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Pyridostigmine bromide/溴化吡啶斯的明 {[allProObj[0].p_purity_real_show]}

货号:A725388 同义名: 溴吡斯的明 / Pyridostigmine (bromide); Ro 1-5130

Pyridostigmine bromide 是一种可逆性胆碱酯酶抑制剂,常被用于研究重症肌无力。

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Pyridostigmine bromide/溴化吡啶斯的明 化学结构 CAS号:101-26-8
Pyridostigmine bromide/溴化吡啶斯的明 化学结构
CAS号:101-26-8
Pyridostigmine bromide/溴化吡啶斯的明 3D分子结构
CAS号:101-26-8
Pyridostigmine bromide/溴化吡啶斯的明 化学结构 CAS号:101-26-8
Pyridostigmine bromide/溴化吡啶斯的明 3D分子结构 CAS号:101-26-8
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Pyridostigmine bromide/溴化吡啶斯的明 生物活性

靶点
  • AChR

描述 Pyridostigmine bromide, a reversible inhibitor of cholinesterase, has been used to treat myasthenia gravis, reverse neuromuscular blockade, and prevent nerve gas (ie, soman) poisoning[3]. Pyridostigmine bromide may act on the heart, at least partially increasing the vagal parasympathetic activity, via the accumulation of acetylcholine in the myocardium[4]. Pyridostigmine(Bromide) significantly attenuated cardiac hypertrophy based on reduction in left ventricular weight/body weight, suppression of the levels of atrial natriuretic peptide, brain natriuretic peptide and β‐myosin heavy chain, and a reduction in cardiac fibrosis. [5].

Pyridostigmine bromide/溴化吡啶斯的明 细胞实验

Cell Line
Concentration Treated Time Description References
Colonic myenteric plexus neurons and glia 250 µM 3 hours To investigate the effects of PB and PEA on the activity of enteric neurons and glia. Results showed that PB pretreatment significantly reduced glial Ca2+ responses to PEA (61.0% decrease) and shifted the signaling mechanisms between neurons and glia from TRPV1-dependent to CB1 receptor- and PPARα-dependent pathways. Neuropharmacology. 2020 Nov 15;179:108264
Rat neural progenitor cells 200 µM 6 days To evaluate the effect of PY on cell viability, results showed PY did not affect cell viability at 200 μM Neurochem Res. 2015 Oct;40(10):2091-101

