Carbetocin acetate (C09-1119-799)

Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a K i of 7.1 nM. Carbetocin acetate has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (K i =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 .In VitroCarbetocin 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoCarbetocin (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:Solid. Specification: 0.99 Molecular Formula: C47H73N11O14S Molecular Weight: 1048.21 PubChem CID: 129319308