β‐Endorphin: synthesis and properties of human β‐endorphin‐(1–28) and its analogs

Abstract
Three analogs of human .beta.-endorphin (.beta.h-EP) were synthesized by the solid-phase 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 [in mice] were as follows: .beta.h-EP; 100; I, 18; II, 36; III, 13.

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