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- 產品描述: 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
- 靶點: mAChR;AChR
- 參考文獻:
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
- 保存條件: -20℃
- 配置溶液濃度參考:
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
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本計算器可幫助您計算出特定溶液中溶質的質量、溶液濃度和體積之間的關系,公式為:
質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)