Fukuda M, Beechan C M, Verlander M, Goodman M, Khan M M, Melmon K L
Int J Pept Protein Res. 1987 Mar;29(3):300-17. doi: 10.1111/j.1399-3011.1987.tb02258.x.
A series of novel catecholamine derivatives has been prepared in which one of the N-methyl substituents of isoproterenol has been extended by a spacer consisting of a chain of four methylenes which terminates with an amide linkage to a peptide, the point of attachment being via the aromatic amino group of p-aminophenylalanine. In one of the derivatives, two catecholamines are attached to the same peptide in this manner. The peptides, which range in size from three to eight amino acid residues and contain phenylalanine, glycine, and L-alpha-amino-delta-hydroxyvaleric acid, were synthesized via stepwise and fragment condensation techniques. The beta-adrenergic agonist activities of the derivatives were evaluated in vitro by measuring the intracellular accumulation of cyclic AMP in S49 mouse lymphoma cells.
已经制备了一系列新型儿茶酚胺衍生物，其中异丙肾上腺素的一个N - 甲基取代基通过由四个亚甲基链组成的间隔基进行了延伸，该间隔基以酰胺键连接到肽上，连接点是通过对氨基苯丙氨酸的芳香氨基。在其中一种衍生物中，两个儿茶酚胺以这种方式连接到同一肽上。这些肽的大小从三到八个氨基酸残基不等，包含苯丙氨酸、甘氨酸和L-α-氨基-δ-羟基戊酸，通过逐步和片段缩合技术合成。通过测量S49小鼠淋巴瘤细胞中环状AMP的细胞内积累，在体外评估了这些衍生物的β-肾上腺素能激动剂活性。
