中文同义词:
艾替班特乙酸盐;D-精氨酸基-L-精氨酸基-L-脯氨酰基-(4R)-4-羟基-L-脯氨酰基糖基-3-(2-噻吩基)-L-丙氨酰基-L-丝氨酰-(3R)-1,2,3,4-四氢-3-异喹啉羰基-(2S,3aS,7aS)-八氢-1H-吲哚-2-羰基-L-精氨酸 乙酸盐;醋酸艾替班特(艾替班特乙酸盐,HOE 140);艾替班特 ACETATE
英文同义词:
HOE-140 (Icatibant);HOE140; ICATIBANT;HOE 140;CS-1399;Firazyr;HOE 140 SYNTHETIC >99% SELECTIVE B2 BRAD YKIN;d-arg-l-arg-l-pro-l-hyp-gly-l-(2-thienyl)ala-l-ser-d-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-l-(2α,3β,7aβ)-octahydro-1h-indole-2-carbonyl-l-arg;Icatibant acetate, D-Arg-L-Arg-L-Pro-L-Hyp-Gly-L-(2-thienyl)Ala-L-Ser-D-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L-(2α,3β,7aβ)-octahydro-1H-indole-2-carbonyl-L-Arg;HOE 140 Acetate
生物活性
Icatibant Acetate是bradykinin B2受体的拮抗剂，可用于治疗遗传性血管性水肿。
靶点
Target Value
bradykinin B2 receptor
()
bradykinin B2 receptor
()
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 (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).
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.
