SB 223412
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Description: Potent, selective non-peptide NK3 antagonist. Brain penetrant
Chemical Name: 3-Hydroxy-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide
Purity: ≥98%
Biological Activity
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.Technical Data
M.Wt:
382.45
Formula:
C25H22N2O2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
174636-32-9
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline.
Background References
-
Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Sarau et al.
J.Pharmacol.Ther.Exp., 1997;281:1303 -
Molecular and pharmacological characterization of the murine tachykinin NK3 receptor.
Sarau et al.
Eur.J.Pharmacol., 2001;413:143 -
Augmentation of antipsychotic-induced neurochemical changes by the NK3 receptor antagonist talnetant (SB-223412).
de la Flor and Dawson
Neuropharmacol., 2009;56:342
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