R 715 (trifluoroacetate salt)

一种缓激肽B1受体拮抗剂；能够抑制表达缓激肽B1受体的离体人脐带中由缓激肽诱导的收缩（pA₂=8.49）；在链脲佐菌素（STZ）诱导的糖尿病神经病变小鼠模型中，以200、400和600µg/kg的剂量给药，可缩短尾部缩回潜伏期（在尾甩实验中）；在髓鞘少突胶质细胞糖蛋白35-55肽（MOG₃₅₋₅₅）诱导的实验性自身免疫性脑脊髓炎（EAE）小鼠模型中，以每天1mg/kg的剂量给药，可减少后肢无力和瘫痪的发生率，改善对称性步态，并减少脊髓炎症病灶数量、神经元脱髓鞘以及病变部位单核细胞的浸润；在自发性高血压大鼠中，通过脑室内注射（i.c.v.）0.01nmol/动物的剂量，可降低平均动脉血压并增加心率。A bradykinin B1 receptor antagonist; inhibits bradykinin-induced contractions in isolated human umbilical cords, which express bradykinin B1 receptors (pA2 = 8.49); decreases the latency to tail withdrawal in the tail-flick test in an STZ-induced mouse model of diabetic neuropathy at 200, 400, and 600 µg/kg; reduces the incidence of hind limb weakness and paralysis, improves symmetrical gait, as well as decreases spinal inflammatory foci numbers, neuron demyelination, and lesion monocyte invasion, in a MOG35-55 peptide-induced mouse model of EAE at 1 mg/kg per day; reduces mean arterial blood pressure and increases heart rate in spontaneously hypertensive rats at 0.01 nmol/animal, i.c.v.分子式C57H81N13O12 • XCF3COOH分子量1140.3O=C(N1[C@@H](CCC1)C(NCC(N[C@H](C(N[C@@H](CO)C(N[C@@H](C(N[C@H](C(O)=O)[C@@H](C)CC)=O)CC2=CC3=C(C=CC=C3)C=C2)=O)=O)CC4=CC=CC=C4)=O)=O)[C@H]5N(CCC5)C([C@H](CCCNC(N)=N)NC([C@@H](NC(C)=O)CCCCN)=O)=O.OC(C(F)(F)F)=O