产品
编 号:F338930
分子式:C45H69N11O12S
分子量:988.16
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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, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.

体内研究:
Carbetocin (2-20 mg/kg; i.p.) has a significant effect of treatment on the percent time spent climbing, swimming and immobile. Carbetocin (1, 10,100 μg/rat, i.c.v.) reveals a dose-dependent increase in the percent time spent swimming and a corresponding reduction in immobility following acute administration of 100 μg/rat. 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 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 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 (Ki=13 nM), E123 (Ki=56 nM), and E1234 (Ki=37 nM).
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