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Submit ReviewSB 223412
Discontinued Product
SB 223412 (Cat. No. 4672) has been withdrawn from sale for commercial reasons.
Description: Potent, selective non-peptide NK3 antagonist. Brain penetrant
Chemical Name: 3-Hydroxy-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for SB 223412
SB 223412 is a potent and selective non-peptide NK3 receptor antagonist (Ki values are 1, 144 and >100000 nM for human NK3, NK2 and NK1 receptors respectively). Selective over a panel of >60 receptors, enzymes and ion channels at concentrations of 1 or 10 μM. Inhibits NKB-induced Ca2+ mobilization in vitro (IC50 = 16.6 nM) and inhibits NK3-agonist-induced behavioral responses in vivo. Orally active and brain penetrant.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Technical Data for SB 223412
| M. Wt | 382.45 |
| Formula | C25H22N2O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 174636-32-9 |
| PubChem ID | 5311424 |
| InChI Key | BIAVGWDGIJKWRM-FQEVSTJZSA-N |
| Smiles | OC1=C(C(N[C@@H](CC)C2=CC=CC=C2)=O)C3=CC=CC=C3N=C1C4=CC=CC=C4 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for SB 223412
References for SB 223412
References are publications that support the biological activity of the product.
Sarau et al (1997) Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist. J.Pharmacol.Ther.Exp. 281 1303 PMID: 9190866
Sarau et al (2001) Molecular and pharmacological characterization of the murine tachykinin NK3 receptor. Eur.J.Pharmacol. 413 143 PMID: 11226387
de la Flor and Dawson (2009) Augmentation of antipsychotic-induced neurochemical changes by the NK3 receptor antagonist talnetant (SB-223412). Neuropharmacol. 56 342 PMID: 18822303
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Keywords: SB 223412, SB 223412 supplier, SB223412, Potent, selective, non-peptide, NK3, antagonists, Brain, penetrant, Tachykinin, Receptors, Neurokinin, orally, active, Receptor, 4672, Tocris Bioscience
Citations for SB 223412
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Currently there are no citations for SB 223412.
Reviews for SB 223412
Average Rating: 5 (Based on 1 Review.)
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tail bleed.
By
Anonymous on 09/07/2017
Assay Type: Ex Vivo
Species: Mouse
bleed assay
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