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    Kappa receptor opioid peptides
    2.
    发明授权
    Kappa receptor opioid peptides 失效
    卡帕受体阿片样肽

    公开(公告)号：US5965701A

    公开(公告)日：1999-10-12

    申请号：US997208

    申请日：1997-12-23

    申请人： Jean Louis Junien ,  Pierre J.M. Riviere ,  Claudio D. Schteingart ,  Javier Sueiras Diaz ,  Jerzy A. Trojnar ,  Todd W. Vanderah

    发明人： Jean Louis Junien ,  Pierre J.M. Riviere ,  Claudio D. Schteingart ,  Javier Sueiras Diaz ,  Jerzy A. Trojnar ,  Todd W. Vanderah

    IPC分类号： A61K38/00 ,  A61K38/07 ,  A61P1/04 ,  A61P13/00 ,  A61P13/10 ,  A61P25/04 ,  C07K5/10 ,  C07K5/107 ,  C07K5/117 ,  C07K5/00

    CPC分类号： C07K5/1027 ,  C07K5/1016 ,  C07K5/1024 ,  A61K38/00

    摘要： Peptides which exhibit high selectivity for the kappa opioid receptor (KOR) and long duration of peripheral action without significant entry into the brain are created which are sequences of four D-isomer amino acid residues having a C-terminus which is a mono or di-substituted amide. Representative compounds, which have an affinity for the KOR at least 1,000 times their affinity for the mu opioid receptor and an ED.sub.50 of not greater than about 0.5 mg/kg, includeH-D-Phe-D-Phe-D-Nle-D-Arg-NHEt,H-D-Phe-D-Phe-D-Nle-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr,H-D-Phe-D-Phe-D-Nle-D-Arg-thiomorpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NEt.sub.2,H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe,H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHhEt,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl,H-D-Ala(2Thi)-D-4Cpa-D-Leu-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-piperidinyl,H-D-Phe-D-Phe-D-Leu-D-Orn-NHEt,H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl,andH-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl.

    摘要翻译： 产生对κ阿片样物质受体（KOR）具有高选择性且长期持续的外周作用而不显着进入脑的肽是具有C末端的四个D-异构体氨基酸残基的序列，其是单或二 - 取代的酰胺。 对KOR具有至少1,000次对μ阿片受体的亲和力和不大于约0.5mg / kg的ED 50的亲和力的代表性化合物包括H-D-Phe-D-Phe-D-Nle-D- Arg-NHEt，HD-Phe-D-Phe-D-Nle-D-Arg-吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲基，HD-Phe- Phe-D-Nle-D-Arg-NHPr，HD-Phe-D-Phe-D-Nle-D-Arg-硫代吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-NEt2， Phe-D-Phe-D-Nle-D-Arg-NHMe，HD-Phe-D-Phe-D-Leu-D-Orn-吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg- NHhEt，HD-Phe-D-Phe-D-Nle-D-Arg-NH-环丙基，HD-Ala（2Thi）-D-4Cpa-D-Leu-D-Arg-吗啉基，HD-Phe-D-Phe -D-Nle-D-Arg-哌啶基，HD-Phe-D-Phe-D-Leu-D-Orn-NHEt，HD-Phe-D-Phe-D-Leu-D-Lys-吗啉基和H-D -Phe-D-Phe-D-Nle-D-Arg-哌嗪基。