Pyridostigmine bromide/溴化吡啶斯的明 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Adult male Sprague Dawley rats Acute diisopropylfluorophosphate (DFP) intoxication model Intramuscular injection 0.1 mg/kg Single dose, 30 minutes before DFP injection To evaluate the effect of PB pretreatment on survival and brain AChE activity in DFP-intoxicated rats. Results showed no significant effect of PB pretreatment on 24-hour survival or brain AChE activity. Neurotoxicology. 2019 Jul;73:81-84
Wistar rats Myocardial infarction model Drinking water administration 0.14 mg/mL Daily administration for 12 weeks To evaluate the effects of PYR alone or combined with exercise on left ventricle dimensions and function, baroreflex sensitivity, autonomic parameters, and systemic and tissue inflammatory profile after myocardial infarction. Results showed that PYR alone or combined with exercise improved the deleterious effects of MI, with additional benefits in skeletal muscle anti-inflammatory state when combined with resistance training. Front Physiol. 2018 Feb 12;9:53
Rats Gulf War Illness model Oral gavage 1.3 mg/kg Once daily for 14 days To evaluate the effects of pyridostigmine bromide and stress on immune function and cholinergic neurochemistry. Results showed that pyridostigmine bromide and stress interact to enhance immune responses and alter cholinergic neurochemistry. Brain Behav Immun. 2019 Aug;80:384-393
Male Sprague Dawley rats Gulf War Illness (GWI) model Oral gavage 1.3 mg/kg Once daily for 14 days To assess the long-term effects of pyridostigmine bromide and repeated restraint stress on the cholinergic anti-inflammatory pathway. Results showed that PB treatment led to enhanced cholinergic responses and paradoxical increases in pro-inflammatory cytokine release in the prefrontal cortex and hippocampus. Neurobiol Stress. 2022 Apr 15;18:100446
Sprague Dawley rats Gulf War Illness model Oral gavage 1.3 mg/kg Once daily for 14 days To investigate the effects of PB and repeated restraint stress (RRS) on glutamatergic neurochemistry, showing that PB and stress interacted to produce brain-region specific effects on glutamate neurochemistry. Neurobiol Stress. 2019 Dec 31;12:100210
Rats Gulf War Illness model Oral gavage 1.3 mg/kg Once daily for 14 days To evaluate the effects of pyridostigmine bromide and stress on cognitive function in a model of Gulf War Illness. Results showed that PB-treated rats exhibited hippocampal-dependent memory deficits at a delayed timepoint. Brain Behav Immun. 2023 Oct;113:248-258
Mice Anti-muscle-specific kinase (MuSK) myasthenia gravis model Subcutaneous minipump 16 mg/kg/day Continuous for 7–9 days Pyridostigmine treatment exacerbated the anti-MuSK-induced reductions in postsynaptic acetylcholine receptor density and endplate potential (EPP) amplitude. J Physiol. 2013 May 15;591(10):2747-62
Male C57BL/6J mice Gulf War Illness model Subcutaneous injection 2 mg/kg Once daily for 14 days To evaluate the long-term effects of pyridostigmine bromide on behavior and neuroinflammation in a Gulf War Illness model. Results showed that pyridostigmine bromide, in combination with other chemicals, led to hyperactivity, impaired sensorimotor function, and altered gait in mice. Brain Behav Immun Health. 2022 Nov 8;26:100553
Mice Pressure overload heart failure model Subcutaneous osmotic pump 2-10 mg/kg/day Once daily for 28 days To study the effects of PYR on cardiac function and rhythmicity in heart failure mice, results showed PYR improved cardiac contractile performance and rhythmic activity J Cell Mol Med. 2021 May;25(10):4637-4648
Mice Rosa26-DTMlc2v-Cre mouse model Subcutaneous osmotic pump 3 mg/kg/d Continuous administration for 7 days, followed by 3-5 days post-DT injection To investigate the effect of pyridostigmine on inflammatory responses following myocardial injury. Results showed that pyridostigmine treatment significantly reduced mortality, cardiac inflammation, and infiltration of MHC-IIloCCR2+ monocytes in DT-injected Rosa26-DTMlc2v-Cre mice, and decreased CCL2/7 mRNA and protein expression. JCI Insight. 2019 Jun 4;5(14):e128961
C57BL/6J mice Chronic Chagasic cardiomyopathy mouse model Oral 30 mg/kg Daily for 30 days To assess the effects of pyridostigmine bromide on electrocardiographic, autonomic, histopathological, immunoinflammatory, and parasitological parameters in chronic Chagas disease in mice. Results showed that pyridostigmine bromide significantly reduced myocardial inflammatory infiltration, fibrosis, and hypertrophy, accompanied by a decrease in serum IFN-γ levels, suggesting a shift toward an anti-inflammatory immune response. Mediators Inflamm. 2014;2014:475946
Sprague Dawley rats Cardiac hypertrophy induced by abdominal aorta constriction Oral 31 mg/kg/day Once daily for 8 weeks Pyridostigmine increased acetylcholine levels by inhibiting acetylcholinesterase, significantly attenuated cardiac hypertrophy, improved cardiac function, inhibited the CaN/NFAT3/GATA4 pathway, and suppressed Orai1/STIM1 complex formation. J Cell Mol Med. 2017 Sep;21(9):2106-2116
Spontaneous hypertensive rats (SHRs) Acute myocardial infarction model Gavage 40 mg/kg Once daily for seven days Pyridostigmine treatment increased parasympathetic tone, reduced M1/M2 macrophage ratio, decreased TNF levels in heart and spleen, and improved cardiac remodeling. Sci Rep. 2021 May 5;11(1):9563
Spontaneously hypertensive rats Spontaneously hypertensive rat model Oral (via drinking water) 5 mg/kg/day and 15 mg/kg/day Daily administration for 2 weeks To evaluate the effects of pyridostigmine bromide on hemodynamic, cardiac morphofunctional, and cardiovascular autonomic adaptations in spontaneously hypertensive rats. Results showed that pyridostigmine bromide reduced BP and HR, increased vagal participation in cardiac autonomic tonic balance, and improved cardiac function parameters. Sci Rep. 2021 Aug 25;11(1):17141
C57BL/6 mice Gulf War Illness model Drinking water 90 μg/mL 7 consecutive days To evaluate the long-term effects of PB on gastrointestinal motility and neuroimmune function. Results showed that PB exposure alone did not cause significant long-term changes at 5 months but dramatically altered the effects of subsequent PEA exposure, leading to significant changes in gut motility, ENS function, and immune responses, which were sex-dependent. Neuropharmacology. 2020 Nov 15;179:108264

