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    • 1. 发明授权
    • Neurotensin Hexapeptides
    • 神经降压肽六肽
    • US5393740A
    • 1995-02-28
    • US920878
    • 1992-07-28
    • Sakae AmagayaTadami FujiwaraMasaki AburadaMichio NagasawaTsutomu Oyama
    • Sakae AmagayaTadami FujiwaraMasaki AburadaMichio NagasawaTsutomu Oyama
    • A61K38/00A61P3/00A61P7/02A61P9/10A61P9/12A61P29/00A61P37/08A61P43/00C07K5/10C07K7/06A61K37/00C07K5/00C07K7/00A61K37/02
    • C07K7/06A61K38/00
    • A hexapeptide represented by formula (II):A-B-Pro-C-D-E (I)where A represents an L- or D- form of arginine or lysine whose N-terminal amino group is alkylated or acylated, B represents an L- or D- form of argine, lysine, or histidine, Pro represents an L- or D- form of proline, C represents an L- or D- form of tyrosine, tryptophan, or phenylalanine, D represents an L- or D- form of valine, isolencine, or leucine, and E represents an L-or D- form of valine, isolencine, or lencine, one of the hydrogen atoms of the amino group of which may be substituted a C.sub.1 to C.sub.4 alkyl group, and C-terminal carboxyl group of which is substituted with --COOR*, --CH.sub.2 OR, or --CONHR wherein R* represents a C.sub.1 to C.sub.4 alkyl group, and R represents a hydrogen atom or an C.sub.1 to C.sub.4 alkyl group. The hexapeptide or a pharmaceutically acceptable salt of the hexapeptide is useful as medical agent such as an anti-edematous agent, an anti-shock agent, an anti-thrombus agent, an anti-arteriosclerotic agent, an anti-allergic agent, a hypotensive agent, a wound healing agent, and an anti-inflammatory agent.
    • 由式(II)表示的六肽:AB-Pro-CDE(I)其中A表示其N-末端氨基被烷基化或酰化的L-或D-型精氨酸或赖氨酸,B表示L-或D- 氨基酸,赖氨酸或组氨酸的形式,Pro代表L-或D-形式的脯氨酸,C代表L-或D-形式的酪氨酸,色氨酸或苯丙氨酸,D表示L-或D-形式的缬氨酸, 异亮氨酸或亮氨酸,E表示缬氨酸,异亮氨酸或氨基酸的L-型或D-型,其氨基的一个氢原子可被C1-C4烷基取代,C-末端羧基 被-COOR *,-CH 2 OR或-CONHR取代,其中R *表示C1至C4烷基,R表示氢原子或C1至C4烷基。 六肽的六肽或药学上可接受的盐可用作药剂,例如抗水肿剂,抗休克剂,抗血栓剂,抗动脉硬化剂,抗过敏剂,降血压剂 ,伤口愈合剂和抗炎剂。