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OT-R antagonist 1

Catalog No. T12331L CAS 364071-17-0

Synonyms: Oxytocin receptor antagonist 1

OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist.

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OT-R antagonist 1, CAS 364071-17-0

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Description	OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist.
In vitro	OT-R antagonist 1 inhibits IP3-Synthesis, rat OT-R (IC50=0.03 uM). OT-R antagonist 1 inhibits phosphodiesterase IV (IC50 = 6.1 μM, a value about 300-fold higher than the affinity for 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. OT-R antagonist 1 displays a very clean selectivity profile with specific interaction with OT-R. Selectivity against vasopressin receptor subtypes is >6-fold for V1a and >350-fold for V2 and V1b[1][4].
In vivo	OT-R antagonist 1 significantly inhibits spontaneous uterine contractions in pregnant rats near term when administered intravenously or orally. Oxytocininduced contraction of isolated rat uterine strips is blocked by OT-R antagonist 1 (pA2 = 7.82). OT-R antagonist 1(single administration; i.v. or oral routes) causes dose-dependent inhibition of contractions elicited by repeated injections of oxytocin (ED50 = 3.5 mg/kg i.v. and 89 mg/kg p.o., respectively), in anesthetized nonpregnant rats [1]

Synonyms	Oxytocin receptor antagonist 1
Molecular Weight	471.55
Formula	C28H29N3O4
CAS No.	364071-17-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 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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Keywords

OT-R antagonist 1 364071-17-0 Others Oxytocin receptor antagonist 1 OT R antagonist 1 OTR antagonist 1 inhibitor inhibit

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