Carbetocin卡贝缩宫素醋酸盐,1631754-28-

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Carbetocin acetate

CAS No. : 1631754-28-3

MCE 国际站：Carbetocin acetate

产品活性：Carbetocin acetate 是一种催产素 (OT) 类似物，是催产素受体 (oxytocin receptor) 激动剂，K_i 是 7.1 nM。Carbetocin acetate 对催产素受体的嵌合 N 末端 (E1) 具有高亲和力 (K_i=1.17 μM)。Carbetocin acetate 具有用于产后出血研究的潜力。Carbetocin acetate 能透过血脑屏障，可以通过激活 CNS 中的催产素受体而具有类抗抑郁活性。

研究领域：GPCR/G Protein

作用靶点：Oxytocin Receptor

In Vitro: Carbetocin acetate is an agonist with about 10-fold lower affinity for the oxytocin receptor but with significantly higher stability and a longer duration of action. Carbetocin acetate has higher affinity to the chimeric E1 receptor and especially to each of the combinations of E1 with the other extracellular domains, i.e. chimeric receptors E13 (K_i=13 nM), E123 (K_i=56 nM), and E1234 (K_i=37 nM).

In Vivo: Carbetocin (2-20 mg/kg; i.p.) acetate has a significant effect of treatment on the percent time spent climbing, swimming and immobile.
Carbetocin (1, 10,100 μg/rat, i.c.v.) acetate reveals a dose-dependent increase in the percent time spent swimming and a corresponding reduction in immobility following acute administration of 100 μg/rat.

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