Pyridostigmine-d3 (bromide)
(Synonyms: 溴化吡啶斯的明 d3 (溴盐)) 目录号 : GC49424
An internal standard for the quantification of pyridostigmine
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pyridostigmine-d3 is intended for use as an internal standard for the quantification of pyridostigmine by GC- or LC-MS. Pyridostigmine is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE; IC50s = 0.35 and 1 μM, respectively, for the human enzymes).1 Pyridostigmine (10 µM) reduces decreases in AChE activity induced by the organophosphate pesticides diisopropyl fluorophosphate, chlorpyrifos-oxon, diazinon-oxon, paraoxon, and malaoxon in isolated bovine red blood cells.2 It also reduces soman-induced membrane depolarization and decreases in AChE activity in isolated human muscle bundles in a concentration-dependent manner.3 Pyridostigmine (3 mg/kg per day for four weeks) prevents tachycardia and increases in sympathetic tone in mice following myocardial infarction induced by left coronary artery ligation.4 Formulations containing pyridostigmine have been used in the treatment of myasthenia gravis and as neuromuscular protective agents against organophosphate poisoning.
1.Strelnik, A.D., Petukhov, A.S., Zueva, I.V., et al.Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profileBioorg. Med. Chem. Lett.26(16)4092-4094(2016) 2.Henderson, J.D., Glucksman, G., Leong, B., et al.Pyridostigmine bromide protection against acetylcholinesterase inhibition by pesticidesJ. Biochem. Mol. Toxicol.26(1)31-34(2012) 3.Maselli, R.A., Henderson, J.D., Ng, J., et al.Protection of human muscle acetylcholinesterase from soman by pyridostigmine bromideMuscle Nerve43(4)591-595(2011) 4.Durand, M.T., Becari, C., de Oliveira, M., et al.Pyridostigmine restores cardiac autonomic balance after small myocardial infarction in micePLoS One9(8)e104476(2014)
| Cas No. | N/A | SDF | |
| 别名 | 溴化吡啶斯的明 d3 (溴盐) | ||
| Canonical SMILES | O=C(N(C)C)OC1=C[N+](C([2H])([2H])[2H])=CC=C1.[Br-] | ||
| 分子式 | C9H10D3N2O2·Br | 分子量 | 264.1 |
| 溶解度 | Water: 100 mg/ml | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7864 mL | 18.9322 mL | 37.8644 mL |
| 5 mM | 0.7573 mL | 3.7864 mL | 7.5729 mL |
| 10 mM | 0.3786 mL | 1.8932 mL | 3.7864 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Metabolism of bromide and its interference with the metabolism of iodine
Physiol Res 2004;53 Suppl 1:S81-90.PMID:15119938doi
The present knowledge about the metabolism of bromide with respect to its goitrogenic effects, including some conclusions drawn from our recent research on this subject, is reviewed. Firstly, the biological behavior of bromide ion is compared with that of chloride and iodide. Secondly, the details about distribution and kinetics of bromide ions in the body and in 15 different organs and tissues of the rat are given. Significant correlation between the values of the steady-state concentration of bromide in the respective tissue and of the corresponding biological half-life was found in most tissues examined. A remarkably high concentration of radiobromide was found in the skin, which represents, due to its large mass, the most abundant depot of bromide in the body of the rat. Thirdly, the effects of excessive bromide on the rat thyroid are summarized, along with the interference of exogenous bromide with the whole-body metabolism of iodine. It is suggested that high levels of bromide in the organism of experimental animals can influence their iodine metabolism in two parallel ways: by a decrease in iodide accumulation in the thyroid and skin (and in the mammary glands in lactating dams), and by a rise in iodide excretion by kidneys. By accelerating the renal excretion of iodide, excessive bromide can also influence the pool of exchangeable iodide in the thyroid. Finally, our recent results concerning the influence of high bromide intake in the lactating rat dam on iodine and bromide transfer to the suckling, and the impact of seriously decreased iodine content and increased bromide concentration in mother's milk on the young are discussed. We must state, however, that the virtue of the toxic effects of excessive bromide on the thyroid gland and its interference with the biosynthesis of thyroid hormones, as well as the exact mechanism of bromide interference with postnatal developmental processes remains to be elucidated.
