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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| 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]. |
| 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 |
| 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 |
| 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 | - | - | |
| 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 |
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| 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) 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
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