毒蜥外泌肽-4的類似物或衍生物。
[0030]胰島素類似物例如Gly (A21)、Arg (B31)、Arg (B32)人胰島素;Lys(B3)、Glu (B29)人胰島素;Lys (B28)、Pro (B29)人胰島素;Asp (B28)人胰島素;人胰島素,其中B28位的脯氨酸被替換為Asp、Lys, Leu, Val或Ala且其中B29位的賴氨酸可以替換為Pro ;Ala(B26)人胰島素;Des(B28-B30)人胰島素;Des(B27)人胰島素;和Des (B30)人胰島素。
[0031]膜島素衍生物例如B29-N-肉?蔑醜-des (B30)人膜島素;B29_N_掠桐醜_des(B30)人膜島素;B29_N_肉?蔑醜人膜島素;Β29_Ν_掠桐醜人膜島素;Β28_Ν_肉豆蔻酰LysB28ProB29人胰島素;Β28_Ν_棕櫚酰_LysB28ProB29人胰島素;B30_N_肉豆蔻酰-ThrB29LysB30 人胰島素;B30_N_ 棕櫚酰 _ThrB29LysB30 人胰島素;B29_N_ (N-棕櫚酰-T -谷氨酰)-des (B30)人膜島素;B29_N_ (N-石膽酰-T -谷氨酰)-des (B30)人膜島素;B29_N_ (ω -竣基十七醜)_des (B30)人膜島素和B29-N- (ω -竣基十七醜)人膜島素。
[0032]毒蜥外泌肽-4意指例如毒蜥外泌肽-4 (1-39),其是具有下述序列的肽:H His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-LyS-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-1le-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser_NH20
[0033]毒蜥外泌肽-4衍生物例如選自下述化合物列表:
[0034]H- (Lys) 4_des Pro36, des Pro37 毒蜥外泌肽 _4 (1-39) -NH2,
[0035]H- (Lys) 5_des Pro36, des Pro37 毒蜥外泌肽 _4 (1-39) -NH2,
[0036]des Pro36 [Asp28]毒蜥'外泌妝-4 (1-39),
[0037]des Pro36 [IsoAsp28]毒蜥'外泌妝-4 (1-39),
[0038]des Pro36 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39),
[0039]des Pro36 [Met (0) 14,IsoAsp28]毒蜥外泌肽 _4 (1-39),
[0040]des Pro36 [Trp (02) 25, Asp28]毒蜥外泌肽 _4 (1-39),
[0041]des Pro36[Trp (02)25, IsoAsp28]毒蜥外泌肽-4(1-39),
[0042]des Pro36 [Met (0) 14Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39),
[0043]des Pro36 [Met (0) 14Trp (02) 25,IsoAsp28]毒蜥外泌肽-4 (1-39);或
[0044]des Pro36 [Asp28]毒蜥'外泌妝-4 (1-39),
[0045]des Pro36 [IsoAsp28]毒蜥'外泌妝-4 (1-39),
[0046]des Pro36 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39),
[0047]des Pro36 [Met (0) 14, IsoAsp28]毒蜥'外泌妝-4 (1-39),
[0048]des Pro36 [Trp (02) 25, Asp28]毒蜥外泌肽 _4 (1-39),
[0049]des Pro36 [Trp (02) 25,IsoAsp28]毒蜥外泌肽 _4 (1-39),
[0050]des Pro36 [Met (0) 14Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39),
[0051]des Pro36 [Met (0) 14Trp (02) 25, IsoAsp28]毒蜥外泌肽-4(1-39),
[0052]其中-Lys6-NH2基團(tuán)可以結(jié)合于毒蜥外泌肽_4衍生物的C端;
[0053]或下述序列的毒蜥外泌肽-4衍生物
[0054]H- (Lys) 6_des Pro36 [Asp28]毒蜥外泌肽 _4 (1-39) -Lys6-NH2,
[0055]des Asp28Pro36, Pro37, Pro38 毒蜥外泌肽 _4 (1-39) -NH2,
[0056]H- (Lys) 6_des Pro36, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) -NH2,
[0057]H-Asn- (Glu) 5des Pro36, Pro37, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) -NH2,
