Synthesis, opiate receptor binding and analgesic activity of enkephalin analogues

J Pless, W Bauer, F Cardinaux, A Closse…

文献索引：Pless; Bauer; Cardinaux; et al. Helvetica Chimica Acta, 1979 , vol. 62, # 2 p. 398 - 411

全文：HTML全文

被引用次数: 51

摘要

Abstract The synthesis and biological testing of analogues of Met-enkephalin, a recently discovered opioid peptide from mammalian brain, are described. Testing involved determination of affinity constants for an opiate receptor site and of analgesic potency in the tail-flick test in mouse. The effects on opioid activity of modifying various parts of the enkephalin molecule are discussed. Tyr-D-Ala-Gly-MePheMet (O)-ol 1 (FK 33-824), which ...