6
analogues were tested for their ability to enhance the binding of the dopamine receptor agonist 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (ADTN) to striatal dopamine receptors. Two of the above analogues, Pro-Ahx-Gly-NH2 (3) and Pro-Phe-Gly-NH2 (6), showed significant activity in this assay system. Pro-Ahx-Gly-NH2 produced a 16% enhancement of ADTN binding at 0.1 microM, while Pro-Phe-Gly-NH2
Pro-Leu-Gly-NH2(PLG)的一系列类似物,其中亮氨酸残基已被脂族氨基酸L-异亮氨酸,L-2-氨基己酸(Ahx),L-2-氨基戊酸和已经合成了L-2-氨基丁酸和芳族氨基酸L-苯基丙氨酸,L-苯基甘氨酸,L-和D-2-氨基-4-苯基丁酸,LO-甲基酪氨酸和L-4-硝基苯基丙氨酸。测试了这些类似物增强多巴胺受体激动剂2-氨基-6,7-二羟基-1,2,3,4-四氢萘(ADTN)与纹状体多巴胺受体结合的能力。上述两个类似物Pro-Ahx-Gly-NH2(3)和Pro-Phe-Gly-NH2(6)在此测定系统中显示出显着活性。Pro-Ahx-Gly-NH2在0.1 microM时可提高16%的ADTN结合力,