Garzia R, Yamashiro D, Li C H, Nicolas P
Int J Pept Protein Res. 1982 Sep;20(3):194-8. doi: 10.1111/j.1399-3011.1982.tb03049.x.
Three analogs of human beta-endorphin (beta h-EP) were synthesized by the solid-phage method: beta h-EP-(1--28) (I). [Gln8]-beta h-EP-(1--28) (II), and [D-Ala2, Gln8]-beta h-EP-(1--28) (III). Radioreceptor binding assay with use of tritiated beta h-EP as primary ligand gave relative potencies as follows: beta h-EP, 100; I, 85; II, 380; III, 146. Relative potencies in an analgesic assay were: beta h-EP; 100; I, 18; II, 36; III, 13.
采用固相噬菌体法合成了三种人β-内啡肽(βh-EP)类似物:βh-EP-(1 - 28)(I)、[Gln8]-βh-EP-(1 - 28)(II)和[D-Ala2, Gln8]-βh-EP-(1 - 28)(III)。以氚标记的βh-EP作为主要配体进行放射受体结合试验,得到的相对效价如下:βh-EP为100;I为85;II为380;III为146。镇痛试验中的相对效价为:βh-EP为100;I为18;II为36;III为13。