中文同义词:
艾替班特;ICATIBANT 艾替班特
英文同义词:
RRP-(HYP)-G-(THI)-S-(D-TIC)-(OIC)-R;H-D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG-OH;H2N-D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG-OH;Icatibatide Acetate;Icatibant;D-Arg-[Hyp3,Thi5,D-Tic7,Oic8]bradykinin;D-Arg-L-Arg-L-Pro-L-t4Hyp-Gly-L-Thi-L-Ser-D-Tic-L-Oic-L-Arg-OH;H0E-140
相关类别:
生物制药;多肽;现货;药物多肽;peptide
密度
1.60±0.1 g/cm3(Predicted)
酸度系数(pKa)
3.60±0.21(Predicted)
作用
艾替班特是一种对缓激肽B2受体选择性的竞争性拮抗剂，亲和力与缓激肽相似。遗传性血管水肿是C1-酯酶-抑制剂的缺乏或功能失调所致，缓激肽是一种血管扩张剂，被认为负责局部化肿胀、炎症、和疼痛等HAE特征性症状。艾替班特通过抑制缓激肽与B2受体结合以治疗HAE急性发作临床症状。除此之外，他还有潜在的治疗适应症如哮喘、肝硬化和其他类型的血管性水肿。
用途
艾替班特是一个合成的、包含10个氨基酸的多肽(H-DAarg-Arg-Pro-Hyp-Gly-Thi-Ser-Dtic-Oic-Arg-OH)，与缓激肽结构类似，是一个强效的、选择性的缓激肽B2受体拮抗药，它能阻止缓激肽与其B2受体结合，从而对急性发作期HAE的患者进行治疗。
生物活性
Icatibant (HOE-140) 是有效的，特异的缓激肽B2受体拮抗剂，IC50 和 Ki 值分别为 1.07 nM 和 0.798 nM。
体外研究
Icatibant (10-30 μM) potentiates angiotensin III, but not angiotensin II (contraction mediated by angiotensin AT1 receptors), and Lys-des-Arg9-bradykinin, but not des-Arg9-bradykinin (effects mediated by the bradykinin B1 receptors).
体内研究
Icatibant (0.3, or 1.5 mg/kg, subcutaneous administration twice daily in mice) shows a significant preventive effect on ulcerative Colitis.
Animal Model: Female mice of the CBA/J (H-2 k ) strain.
Dosage: 0.06, 0.3, or 1.5 mg/kg.
Administration: Subcutaneous administration twice daily.
Result: The length of the large intestine was 93.6±6.8 mm with the 1.5 mg/kg dosage and 94.0±4.1 mm with the 0.3 mg/kg dosage , showing a significant preventive effect on shortening.
Animal Model:
Female mice of the CBA/J (H-2 k ) strain.
Dosage:
0.06, 0.3, or 1.5 mg/kg.
Administration:
Subcutaneous administration twice daily.
Result:
The length of the large intestine was 93.6±6.8 mm with the 1.5 mg/kg dosage and 94.0±4.1 mm with the 0.3 mg/kg dosage , showing a significant preventive effect on shortening.
