Osanetant (hydrate)

NK3受体拮抗剂（在表达人类受体的CHO细胞中Ki=0.21nM）；对NK3受体的选择性优于NK1和NK2受体（Kis分别为>100和0.02µM）；抑制豚鼠回肠条带中神经激肽B诱发的收缩和乙酰胆碱释放；抑制卵清蛋白致敏的过敏性哮喘小鼠模型中卵清蛋白诱发的BALF中性粒细胞、嗜酸性粒细胞和淋巴细胞浸润增加；在5和10mg/kg剂量下对沙鼠具有抗焦虑和抗抑郁作用。An NK3 receptor antagonist (Ki = 0.21 nM in CHO cells expressing the human receptor); selective for NK3 over NK1 and NK2 receptors (Kis = >100 and 0.02 µM, respectively); inhibits neurokinin B-induced contractions and acetylcholine release in isolated guinea pig ileal strips; inhibits ovalbumin-induced increases in BALF neutrophil, eosinophil, and lymphocyte infiltration in an ovalbumin-sensitized mouse model of allergic asthma; has anxiolytic-like and antidepressant-like activities in gerbils at 5 and 10 mg/kg.分子式C35H41Cl2N3O2 • H2O分子量624.7O=C(C1=CC=CC=C1)N(CCC2)C[C@]2(C3=CC(Cl)=C(C=C3)Cl)CCCN4CCC(C5=CC=CC=C5)(N(C)C(C)=O)CC4.O