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首页 / 抑制剂/激动剂 / 神经信号通路 / AChR / Hexamethonium Bromide/六甲溴铵

Hexamethonium Bromide/六甲溴铵 {[allProObj[0].p_purity_real_show]}

货号：A139736 同义名： 溴化六甲铵 / Hexamethonium (bromide)

Hexamethonium Bromide是一种尼古丁型胆碱受体拮抗剂，是典型的神经节阻滞药。

Hexamethonium Bromide/六甲溴铵 化学结构 CAS号：55-97-0
Hexamethonium Bromide/六甲溴铵 化学结构
CAS号：55-97-0
Hexamethonium Bromide/六甲溴铵 3D分子结构
CAS号：55-97-0
Hexamethonium Bromide/六甲溴铵 化学结构 CAS号：55-97-0
Hexamethonium Bromide/六甲溴铵 3D分子结构 CAS号：55-97-0
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Hexamethonium Bromide/六甲溴铵 纯度/质量文件 产品仅供科研

货号：A139736 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 AChE ↓ AChR ↓ mAChR ↓ nAChR ↓ 其他靶点 纯度
Donepezil +++

hAChE, IC50: 11.6 nM

bAChE, IC50: 8.12 nM

 		98%
Loganin ++

AChE, IC50: 3.95 μM

 		99%+
topride HCl ++

AChE, IC50: 2.04 μM

 		98%
Dehydroevodiamine HCl ✔ 99%+
Jatrorrhizine ++

AChE, IC50: 872 nM

 		99%+
Palmatine ++

AChE, IC50: 0.51 μM

 		95%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

 		98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

 		98%
Trospium chloride ✔ 99%
Tiotropium Bromide Monohydrate ✔ 97%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

 		98%
Hexamethonium Bromide ✔ 99%
Pancuronium dibromide ✔ 98%
Neostigmine bromide ✔ 98%
Orphenadrine citrate ✔ 98%
Oxybutynin ✔ 98%
Irsogladine ✔ PDE 99%
Pyridostigmine bromide ✔ 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

 		98%
Paroxetine HCl ✔ 99%
Rocuronium Bromide ✔ 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

 		98%
Diphenmanil methylsulfate ✔ 97%
Umeclidinium bromide ✔ 95%
Otilonium bromide ✔ 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

 		99%
Ipratropium bromide ✔ 98%
Diphenidol HCl ✔ 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

 		98%
Aclidinium Bromide ++++

M4 mAChR, Ki: 0.21 nM

M2 mAChR, Ki: 0.1 nM

 		98%
Oxybutynin chloride ✔ 99%
Pentoxyverine citrate ✔ 98%
Solifenacin ✔ 98%
Catharanthine ✔ 98%
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

 		99+%
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

 		99%
PNU-120596 ++

α7 nAChR, EC50: 216 nM

 		99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Hexamethonium Bromide/六甲溴铵 生物活性

靶点

  • AChR
描述 Hexamethonium Bromide is effective against Ach and carbachol (CCh) on the amplitude of endplate responses of rat omohyoid muscle with EC50 of 300 μM and 100 μM, respectively. Hexamethonium Bromide is also a weak inhibitor of acetylcholinesterase activity in rat muscle homogenates with EC50 of 1.5 mM[3]. At low frequencies of stimulation (0.5-2 Hz), hexamethonium (200 mM) and methyllycaconitine (2.0 mM) increased e.p.c. quantal content by 30-40%. The low frequency augmentation of e.p.c. quantal content by hexamethonium was absent when extracellular [Ca2+] was lowered from 2.0 to 0.5 mM[4].

