Muscarinic acetylcholine receptors.

A 30-hr period of restraint in rats was followed by the appearance of ulcers in the gastric corpus coincidental with a marked reduction of gastric juice volume, acid and also of hexosamine which was used as an estimation of mucus content. 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]

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In rats, 30 - hour restraint can lead to the appearance of ulcers in the gastric corpus, accompanied by a significant decrease in gastric juice volume, acid, and hexosamine (used to estimate mucus content). Methscopolamine Bromide can prevent ulcer formation, further reduce the volume and acid output, and increase the hexosamine concentration by 3 - 4 times. The drug can counteract the decrease in hexosamine in the gastric corpus caused by restraint, but has no effect on the hexosamine in the antrum. Its anti - ulcer effect may be related not only to its inhibitory effect on acid secretion but also to the increase in gastric mucus concentration [1].

Animal Protocol：The literature used rats as experimental animals, and the rats were restrained for 30 hours to induce gastric ulcers. However, the literature did not describe the specific dissolution formula, dosage form, administration frequency, and administration route of Methscopolamine Bromide, only indicating that the drug was used for relevant interventions during the experiment to observe its effect on ulcer formation and gastric mucus - related indicators [1].

Absorption, Distribution and Excretion
Absorption
Poorly and unreliably absorbed, total absorption is 10-25%.

Metabolism / Metabolites
Little is known about the fate and excretion of methscopolamine.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the use of methscopolamine bromide during breastfeeding. Because methscopolamine bromide is a quaternary ammonium compound, it is not likely to be absorbed and reach the bloodstream of the infant. Long-term use of methscopolamine bromide might reduce milk production or milk letdown, but a single dose is unlikely to interfere with breastfeeding. During long-term use, observe for signs of decreased lactation (e.g., insatiety, poor weight gain).
To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information in nursing mothers was not found as of the revision date. Anticholinergics can inhibit lactation in animals, apparently by inhibiting growth hormone and oxytocin secretion. Anticholinergic drugs can also reduce serum prolactin in nonnursing women. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

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5459110 human TDLo intramuscular 1 ug/kg SENSE ORGANS AND SPECIAL SENSES: MYDRIASIS (PUPILLARY DILATION): EYE Possible Long-Term Health Effects of Short-Term Exposure to Chemical Agents, National Research Council, 3 vols., Washington, DC, National Academy Press, 1982-85, 1(L1), 1982
5459110 rat LD50 intravenous 42500 ug/kg BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY); BEHAVIORAL: ATAXIA; LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION Toxicology and Applied Pharmacology., 1(391), 1959 5459110 rat LD50 intraduodenal 870 mg/kg Archives Internationales de Pharmacodynamie et de Therapie., 180(155), 1969 [PMID:5357002]
5459110 mouse LD50 oral 619 mg/kg BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD Therapie., 14(1096), 1959 [PMID:14435525]
5459110 mouse LD50 intraperitoneal 150 mg/kg Journal of the American Chemical Society., 79(4451), 1957

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

Scopolamine methobromide is a quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide. It has a role as a muscarinic antagonist, an antiemetic, an antispasmodic drug and a parasympatholytic. It is a quaternary ammonium salt and a bromide salt. It is functionally related to a scopolamine.
A muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.
See also: Methscopolamine Bromide (annotation moved to).

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The literature mainly explores the effect of Methscopolamine Bromide on ulcer formation and gastric mucus, suggesting that it has a protective effect on the gastric mucosa, and its mechanism may be related to reducing acid secretion and increasing mucus concentration [1].

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Pharmacodynamics: Methscopolamine is a muscarinic antagonist structurally similar to the neurotransmitter acetylcholine and acts by blocking the muscarinic acetylcholine receptors and is thus classified as an anticholinergic. Methscopolamine has many uses including the prevention of motion sickness. It is not clear how Methscopolamine prevents nausea and vomiting due to motion sickness. The vestibular part of the ear is very important for balance. When a person becomes disoriented due to motion, the vestibule sends a signal through nerves to the vomiting center in the brain, and vomiting occurs. Acetylcholine is a chemical that nerves use to transmit messages to each other. It is believe that Methscopolamine prevents communication between the nerves of the vestibule and the vomiting center in the brain by blocking the action of acetylcholine. Methscopolamine also may work directly on the vomiting center. Methscopolamine must be taken before the onset of motion sickness to be effective.

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Mechanism of Action: Methscopolamine acts by interfering with the transmission of nerve impulses by acetylcholine in the parasympathetic nervous system (specifically the vomiting center). It does so by acting as a muscarinic antagonist.

C18H24BRNO4

398.29

397.088

C, 54.28; H, 6.07; Br, 20.06; N, 3.52; O, 16.07

155-41-9

13265-10-6 (cation);155-41-9 (bromide);6106-46-3 (nitrate);

5459110

White to off-white solid powder

-24 ° (C=1, H2O)

1

5

5

24

454

5

[Br-].O1[C@@]2([H])[C@]1([H])[C@]1([H])C([H])([H])C([H])(C([H])([H])[C@@]2([H])[N+]1(C([H])([H])[H])C([H])([H])[H])OC([C@@]([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C([H])([H])O[H])=O

CXYRUNPLKGGUJF-OZVSTBQFSA-M

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+;/m1./s1

[(1S,2S,4R,5R)-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-7-yl] (2S)-3-hydroxy-2-phenylpropanoate;bromide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)