Modified polypeptide compound with VIP-like activity
    2.
    发明授权
    Modified polypeptide compound with VIP-like activity 失效
    具有VIP样活性的修饰的多肽化合物

    公开(公告)号:US5521157A

    公开(公告)日:1996-05-28

    申请号:US361443

    申请日:1994-12-20

    CPC分类号: C07K14/57563 A61K38/00

    摘要: The modified polypeptide compound of the present invention is represented by the following general formula ((SEQ ID NO: 2)-X):His-Ser-Asp-Ala-Val-Phe-Thr-Gly-Asn-Tyr-Thr-Lys-Leu-Arg-Lys-Gln-Leu-Ala-Ala-Lys-Lys-Tyr-Leu-R.sup.1 -Lys-Ala-Leu-R.sup.2 -Hse-Xwherein R.sup.1 represents an Asn, Lys or Gln residue, R.sup.2 represents a Lys or Arg residue, Hse represents a homoserine residue, and X represents NHR.sup.3 or NR.sup.4 R.sup.5, wherein R.sup.3 represents a hydrocarbon residue having 18 or less carbon atoms or a polyalkylamine having 2 or more amino groups in its molecule, or R.sup.4 and R.sup.5 represent hydrocarbon residues, provided that the total carbon number of R.sup.4 and R.sup.5 is 18 or less. This modified polypeptide compound has a strong activity as a smooth muscle relaxant, and has excellent stability and prolonged duration of action. These characteristics make it suitable as an active ingredient in a drug for preventing and treating bronchial asthma and impotence.

    摘要翻译: 本发明的修饰多肽化合物由以下通式((SEQ ID NO:2)-X)表示:His-Ser-Asp-Ala-Val-Phe-Thr-Gly-Asn-Tyr-Thr-Lys -Leu-Arg-Lys-Gln-Leu-Ala-Ala-Lys-Lys-Tyr-Leu-R1-Lys-Ala-Leu-R2-Hse-X其中R1表示Asn,Lys或Gln残基,R2表示 Lys或Arg残基,Hse表示高丝氨酸残基,X表示NHR3或NR4R5,其中R3表示碳原子数为18以下的烃残基或其分子中具有2个以上氨基的多烷基胺,或者R4和R5表示烃残基 条件是R4和R5的总碳数为18以下。 这种修饰的多肽化合物作为平滑肌松弛剂具有强烈的活性,并且具有优异的稳定性和延长的作用持续时间。 这些特征使其适合作为预防和治疗支气管哮喘和阳a药物的有效成分。