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Submit ReviewGR 159897 is a potent, selective, non-peptide, orally active neurokinin NK2 receptor antagonist. Competes for binding of [3H]GR100679 to hNK2-transfected CHO cells with a pKi of 9.5. Inhibits NK2 receptor-mediated contraction of guinea pig trachea with a pA2 of 8.7. Anxiolytic in vivo.
Sold with the permission of GlaxoSmithKline
分子量 | 414.54 |
公式 | C23H27FN2O2S |
储存 | Desiccate at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 158848-32-9 |
PubChem ID | 9953599 |
InChI Key | BANYJBHWTOJQDU-GDLZYMKVSA-N |
Smiles | FC1=CC=C2C(C(CCN3CCC(C[S@@+]([O-])C4=CC=CC=C4)(OC)CC3)=CN2)=C1 |
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。
Beresford et al (1995) GR 159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur.J.Pharmacol. 272 241 PMID: 7713168
Walsh et al (1995) The anxiolytic-like activity of GR 159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety. Psychopharmacology 121 186 PMID: 8545524
Cooper et al (1994) GR 159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists. Bioorg.Med.Chem.Lett. 4 1951
关键词: GR 159897, GR 159897 supplier, Non-peptide, potents, NK2, antagonist, Tachykinin, Receptors, Neurokinin, GR159897, GlaxoSmithKline, GSK, Receptor, 1274, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GR 159897 的部分引用包括:
Kojima et al (2012) A role for endogenous peptide YY in tachykinin NK(2) receptor-triggered 5-HT release from guinea pig isolated colonic mucosa. Br J Pharmacol 167 1362 PMID: 22758653
Hegde et al (2010) Neurokinin-1 receptor antagonist treatment in polymicrobial sepsis: molecular insights. Int J Inflam 2010 601098 PMID: 21188216
Cunin et al (2011) The tachykinins substance P and hemokinin-1 favor the generation of human memory Th17 cells by inducing IL-1β, IL-23, and TNF-like 1A expression by monocytes. J Immunol 186 4175 PMID: 21368235
Grant (2012) Tachykinins stimulate a subset of mouse taste cells. Cell Commun Signal 7 e31697 PMID: 22363709
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