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Submit ReviewSB 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.
Sold for research purposes under agreement from GlaxoSmithKline.
分子量 | 382.45 |
公式 | C25H22N2O2 |
储存 | Store at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: SB 223412, SB 223412 supplier, SB223412, Potent, selective, non-peptide, NK3, antagonists, Brain, penetrant, Tachykinin, Receptors, Neurokinin, orally, active, Receptor, 4672, Tocris Bioscience
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.