The toxicology of bromide ion
Crit Rev Toxicol 1987;18(3):189-213.PMID:3325227DOI:10.3109/10408448709089861.
Inorganic bromide is widely distributed in nature. Its natural physiological role in animal life is unknown. More than a century ago bromide was introduced in medicine as an antiepileptic drug. Nowadays, man is primarily exposed to bromide via food as the result of use of bromide-containing fumigants in intensive horticulture and in the treatment of food stocks. In this review exposure of man to bromide is described, and the pharmacological and toxicological effects of bromide ion are discussed.
[Bromism or chronic bromide poisoning]
Klin Padiatr 1993 Nov-Dec;205(6):432-4.PMID:8309208DOI:10.1055/s-2007-1025264.
Bromism, the chronic intoxication with bromide is rare and has been almost forgotten. In the recent past bromide is rediscovered as an anticonvulsive drug. The increasing frequency of bromism in children coming to admission induced this report. We describe the cause, the symptoms and the pseudohyperchloremia associated with bromism. If unclarified neurological or psychiatric symptoms are associated with the determination of an elevated serum chloride concentration and a diminished anion gap chronic intoxication with bromide has to be excluded.
bromide intoxication
Prescrire Int 1998 Dec;7(38):179.PMID:10848051doi
(1) A possible cause of asymptomatic "hyperchloraemia" or hyperchloraemia associated with neurological disorders. (2) Bromide-based preparations must not be prescribed or dispensed.
Oxidative treatment of bromide-containing waters: formation of bromine and its reactions with inorganic and organic compounds--a critical review
Water Res 2014 Jan 1;48:15-42.PMID:24184020DOI:10.1016/j.watres.2013.08.030.
bromide (Br(-)) is present in all water sources at concentrations ranging from ≈ 10 to >1000 μg L(-1) in fresh waters and about 67 mg L(-1) in seawater. During oxidative water treatment bromide is oxidized to hypobromous acid/hypobromite (HOBr/OBr(-)) and other bromine species. A systematic and critical literature review has been conducted on the reactivity of HOBr/OBr(-) and other bromine species with inorganic and organic compounds, including micropollutants. The speciation of bromine in the absence and presence of chloride and chlorine has been calculated and it could be shown that HOBr/OBr(-) are the dominant species in fresh waters. In ocean waters, other bromine species such as Br2, BrCl, and Br2O gain importance and may have to be considered under certain conditions. HOBr reacts fast with many inorganic compounds such as ammonia, iodide, sulfite, nitrite, cyanide and thiocyanide with apparent second-order rate constants in the order of 10(4)-10(9)M(-1)s(-1) at pH 7. No rate constants for the reactions with Fe(II) and As(III) are available. Mn(II) oxidation by bromine is controlled by a Mn(III,IV) oxide-catalyzed process involving Br2O and BrCl. Bromine shows a very high reactivity toward phenolic groups (apparent second-order rate constants kapp ≈ 10(3)-10(5)M(-1)s(-1) at pH 7), amines and sulfamides (kapp ≈ 10(5)-10(6)M(-1)s(-1) at pH 7) and S-containing compounds (kapp ≈ 10(5)-10(7)M(-1)s(-1) at pH 7). For phenolic moieties, it is possible to derive second-order rate constants with a Hammett-σ-based QSAR approach with [Formula in text]. A negative slope is typical for electrophilic substitution reactions. In general, kapp of bromine reactions at pH 7 are up to three orders of magnitude greater than for chlorine. In the case of amines, these rate constants are even higher than for ozone. Model calculations show that depending on the bromide concentration and the pH, the high reactivity of bromine may outweigh the reactions of chlorine during chlorination of bromide-containing waters.