Hexamethonium Bromide/六甲溴铵 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Neuropathic pain model Intravenous injection 30 mg/kg Single dose, 15 min before IR surgery To investigate the effect of hexamethonium bromide on neuropathic pain-induced cardioprotection. Results showed that hexamethonium bromide abolished the SNI-induced cardioprotection. Nat Commun. 2017 Oct 10;8(1):826
Female Danish landrace pigs Anesthetized pig model Intravenous injection 8 mg/kg Two injections, interval not specified To evaluate the effect of hexamethonium on GLP-1-induced heart rate increase, results showed that GLP-1 still increased heart rate even after hexamethonium administration Cardiovasc Res. 2024 Oct 14;120(12):1427-1441
Spontaneously Hypertensive Rats (SHR) Spontaneously Hypertensive Rat Model Intravenous injection 20 mg/kg BW Single dose Assessed indirect sympathetic nervous system activity, showing enhanced depressor response in SHRs, which was restored to normal levels after TLR4 blockade. Pharmacol Res. 2021 Dec;174:105877
Mice Smooth muscle-specific STIM1 knockout mice Intraperitoneal injection 5 mg/kg Single injection To study the effect of STIM1 deletion on blood pressure, results showed that STIM1 knockout mice had a more pronounced reduction in BP after sympathetic blockade Cardiovasc Res. 2018 Apr 1;114(5):668-678
Rats Ischemia-reperfusion injury model Perfusion 50 μM 5 minutes pretreatment and during dialysate perfusion To investigate the effect of hexamethonium bromide on remote ischemic conditioning (RIC)-mediated cardioprotection. Results showed that 50 μM hexamethonium bromide abrogated the cardioprotection mediated by RIC dialysate. Basic Res Cardiol. 2016 Jul;111(4):50
Male Sprague-Dawley rats Isolated perfused rat heart model Perfusion 50 μM 5 min prior to and during the 3-cycle preconditioning To investigate the role of hexamethonium bromide in ischemic preconditioning, results showed that hexamethonium bromide blocked the protective effect of IPC. Basic Res Cardiol. 2017 Mar;112(2):11
Male Wistar rats Pithed rat model Intravenous infusion 2 mg/kg·min Continuous infusion To block the electrically-induced vasopressor responses J Headache Pain. 2018 May 25;19(1):40
BPH/2J mice Genetically hypertensive model Intraperitoneal injection 10 mg/kg Measured on control day 3 and postoperative day 10 To measure global neurogenic pressor activity. The depressor response to hexamethonium in the RDNX group was significantly smaller on postoperative day 10 compared with baseline control, whereas no such effect was observed in SHAM or CGX groups. Hypertension. 2021 Feb;77(2):519-528

Hexamethonium Bromide/六甲溴铵 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03360136 Exhaustion; Syndrome ... 展开 >> Burnout, Professional Burnout Syndrome Adjustment Disorders 收起 << Not Applicable Recruiting July 1, 2020 Sweden ... 展开 >> PBM Sweden AB Globen Recruiting Stockholm, Södermanland, Sweden, 12177 Contact: Gunilla Brodda Jansen, Assoc. Proff.    070-716 39 13 ext +46    gunillabroddajansen@pbm.se    PBM Sweden City Recruiting Stockholm, Uppland, Sweden, 114 47 Contact: Gunilla Brodda Jansen, Assoc. Proff.    070-716 39 13 ext +46    gunillabroddajansen@pbm.se 收起 <<
NCT03468114 Enteric Infections ... 展开 >> Diarrhea 收起 << Not Applicable Recruiting December 2018 Kenya ... 展开 >> Great Lakes University Kisumu Recruiting Kisumu, Kenya Contact: Sheillah Simiyu, PhD    +254 722 215291    sheillahshie@gmail.com 收起 <<
NCT01626703 Depression Sc... 展开 >>reening Elderly 收起 << Not Applicable Completed - Korea, Republic of ... 展开 >> Chungju community health care center Chungju, Choongbuk, Korea, Republic of, 123456 收起 <<

Hexamethonium Bromide/六甲溴铵 参考文献

[1]Tian L, Prior C, et al. Hexamethonium- and methyllycaconitine-induced changes in acetylcholine release from rat motor nerve terminals. Br J Pharmacol. 1997 Nov;122(6):1025-34.

[2]Rang HP, Rylett RJ. The interaction between hexamethonium and tubocurarine on the rat neuromuscular junction. Br J Pharmacol. 1984 Mar;81(3):519-31.

[3]Rang HP, Rylett RJ. The interaction between hexamethonium and tubocurarine on the rat neuromuscular junction. Br J Pharmacol. 1984 Mar;81(3):519-31.

[4]Tian L, Prior C, Dempster J, Marshall IG. Hexamethonium- and methyllycaconitine-induced changes in acetylcholine release from rat motor nerve terminals. Br J Pharmacol. 1997 Nov;122(6):1025-34.

Hexamethonium Bromide/六甲溴铵 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.80mL

2.76mL

1.38mL

27.61mL

5.52mL

2.76mL

Hexamethonium Bromide/六甲溴铵 技术信息

CAS号55-97-0
分子式C12H30Br2N2
分子量 362.19
SMILES Code C[N+](C)(C)CCCCCC[N+](C)(C)C.[Br-].[Br-]
MDL No. MFCD00011787
别名 溴化六甲铵 ;Hexamethonium (bromide)
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 16 mg/mL(44.18 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(276.1 mM)

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Hexamethonium | 55-97-0 | nAChR Antagonist | Membrane Transporter/Ion Channel | Neuronal Signaling | Apoptosis | nAChR | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Hexamethonium Bromide/六甲溴铵 纯度/质量文件 | Hexamethonium Bromide/六甲溴铵 亚型比较 | Hexamethonium Bromide/六甲溴铵 生物活性 | Hexamethonium Bromide/六甲溴铵 临床数据 | Hexamethonium Bromide/六甲溴铵 参考文献 | Hexamethonium Bromide/六甲溴铵 实验方案 | Hexamethonium Bromide/六甲溴铵 技术信息

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