| 产品描述： | 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 |
| 靶点： |
Neurokinin Receptor;Neurokininreceptor |
| 体内研究： |
Talnetant (SB 223412) (0.5-2 mg/kg iv, 2min pretreatment) can inhibit the miosis induced by senktide (25µg, iv) in a dose-dependent manner with an ED50 of 0.44mg/kg in conscious rabbits. Talnetant (SB 223412) (i.p., 1-100 mg/kg, 1 h) can significantly attenuate senktide-induced wet dog wagging behavior in a dose-dependent manner, significantly increase extracellular dopamine and norepinephrine in the medial prefrontal cortex and reduce haloperidol-induced increases in dopamine levels in the vomeronasal nucleus of freely moving guinea pigs |
| 参考文献： |
1. Giardina GA, et al. 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. 1999 Mar 25;42(6):1053- 2. Houghton LA, et al. Effect of the NK(3) receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans. Neurogastroenterol Motil. 2007 Sep;19(9):732-43. 3. Dawson LA, et al. 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. 2008 Jun;33(7):1642-52. |
| 溶解性： |
DMSO : ≥ 100 mg/mL (261.47 mM) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.615 ml |
13.074 ml |
26.147 ml |
| 5 mM |
0.523 ml |
2.615 ml |
5.229 ml |
| 10 mM |
0.261 ml |
1.307 ml |
2.615 ml |
| 50 mM |
0.052 ml |
0.261 ml |
0.523 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京