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Methscopolamine

Muscarinic acetylcholine receptor blocker CAS# 155-41-9

Methscopolamine

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Chemical structure

Methscopolamine

3D structure

Chemical Properties of Methscopolamine

Cas No. 155-41-9 SDF Download SDF
PubChem ID 9072 Appearance Powder
Formula C18H24BrNO4 M.Wt 398.29
Type of Compound N/A Storage Desiccate at -20°C
Synonyms (-)-Scopolamine methyl bromide; Hyoscine methyl bromide
Solubility H2O : 50 mg/mL (125.54 mM; Need ultrasonic)
DMSO : ≥ 34 mg/mL (85.36 mM)
*"≥" means soluble, but saturation unknown.
SMILES C[N+]1(C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4)C.[Br-]
Standard InChIKey CXYRUNPLKGGUJF-ODDNLWGVSA-M
Standard InChI InChI=1S/C18H24NO4.BrH/c1-19(2)14-8-12(9-15(19)17-16(14)23-17)22-18(21)13(10-20)11-6-4-3-5-7-11;/h3-7,12-17,20H,8-10H2,1-2H3;1H/q+1;/p-1/t12?,13?,14-,15-,16-,17+;/m0./s1
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.
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.
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.

Biological Activity of Methscopolamine

DescriptionMethscopolamine (Pamine) is a muscarinic acetylcholine receptor blocker. Target: mAChR Methylscopolamine is an oral medication used along with other medications to treat peptic ulcers by reducing stomach acid secretion. With the advent of proton pump inhibitors and antihistamine medications it is rarely used for this. It can also be used for stomach or intestinal spasms, to reduce salivation, and to treat motion sickness. From Wikipedia. Methscopolamine (Pamine), an anti-acetylcholine drug, prevented ulcer formation, reduced further volume and acid output but produced a 3-4 fold increase in hexosamine concentration. Tissue (corpus and antrum) hexosamine was moderately reduced by restraint. In the corpus, this was counteracted by methscopolamine but antrum hexosamine was not influenced by this drug. The anti-ulcer property of methscopolamine may be due not only to its effect on acid secretion but also to the rise in gastric mucus concentration that it produced [1].

References:
[1]. Robert, A. and J.E. Nezamis, Effect of an Anti-Acetylcholine Drug, Methscopolamine Bromide, on Ulcer Formation and Gastric Mucus. J Pharm Pharmacol, 1964. 16: p. 690-5. [2]. Kong Q, et al. Effects of pharmacological treatments on hippocampal NCAM1 and ERK2 expression in epileptic rats with cognitive dysfunction. Oncol Lett. 2016 Sep;12(3):1783-1791.

Methscopolamine Dilution Calculator

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Methscopolamine Molarity Calculator

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Preparing Stock Solutions of Methscopolamine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5107 mL 12.5537 mL 25.1073 mL 50.2147 mL 62.7683 mL
5 mM 0.5021 mL 2.5107 mL 5.0215 mL 10.0429 mL 12.5537 mL
10 mM 0.2511 mL 1.2554 mL 2.5107 mL 5.0215 mL 6.2768 mL
50 mM 0.0502 mL 0.2511 mL 0.5021 mL 1.0043 mL 1.2554 mL
100 mM 0.0251 mL 0.1255 mL 0.2511 mL 0.5021 mL 0.6277 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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Background on Methscopolamine

Methscopolamine (Pamine) is a muscarinic acetylcholine receptor blocker.Methylscopolamine is an oral medication used along with other medications to treat peptic ulcers by reducing stomach acid secretion. With the advent of proton pump inhibitors and anti

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References on Methscopolamine

Determination of phenylephrine hydrochloride, chlorpheniramine maleate, and methscopolamine nitrate in tablets or capsules by liquid chromatography with two UV absorbance detectors in series.[Pubmed:16512228]

J AOAC Int. 2006 Jan-Feb;89(1):53-7.

A procedure is presented for the simultaneous determination of phenylephrine HCI (PE), chlorpheniramine maleate (CM), and Methscopolamine nitrate in commercial tablets or capsules by liquid chromatography (LC) with 2 UV absorbance detectors in series. Reference and sample solutions are prepared in methanol. LC separations are performed on a 7.5 cm Novapak silica column. The mobile phase is prepared by mixing 930 mL methanol with 70 mL of a 0.5% aqueous solution of 1-pentanesulfonic acid, sodium salt. The injection volume is 20 microL; the flow rate is approximately 1 mL/min. Retention times are approximately 1.5 min for PE, 3 min for CM, and 6 min for Methscopolamine nitrate. One detector determines the first 2 compounds at 265 nm, but the third compound does not produce a detectable peak. The other detector set at 210 nm generates peaks for all 3 compounds, but only Methscopolamine is within the recorder range; the other 2 compounds are exceedingly off scale. If it is not feasible or desirable to arrange 2 UV absorbance detectors in series, separate determinations can be made, one for the first 2 compounds and the other for the third component of the mixture. Two commercial samples of tablets and 2 commercial samples of capsules were analyzed by the proposed method. Recovery studies were also conducted with amounts of the 3 compounds ranging from 80 to 120% of the quantities present in the sample solutions.

