| Identification | Back Directory | [Name]
OT-R antagonist 1 | [CAS]
364071-17-0 | [Synonyms]
OT-R antagonist 1
LS-192629（OT-R antagonist 1）
Oxytocin receptor antagonist 1
2-PyrrolidinecarboxaMide, N-[(2S)-2-hydroxy-2-phenylethyl]-4-(MethoxyiMino)-1-[(2'-Methyl[1,1'-biphenyl]-4-yl)carbonyl]-, (2S,4Z)- | [Molecular Formula]
C28H29N3O4 | [MOL File]
364071-17-0.mol | [Molecular Weight]
471.55 |
| Hazard Information | Back Directory | [Uses]
OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM).
IC50 value: 8 nM
Target: oxytocin receptor
in vitro: OT-R antagonist 1 inhibitis IP3-Synthesis, rat OT-R (IC50=0.03 uM). [4] OT-R antagonist 1 inhibits phosphodiesterase IV with IC50 = 6.1 μM, a value about 300-fold higher than the affinity for OT-R. OT-R antagonist 1 shows a very clean selectivity profile with specific interaction with OT-R. OT-R antagonist 1 competitively inhibits binding of [3H]oxytocin and the peptide antagonist 125I-ornithine vasotocin analog to human and rat oxytocin receptor expressed in human embryonic kidney 293-EBNA or Chinese hamster ovary cells with nanomolar potency. Selectivity against vasopressin receptor subtypes is >6-fold for V1a and >350-fold for V2 and V1b. [1]
in vivo: Oxytocininduced contraction of isolated rat uterine strips is blocked by OT-R antagonist 1 (pA2 = 7.82). In anesthetized nonpregnant rats, single administration of OT-R antagonist 1 by i.v. or oral routes causes dose-dependent inhibition of contractions elicited by repeated injections of oxytocin with ED50 = 3.5 mg/kg i.v. and 89 mg/kg p.o., respectively. OT-R antagonist 1 significantly inhibits spontaneous uterine contractions in pregnant rats near term when administered intravenously or orally. [1] | [Biological Activity]
OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist. It inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). | [in vitro]
OT-R antagonist 1 inhibitis IP3-Synthesis, rat OT-R (IC50=0.03 uM). OT-R antagonist 1 inhibits phosphodiesterase IV with IC50 = 6.1 μM, a value about 300-fold higher than the affinity for OT-R. OT-R antagonist 1 shows a very clean selectivity profile with specific interaction with OT-R. OT-R antagonist 1 competitively inhibits binding of [3H]oxytocin and the peptide antagonist 125I-ornithine vasotocin analog to human and rat oxytocin receptor expressed in human embryonic kidney 293-EBNA or Chinese hamster ovary cells with nanomolar potency. Selectivity against vasopressin receptor subtypes is >6-fold for V1a and >350-fold for V2 and V1b. | [in vivo]
Oxytocininduced contraction of isolated rat uterine strips is blocked by OT-R antagonist 1 (pA2 = 7.82). In anesthetized nonpregnant rats, single administration of OT-R antagonist 1 by i.v. or oral routes causes dose-dependent inhibition of contractions elicited by repeated injections of oxytocin with ED50 = 3.5 mg/kg i.v. and 89 mg/kg p.o., respectively. OT-R antagonist 1 significantly inhibits spontaneous uterine contractions in pregnant rats near term when administered intravenously or orally. | [storage]
Store at -20°C | [References]
[1] Serge Halazy, et al. Pharmaceutically active pyrrolidine derivatives as bax inhibitors. WO/2001072705/A1.
[2] Cirillo R, et al. Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor. J Pharmacol Exp Ther. 2003 Jul;306(1):253-61. DOI:10.1124/jpet.103.049395
[3] William Nadler, et al. Method for preparing pyrrolidine oximes. WO/2005082848/A2.
[4] Serge Halazy, et al. Pharmaceutically active pyrrolidine derivatives as bax inhibitors.WO/2001074769/A1. |
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