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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 50 mg/mL|
In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia.
Dawson LA, et al. Neuropsychopharmacology. 2008 Jun;33(7):1642-52. PMID: 17728699.
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).
Giardina GA, et al. J Med Chem. 1999 Mar 25;42(6):1053-65. PMID: 10090788.
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|[Leu31,Pro34]-NPY TFA (human,rat)
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Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
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