The muscarine antagonist methscopolamine and the NMDA antagonist AP-5 injected unilaterally into the nucleus accumbens cause mice to rotate in opposite directions.[Pubmed:8695045]

J Neural Transm Gen Sect. 1995;101(1-3):149-57.

Previously, we have reported that the NMDA antagonist AP-5, injected unilaterally into the nucleus accumbens of mice, induces ipsilateral rotation in monoaminergically intact mice, but contralateral rotation in monoamine-depleted animals. In this paper we report that the muscarine antagonist Methscopolamine, injected unilaterally into the nucleus accumbens, induced predominantly contralateral rotation in monoaminergically intact mice. In monoamine-depleted animals intra-accumbens Methscopolamine induced only a weak stimulation of rotational behaviour (not significant), but the direction of the rotation was exclusively contralateral, and the animals showed contralateral body deviation. Moreover, when these animals received additional treatment with the alpha-adrenergic agonist clonidine, which potentiates the motor effects of cholinergic antagonists in monoamine-depleted mice (Carlsson et al., 1991), a clear-cut contralateral rotation was induced. The observed behavioural effects are discussed in relation to the positive and negative feedback circuits, which link the nucleus accumbens with the cerebral cortex and thalamus. In previous papers, we have suggested that the ipsilateral rotation induced by AP-5 is mediated primarily by the positive feedback circuit, whereas the AP-5-induced contralateral rotation is due to interference with primarily the negative feedback circuit. Applying this reasoning to the rotational effects of Methscopolamine, it seems that Methscopolamine interferes primarily with the negative feedback circuit.

Reducing milk production in ewes at weaning using restricted feeding and methscopolamine bromide.[Pubmed:9250502]

J Anim Sci. 1997 Jun;75(6):1434-42.

Restricted feed (RF) and Methscopolamine bromide (MB), an anticholinergic agent reported to block growth hormone secretion, were evaluated as potential means for reducing milk production in ewes at weaning. On d 58 +/- 1 postpartum (d 0), 40 fall-lambing ewes were allotted to treatments in a 2 (RF vs full feed [FF]) x 2 (MB vs saline [SAL]) factorial arrangement according to breed, age, and number of lambs born and suckled. On d 0 at 0800, ewes were separated from lambs, injected with 40 IU of oxytocin, and machine milked 30 s later. Ewes remained separated from lambs for 3 h, and at 1100 they were milked and yields were determined. From d 0 through 6, FF ewes received a daily ration of 1.8 kg of alfalfa hay and .9 kg of corn; RF ewes received only 1.8 kg of alfalfa hay. On d 7 at 0800 and 1400, ewes were separated from lambs, milked, treated with a s.c. injection of either 96 mg of MB dissolved in 2 mL of SA or SA alone, and after 3-h separations were milked at 1100 and 1700 and yields determined. Lambs were weaned at 1400. After milking at 1700, all ewes were placed in drylot without feed or water. At 1100 on d 9, residual milk yields were collected. Milk samples were retained for compositional analysis at each collection time. The RF ewes produced less milk than FF ewes (106 vs 137.4 g; P < .01) at 1100 on d 7, but yields of MB and SA ewes were similar. At 1700 on d 7, milk yield was only 15.9 g less (74.3 vs 90.2 g; P < .10) for RF than for FF ewes, but it was 26 g less (69.2 vs 95.2 g; P < .01) for MB than for SA ewes. On d 9, there was no significant difference in yields of RF and FF ewes; however, MB ewes continued to produce less milk than SA ewes (96.6 vs 125.4 g; P < .10). No significant interactions between feeding regimen and MB treatment were found for milk yield. These data provide evidence that MB treatment of ewes is effective in reducing milk production. Furthermore, even greater reduction can be achieved when MB is combined with RF.

Methscopolamine bromide blocks hypothalamic-stimulated release of growth hormone in ewes.[Pubmed:9159285]

J Anim Sci. 1997 May;75(5):1359-62.

Twenty-five nonlactating ewes were used to test the hypothesis that Methscopolamine bromide (MB) blocks secretion of growth hormone (GH) by affecting hypothalamic rather than pituitary mechanisms. Ewes were randomly assigned to receive a s.c. injection of 96 mg of MB or 2 mL of saline at min = 0. Saline-treated ewes were assigned to receive a subsequent (at +60 min) i.v. injection of 10 microg of growth hormone-releasing hormone (GHRH) to test pituitary responsiveness or .3 mg of clonidine to test hypothalamic responsiveness. Methscopolamine bromide-treated ewes were assigned to receive a subsequent (at +60 min) i.v. injection of 10 microg of GHRH, .3 mg of clonidine, or 2 mL of saline. Jugular blood samples were collected at 10-min intervals from -120 min to +240 min, and serum concentrations of GH were quantified with a RIA. No difference was detected in serum concentrations of GH with respect to MB vs saline treatment (P = .20). Concentrations of GH increased in saline-pretreated ewes following injections of clonidine or GHRH (P < .01). Treatment of ewes with MB, however, limited the ability of clonidine-induced mechanisms to increase concentrations of GH, but did not affect pituitary responsiveness to GHRH (P < .01). These data support the hypothesis that MB inhibits hypothalamic and not pituitary mediated mechanisms that regulate the secretion of GH.

Description

Methscopolamine (Pamine) is a muscarinic acetylcholine receptor blocker.

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