Pyridostigmine bromide/溴化吡啶斯的明 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
NCT03619759 - Recruiting August 31, 2019 Korea, Republic of ... 展开 >> Ajou university school of medicine Recruiting Suwon, Gyeonggi-do, Korea, Republic of, 16377 Contact: In Kyong Yi, MD 收起 <<
NCT00624663 Rivastigmine Toxicity Not Applicable Completed - Israel ... 展开 >> Tel Aviv Sourasky Medical Center Tel Aviv, Israel Tasmc Clinical Research Center Tel-Aviv, Israel, 64239 收起 <<
NCT03468452 - Completed - -

Pyridostigmine bromide/溴化吡啶斯的明 参考文献

[1]Kanjwal K, Karabin B, et al. Pyridostigmine in the treatment of postural orthostatic tachycardia: a single-center experience. Pacing Clin Electrophysiol. 2011 Jun;34(6):750-5.

[2]Gales BJ, Gales MA. Pyridostigmine in the treatment of orthostatic intolerance. Ann Pharmacother. 2007 Feb;41(2):314-8.

[3]Tan Q, Jiang R, Xu M, Liu G, Li S, Zhang J. Nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics. Int J Nanomedicine. 2013;8:737-45. doi: 10.2147/IJN.S40860. Epub 2013 Feb 20. PMID: 23459707; PMCID: PMC3582480.

[4]de Cuba MB, Machado MP, Farnesi TS, Alves AC, Martins LA, de Oliveira LF, Capitelli CS, Leite CF, Silva MV, Machado JR, Kappel HB, de Campos HS, Paiva L, Gomes NL, Faleiros AC, Britto CF, Savino W, Moreira OC, Rodrigues V Jr, Montano N, Lages-Silva E, Ramirez LE, da Silva VJ. Effects of cholinergic stimulation with pyridostigmine bromide on chronic chagasic cardiomyopathic mice. Mediators Inflamm. 2014;2014:475946. doi: 10.1155/2014/475946. Epub 2014 Aug 24. PMID: 25221388; PMCID: PMC4158292.

[5]Lu Y, Zhao M, Liu JJ, He X, Yu XJ, Liu LZ, Sun L, Chen LN, Zang WJ. Long-term administration of pyridostigmine attenuates pressure overload-induced cardiac hypertrophy by inhibiting calcineurin signalling. J Cell Mol Med. 2017 Sep;21(9):2106-2116. doi: 10.1111/jcmm.13133. Epub 2017 Mar 10. PMID: 28296184; PMCID: PMC5571547.

Pyridostigmine bromide/溴化吡啶斯的明 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.83mL

0.77mL

0.38mL

19.15mL

3.83mL

1.91mL

38.30mL

7.66mL

3.83mL

Pyridostigmine bromide/溴化吡啶斯的明 技术信息

CAS号101-26-8
分子式C9H13BrN2O2
分子量 261.12
SMILES Code C[N+]1=CC=CC(OC(N(C)C)=O)=C1.[Br-]
MDL No. MFCD00079283
别名 溴吡斯的明 ;Pyridostigmine (bromide); Ro 1-5130; Pyridostigmine Br, Pyridostigmine; Kalimin; Regonol; Mestinon; NSC 679759
运输蓝冰
InChI Key VNYBTNPBYXSMOO-UHFFFAOYSA-M
Pubchem ID 7550
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature

溶解方案

DMSO: 50 mg/mL(191.49 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: 8.5 mg/mL(32.55 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
方案 三
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
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