质量水平
检测方案
≥97% (NMR)
形式
solid
颜色
white
溶解性
H2O: >20 mg/mL
储存温度
2-8°C
SMILES字符串
O.Cl.Cl.Cl.Cl.COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc2ccccc2OC.COc3ccccc3CNCCCCCCNCCCCCCCCNCCCCCCNCc4ccccc4OC
InChI
1S/2C36H62N4O2.4ClH.H2O/c2*1-41-35-23-13-11-21-33(35)31-39-29-19-9-7-17-27-37-25-15-5-3-4-6-16-26-38-28-18-8-10-20-30-40-32-34-22-12-14-24-36(34)42-2;;;;;/h2*11-14,21-24,37-40H,3-10,15-20,25-32H2,1-2H3;4*1H;1H2
InChI key
XIIINYPADNNZHA-UHFFFAOYSA-N
基因信息
human ... CHRM2(1129)
一般描述
甲辛胺(N, N′-双[6-[[((2-甲氧基苯基)-甲基]己基] -1,8-辛烷]二胺)是聚亚甲基四胺的衍生物。
应用
水合甲辛胺:
- 作为毒蕈碱受体 2 的拮抗剂已用于。
- 作为测试分子,检查其对 HGPS(Hutchinson-Gilford 早衰综合症)iPS(诱导多能性)衍生的间充质干细胞的过早成骨分化的影响。
生化/生理作用
美索曲明是 nM 浓度下的选择性 M2 毒蕈碱受体拮抗剂。在 mM 浓度下,美索曲明直接抑制 G 蛋白的高亲和力 GTPase 活性。在食管肌肉中,M2 受体拮抗剂美索曲明可降低乙酰胆碱介导的钙和花生四烯酸释放的增加。在背外侧纹状体两侧注入美索曲明,使得认知功能受损的老年大鼠记忆力显著增强。美索曲明在毒蕈碱受体分类中起着至关重要的作用。
美索曲明是 nM 浓度下的选择性 M2 毒蕈碱受体拮抗剂。在 mM 浓度下,美索曲明直接抑制 G 蛋白的高亲和力 GTPase 活性。M2 受体拮抗剂美索曲明可降低钙和花生四烯酸释放的增加,但 M3 受体拮抗剂对氟-六氢-硅杂-地芬尼多不能。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
The Journal of pharmacology and experimental therapeutics, 335(3), 622-635 (2010-09-02)
The novel quaternary ammonium salt (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino]carbonyl]oxy]-1-[2-oxo-2-(2-thienyl)ethyl]-1-azoniabicyclo[2.2.2]octane bromide (CHF5407) showed subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2), and M3 (hM3) receptors and dissociated very slowly from hM3 receptors (t(½) = 166 min) with a large part of the receptorial
Developmental neuroscience, 38(6), 407-419 (2017-04-27)
The development of the nervous system involves the initial overproduction of synapses, which promotes connectivity. Hebbian competition between axons with different activities leads to the loss of roughly half of the overproduced elements and this refines connectivity. We used quantitative
Chemico-biological interactions, 181(3), 409-416 (2009-07-07)
Methoctramine and its analogues are polymethylene tetramines that selectively bind to a variety of receptor sites. Although these compounds are widely used as pharmacological tools for receptor characterization, the toxicological properties of these polyamine-based structures are largely unknown. We have
Presynaptic Muscarinic Acetylcholine Receptors and TrkB Receptor Cooperate in the Elimination of Redundant Motor Nerve Terminals during Development.
Frontiers in Aging Neuroscience, 9, 24-24 (2017)
British journal of pharmacology, 127(4), 1021-1029 (1999-08-05)
1. The effects of spermine and methoctramine, a selective M2 muscarinic receptor antagonist, were studied on the high-affinity GTPase activity of G proteins, and on ligand binding to M2 muscarinic receptors in pig heart sarcolemma. 2. The spontaneous GTP hydrolysis
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