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Merck
CN

M105

美索曲明 水合物

≥97% (NMR), muscarinic receptor 2 antogonist, solid

别名:

N,N′-bis[6-[[(2-甲氧基苯基)甲基]氨基]己基] -1,8-辛烷二胺 四盐酸盐 水合物, 美索曲明 四盐酸盐 水合物

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关于此项目

经验公式(希尔记法):
C36H62N4O2 · 4HCl · xH2O
化学文摘社编号:
分子量:
728.75 (anhydrous basis)
UNSPSC Code:
12352116
PubChem Substance ID:
NACRES:
NA.32
MDL number:
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产品名称

美索曲明 水合物, ≥97% (NMR), solid

SMILES string

O.Cl.Cl.Cl.Cl.COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc2ccccc2OC.COc3ccccc3CNCCCCCCNCCCCCCCCNCCCCCCNCc4ccccc4OC

InChI key

XIIINYPADNNZHA-UHFFFAOYSA-N

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

assay

≥97% (NMR)

form

solid

color

white

solubility

H2O: >20 mg/mL

storage temp.

2-8°C

Quality Level

Gene Information

human ... CHRM2(1129)

Biochem/physiol Actions

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。
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。

General description

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。

Application

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。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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R E Delmendo et al.
British journal of pharmacology, 96(2), 457-464 (1989-02-01)
1. A range of muscarinic receptor antagonists were examined for affinity at the M1 muscarinic binding site, present in rat cerebrocortical membranes and the M2 muscarinic binding sites of rat cardiac and submaxillary gland membranes. 2. The results obtained were
U D Sohn et al.
Cellular signalling, 12(4), 215-222 (2000-04-27)
We have previously shown that acetylcholine-induced contraction of oesophageal circular muscle depends on activation of phosphatidylcholine selective phospholipase C and D, which result in formation of diacylglycerol, and of phospholipase 2 which produces arachidonic acid. Diacylglycerol and arachidonic acid interact
A High Throughput Phenotypic Screening reveals compounds that counteract premature osteogenic differentiation of HGPS iPS-derived mesenchymal stem cells.
Lo Cicero A
Scientific Reports, 6:34798 (2016)
Wei Wu et al.
Neurobiology of learning and memory, 98(1), 41-46 (2012-05-09)
Microinfusions of the nonselective muscarinic antagonist scopolamine into perirhinal cortex impairs performance on visual recognition tasks, indicating that muscarinic receptors in this region play a pivotal role in recognition memory. To assess the mnemonic effects of selective blockade in perirhinal
Neus Garcia et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 30(49), 16514-16522 (2010-12-15)
The neurotrophin brain-derived neurotrophic factor (BDNF), neurotrophin-4 (NT-4) and the receptors tropomyosin-related kinase B (trkB) and p75(NTR) are present in the nerve terminals on the neuromuscular junctions (NMJs) of the levator auris longus muscle of the adult mouse. Exogenously added

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