| 产品描述： | TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats. IC50 value: 289 nM(EC50) Target: M1 mAChR agonist in vitro: TBPB activates M(1) through an allosteric site rather than the orthosteric acetylcholine binding site, which is likely critical for its unprecedented selectivity. Whole-cell patch-clamp recordings demonstrated that activation of M(1) by TBPB potentiates NMDA receptor currents in hippocampal pyramidal cells but does not alter excitatory or inhibitory synaptic transmission, responses thought to be mediated by M(2) and M(4) . in vivo: TBPB was efficacious in models predictive of antipsychotic-like activity in rats at doses that did not produce catalepsy or peripheral adverse effects of other mAChR agonists |
| 靶点： |
mAChR |
| 体内研究： |
TBPB (60 mg/kg；皮下注射；单次；建模前 2 小时) 显著降低大肠杆菌诱导的小鼠败血症模型死亡率，4 小时和 24 小时死亡率分别下降 20% 和 23.2%，并抑制 TNF-α、IL-1β 和 IL-6 水平。 |
| 参考文献： |
1. Jones CK, et al. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J Neurosci. 2008 Oct 8;28(41):10422-33. 2. Miller NR, et al. Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5443-7. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.472 ml |
12.359 ml |
24.719 ml |
| 5 mM |
0.494 ml |
2.472 ml |
4.944 ml |
| 10 mM |
0.247 ml |
1.236 ml |
2.472 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.494 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)
