Neostigmine BromideCholinesterase inhibitor CAS# 114-80-7 |
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Quality Control & MSDS
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| Cas No. | 114-80-7 | SDF | Download SDF |
| PubChem ID | 8246 | Appearance | Powder |
| Formula | C12H19BrN2O2 | M.Wt | 303.2 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Eustigmin bromide; Neoserine bromide | ||
| Solubility | DMSO : ≥ 38 mg/mL (125.33 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | [3-(dimethylcarbamoyloxy)phenyl]-trimethylazanium;bromide | ||
| SMILES | CN(C)C(=O)OC1=CC=CC(=C1)[N+](C)(C)C.[Br-] | ||
| Standard InChIKey | LULNWZDBKTWDGK-UHFFFAOYSA-M | ||
| Standard InChI | InChI=1S/C12H19N2O2.BrH/c1-13(2)12(15)16-11-8-6-7-10(9-11)14(3,4)5;/h6-9H,1-5H3;1H/q+1;/p-1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Neostigmine Bromide is a cholinesterase inhibitor used in the treatment of myasthenia gravis.
Target: Cholinesterase
Neostigmine is a parasympathomimetic that acts as a reversible acetylcholinesterase inhibitor. Neostigmine enhances excitatory parasympathetic activity by competing with acetylcholine for attachment to acetylcholinesterase at sites of cholinergic transmission and enhancing cholinergic action. Neostigmine is a safe and effective treatment for acute colonic pseudo-obstruction [1]. References: | |||||
Neostigmine Bromide Dilution Calculator
Neostigmine Bromide Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2982 mL | 16.4908 mL | 32.9815 mL | 65.9631 mL | 82.4538 mL |
| 5 mM | 0.6596 mL | 3.2982 mL | 6.5963 mL | 13.1926 mL | 16.4908 mL |
| 10 mM | 0.3298 mL | 1.6491 mL | 3.2982 mL | 6.5963 mL | 8.2454 mL |
| 50 mM | 0.066 mL | 0.3298 mL | 0.6596 mL | 1.3193 mL | 1.6491 mL |
| 100 mM | 0.033 mL | 0.1649 mL | 0.3298 mL | 0.6596 mL | 0.8245 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Neostigmine bromide is a reversible inhibitor of acetylcholinesterase.[1]
AChE (acetylcholinesterase) is a hydrolase that hydrolyzes the neurotransmitter acetylcholine at the neuromuscular junction and cholinergic synaspe. It terminates the signal transductions and plays a role in neuronal apoptosis.
Neostigmine bromide is a quaternary amine that blocked cholinesterase activity to extend and enhance the muscarinic and nicotinic effects of acetylcholine. It is implicated for the treatment of primary open-angle glaucoma, postoperative urinary retention, paralytic ileus, myasthenia gravis etc. It is also reported to be an adjuvant to local anaesthetics and opioids for post-surgical pain after gynaecological or abdominal surgery. [1]
Reference:
[1] El-Kosasy AM, Nebsen M, Abd El-Rahman MK, Salem MY, El-Bardicy MG. Comparative study of 2-hydroxy propyl beta cyclodextrin and calixarene as ionophores in potentiometric ion-selective electrodes for neostigmine bromide. Talanta. 2011 Aug 15;85(2):913-8.
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Modified carbon paste sensor for the potentiometric determination of neostigmine bromide in pharmaceutical formulations, human plasma and urine.[Pubmed:23948245]
Biosens Bioelectron. 2014 Jan 15;51:143-9.
A novel, simple, rapid, selective and sensitive method for the determination of neostigmine (Ns) ion in its bulk powder, different pharmaceutical dosage forms, and biological fluids (plasma and urine) using four modified carbon paste electrodes was developed. Sensor 1 is based on ion-association Ns-TPB, sensor 2 used Ns-PT, sensor 3 comprises a mixture of (Ns-PT+Ns-TPB) and sensor 4 was constructed using (Ns-PT+beta-CD). Solvent mediator 2-NPPE exhibited a proper behavior including Nernstian slope ranging from 61.5+/-0.5 to 64.5+/-0.5 mV per decade over the pH range of 3.8-10 for the four sensors. Linear responses of Ns within the concentration range 1.0x10(-7)-1.0x10(-2) mol/L were obtained. The response time is very short (
Comparative study of 2-hydroxy propyl beta cyclodextrin and calixarene as ionophores in potentiometric ion-selective electrodes for neostigmine bromide.[Pubmed:21726718]
Talanta. 2011 Aug 15;85(2):913-8.
