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| | barusiban Basic information |
| Product Name: | barusiban | | Synonyms: | barusiban;Arasertaconazole Nitrate;L-Homocysteinamide, N-(3-mercapto-1-oxopropyl)-D-tryptophyl-L-isoleucyl-L-alloisoleucyl-L-asparaginyl-N-[(1S)-4-amino-1-(hydroxymethyl)butyl]-N-methyl-, cyclic (1→5)-thioether | | CAS: | 285571-64-4 | | MF: | C40H63N9O8S | | MW: | 830.05 | | EINECS: | | | Product Categories: | | | Mol File: | 285571-64-4.mol |  |
| | barusiban Chemical Properties |
| Boiling point | 1262.1±65.0 °C(Predicted) | | density | 1.175±0.06 g/cm3(Predicted) | | pka | 12.96±0.70(Predicted) |
| | barusiban Usage And Synthesis |
| Uses | Barusiban (FE-200440) is an oxytocin receptor (OT-R) antagonist (Ki=0.8 nM), inhibits OT-induced contraction. Barusiban can be used in preterm labor (PTL), in vitro fertilisation (IVF) and infertility research[1][2][3]. | | in vivo | Barusiban (intravenous injection; 50 or 150 μg/kg; once) treatment shows inhibition on OT-induced contractions[2]. | Animal Model: | Pregnant cynomolgus monkeys injected with oxytocin (OT)[2] | | Dosage: | 50 or 150 μg/kg | | Administration: | Intravenous injection; 50 or 150 μg/kg; once | | Result: | Reduced uterine contractions to baseline levels effectively.
Reduced intrauterine pressure (IUP) from 6-7.5 kmm Hgh to approximately 1 kmm Hgh. |
| | References | [1] Helmer H, et al. Barusiban, a selective oxytocin receptor antagonist: placental transfer in rabbit, monkey, and human. Biol Reprod. 2020 Jun 23;103(1):135-143. DOI:10.1093/biolre/ioaa048
[2] Reinheimer TM, et al. Barusiban, a new highly potent and long-acting oxytocin antagonist: pharmacokinetic and pharmacodynamic comparison with atosiban in a cynomolgus monkey model of preterm labor. J Clin Endocrinol Metab. 2005 Apr;90(4):2275-81. DOI:10.1210/jc.2004-2120
[3] Gimpl G, et al. Binding domains of the oxytocin receptor for the selective oxytocin receptor antagonist barusiban in comparison to the agonists oxytocin and carbetocin. Eur J Pharmacol. 2005 Mar 7;510(1-2):9-16. DOI:10.1016/j.ejphar.2005.01.010 |
| | barusiban Preparation Products And Raw materials |
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