Cyclic polypeptides having mu-receptor specificity

作者: Victor J. Hruby , John T. Pelton

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摘要: Novel compounds which are capable of binding with enhanced specificity to the mu opioid receptor disclosed. The analogs somatostain and have formula: ##STR1## wherein X is CONH 2 or CH OH; Y Z independently sulfur ; R 1 , may be same different, hydrogen, methyl, ethyl, cyclopentamethylene, a lower alkyl group having five less carbon atoms; 3 4 atoms, provided, however, that not all hydrogen; AA Phe, D-Phe, phenyl-Gly, D-phenyl-Gly, Tyr, D-Tyr, L-1-Naphthylalanine, D-1-Naphthylalanine, D-Phe(4-Me); Tyr(OMe), Phe(4-Me), Tyr(OEt), Phe(4-Et); Lys, Arg, Orn homo-Arg. novel antagonist activity used induce pharmacological therapeutic effects in humans other animals.

参考文章(4)
Dimitrios Sarantakis, Octapeptides lowering growth hormone ,(1980)
R. Maurer, B. H. Gaehwiler, H. H. Buescher, R. C. Hill, D. Roemer, Opiate antagonistic properties of an octapeptide somatostatin analog Proceedings of the National Academy of Sciences of the United States of America. ,vol. 79, pp. 4815- 4817 ,(1982) , 10.1073/PNAS.79.15.4815