Three novel Neostigmine Bromide (NEO) selective electrodes were investigated with 2-nitrophenyl octyl ether as a plasticiser in a polymeric matrix of polyvinyl chloride (PVC). Sensor 1 was fabricated using tetrakis(4-chlorophenyl)borate (TpClPB) as an anionic exchanger without incorporation of an ionophore. Sensor 2 used 2-hydroxy propyl beta-cyclodextrin as an ionophore while sensor 3 was constructed using 4-sulfocalix-8-arene as an ionophore. Linear responses of NEO within the concentration ranges of 10(-5) to 10(-2), 10(-6) to 10(-2) and 10(-7) to 10(-2) mol L(-1) were obtained using sensors 1, 2 and 3, respectively. Nernstian slopes of 51.6 +/- 0.8, 52.9 +/- 0.6 and 58.6 +/- 0.4 mV/decade over the pH range of 4-9 were observed. The selectivity coefficients of the developed sensors indicated excellent selectivity for NEO. The utility of 2-hydroxy propyl beta-cyclodextrin and 4-sulfocalix[8]arene as ionophores had a significant influence on increasing the membrane sensitivity and selectivity of sensors 2 and 3 compared to sensor 1. The proposed sensors displayed useful analytical characteristics for the determination of NEO in bulk powder, different pharmaceutical formulations, and biological fluids (plasma and cerebrospinal fluid (CSF)) and in the presence of its degradation product (3-hydroxyphenyltrimethyl ammonium bromide) and thus could be used for stability-indicating methods.
[Correlation between in vitro release and in vivo absorption of sustained-releasing tablets of neostigmine bromide].[Pubmed:23600216]
Sichuan Da Xue Xue Bao Yi Xue Ban. 2013 Jan;44(1):80-3.
OBJECTIVE: To determine the correlation between in vitro release and in vivo absorption of sustained-releasing tablets of Neostigmine Bromide. METHODS: Water was used as dissolution medium to measured in vitro release of Neostigmine Bromide. After a single oral administration of 100 mg Neostigmine Bromide to rabbits, the plasma concentrations of Neostigmine Bromide in the rabbits were determined by HPLC. The compartment model and deconvolution method were employed to explain the in vitro-in vivo correlation. RESULTS: Using Y as cumulative in vitro release and Fa as percentage of absorption, the regression equation was established: Fa = 0.9298Y + 4.6074, r = 0.9961. The input function of R = 2.0163Y-11.242,r = 0.9270. CONCLUSION: The correlation between in vitro release and in vivo absorption of Neostigmine Bromide is good.
[Pharmacokinetics and relative bioavailability of neostigmine bromide sustained-release tablets].[Pubmed:22007493]
Sichuan Da Xue Xue Bao Yi Xue Ban. 2011 Sep;42(5):657-60.
OBJECTIVE: To study the pharmacokinetics and relative bioavailability of Neostigmine Bromide conventional tablets and sustained-release tablets in rabbits. METHODS: Six healthy rabbits were randomly divided into two groups for a cross self-contrast trial. RP-HPLC was used to detect plasma concentrations of Neostigmine Bromide. The pharmacokinetic parameters were calculated with the aid of DAS 2.0 software. RESULTS: The main pharmacokinetics parameters of the sustained-release tablets and conventional tablets were as follows, respectively: T(max)(3.67 +/- 1.51) hand (1.58 +/- 0.38) h; C(max) (5.04 +/- 1.19) mg/L and (4.56 +/- 1.70) mg/L; AUC(0 --> infinity) (32.82 +/- 9.88) mg/L x h and (29.84 +/- 14.27) mg/L x h. The relative bioavailability of the Neostigmine Bromide sustained-release tablets was 115.4%. CONCLUSION: The pharmacokinetics of Neostigmine Bromide accords with two compartments model, showing constant plasma concentration and relatively high bioavailability.