[0058]des Pro36, Pro37, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0059]H- (Lys) 6_des Pro36, Pro37, Pro38 [Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0060]H-Asn - (Glu) 5-des Pro36, Pro37, Pro38 [Asp28]毒撕外泌肽-4 (1-39)-(Lys) 6-NH2,
[0061 ] H- (Lys) 6_des Pro36 [Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39) -Lys6-NH2,
[0062]H-des Asp28Pro36, Pro37, Pro38 [Trp (02) 25]毒蜥外泌肽 _4 (1-39) -NH2,
[0063]H-(Lys) 6_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒蜥' 外泌肽-4(1-39)-ΝΗ2,
[0064]H-Asn-(Glu) 5_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒蜥' 外泌肽-4(1-39)-ΝΗ2,
[0065]des Pro36, Pro37, Pro38 [Trp (02) 25,Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0066]H-(Lys) 6_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒蜥' 外泌肽-4 (1-39)-(Lys) 6-NH2,
[0067]H-Asn-(Glu) 5_des Pro36, Pro37, Pro38 [Trp (02) 25, Asp28]毒蜥' 外泌肽-4 (1-39)-(Lys) 6-NH2,
[0068]H- (Lys) 6_des Pro36 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) -Lys6-NH2,
[0069]des Met (0) 14Asp28Pro36, Pro37, Pro38 毒蜥外泌肽 _4 (1-39) -NH2,
[0070]H- (Lys) 6-desPro36, Pro37, Pro38 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) -NH2,
[0071]H-Asn-(Glu) 5-des Pro36, Pro37, Pro38 [Met (0) 14, Asp28]毒蜥外泌肽-4(1-39)-ΝΗ2,
[0072]des Pro36, Pro37, Pro38 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) - (Lys) 6-NH2,
[0073]H-(Lys) 6_des Pro36, Pro37, Pro38 [Met (0) 14, Asp28]毒蜥' 外泌肽-4 (1-39)-(Lys) 6-NH2,
[0074]H-Asn-(Glu) 5des Pro36, Pro37, Pro38 [Met (0) 14, Asp28]毒蜥' 外泌肽-4 (1-39)-(Lys) 6-NH2,
[0075]H-Lys6-des Pr ο 3 6 [Me t (O) I 4, Trp (02) 25, Asp 28]毒蜥外泌月太-4(l-39)-Lys6-NH2,
[0076]H-des Asp28Pro36, Pro37, Pro38 [Met (0) 14, Trp (02) 25]毒蜥外泌肽-4(1-39)-ΝΗ2,
[0077]H- (Lys) 6_des Pro36, Pro37, Pro38 [Met (0) 14,Asp28]毒蜥外泌肽 _4 (1-39) -NH2,
[0078]H-Asn-(Glu) 5-des Pro36, Pro37, Pro38 [Met (0) 14, Trp (02) 25, Asp28]毒蜥外泌肽-4(1-39)-ΝΗ2,
[0079]des Pro36, Pro37, Pro38 [Met (0) 14, Trp (02) 25, Asp28]毒蜥' 外泌肽-4 (1-39)-(Lys) 6-NH2,
[0080]H-(Lys)6~des Pro36, Pro37, Pro38[Met(0)14, Trp(02)25, Asp28]毒蜥' 外泌肽-4 (Sl-39)-(Lys)6-NH2,
[0081]H-Asn-(Glu) 5-des Pro36, Pro37, Pro38 [Met (0) 14, Trp (02) 25, Asp28]毒蜥外泌肽-4 (1-39)-(Lys)6-NH2 ;
[0082]或前述任一種毒蜥外泌肽-4衍生物的藥學(xué)可接受鹽或溶劑合物。
[0083]激素例如在Rote Liste, ed.2008,第50章中列出的垂體激素(hypophysishormones)或下丘腦激素(hypothalamus hormones)或調(diào)節(jié)性活性月太(regulatoryactive peptides)和它們的措抗劑,諸如促性腺激素(促濾泡素(Follitropin)、促黃體激素(Lutropin)、絨毛膜促性腺激素(Chor1ngonadotropin)、絕經(jīng)促性素(Menotropin))、Somatropine (生長激素(Somatropin))、去氨加壓素(Desmopressin