Potent and selective non-peptide NK3receptor antagonist (Kivalues are 1, 144 and >100000 nM for human NK3, NK2and NK1receptors respectively). Selective over a panel of >60 receptors, enzymes and ion channels at concentrations of 1 or 10μM. Inhibits NKB-in
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST
Mechanism of action
Neurokinin 3 receptor antagonist
Product Description
Product description
Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies.
1.Giardina GA, Raveglia LF, Grugni M, Sarau HM, Farina C, Medhurst AD, Graziani D, Schmidt DB, Rigolio R, Luttmann M et al.. (1999) 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).. J Med Chem, 42 (6):(1053-65). [PMID:10090788]
2.Liem-Moolenaar M, Gray FA, de Visser SJ, Franson KL, Schoemaker RC, Schmitt JA, Cohen AF, van Gerven JM. (2010) Psychomotor and cognitive effects of a single oral dose of talnetant (SB223412) in healthy volunteers compared with placebo or haloperidol.. J Psychopharmacol (Oxford), 24 (1):(73-82). [PMID:18755817]
3.de la Flor R, Dawson LA. (2009) Augmentation of antipsychotic-induced neurochemical changes by the NK3 receptor antagonist talnetant (SB-223412).. Neuropharmacology, 56 (2):(342-9). [PMID:18822303]
4.Dawson LA, Cato KJ, Scott C, Watson JM, Wood MD, Foxton R, de la Flor R, Jones GA, Kew JN, Cluderay JE et al.. (2008) In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia.. Neuropsychopharmacology, 33 (7):(1642-52). [PMID:17728699]
5.Sarau HM, Griswold DE, Potts W, Foley JJ, Schmidt DB, Webb EF, Martin LD, Brawner ME, Elshourbagy NA, Medhurst AD 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 Exp Ther, 281 (3):(1303-11). [PMID:9190866]
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C2323812