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编 号:F746363
分子式:C47H73N11O14S
分子量:1048.21
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin acetate has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.

体内研究:
Carbetocin acetate (2 -20 mg/kg;腹腔注射) 对攀爬、游泳和不动的时间百分比有显著的处理效果。 Carbetocin acetate (1、10,100 μg/大鼠,icv) 显示,在急性给药 100 μg/大鼠后,游泳时间百分比呈剂量依赖性增加。Animal Model:Male Sprague-Dawley rats weighing between 300 and 500 g
Dosage:2, 6.4, 20 mg/kg
Administration:IP; single dose
Result:Increased climbing with 6.4 mg/kg and resulted in a significantly greater proportion of time spent swimming with 20 mg/kg.

体外研究:
Carbetocin acetate 是一种激动剂,对催产素受体的亲和力低约 10 倍,但具有显著更高的稳定性和更长的作用持续时间。Carbetocin acetate 对嵌合 E1 受体具有更高的亲和力,尤其是对 E1 与其他细胞外结构域的结合,即嵌合受体 E13 (Ki=13 nM)、E123 (K i=56 nM),E1234 (Ki=37 nM)。
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