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 absorbed and unstable, with a total absorption rate of 10-25%.
Metabolism/Metabolites
Little is known about the metabolism and excretion of methyl scopolamine.

Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation
There is currently no information regarding the use of metoclopramide bromide during lactation. Because metoclopramide bromide is a quaternary ammonium compound, it is unlikely to be absorbed by the infant and enter the bloodstream. Long-term use of metoclopramide bromide may reduce milk production or the milk ejection reflex, but a single dose is unlikely to interfere with breastfeeding. With prolonged use, observe for signs of reduced milk production (e.g., dissatisfaction, poor weight gain).
After using eye drops, to significantly reduce the amount of medication entering breast milk, press the tear duct at the corner of the eye for at least 1 minute, then blot away excess medication with absorbent paper.
◉ Effects on Breastfed Infants
No published information found as of the revision date.
◉ Effects on Lactation and Breast Milk
No published information found regarding breastfeeding mothers as of the revision date. Anticholinergic drugs can inhibit lactation in animals, possibly by suppressing the secretion of growth hormone and oxytocin. Anticholinergic drugs can also lower serum prolactin levels in non-lactating women. Prolactin levels in established lactating mothers may not affect their ability to breastfeed.

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5459110 Human TDLo 1 ug/kg IM Sensory organs and special senses: pupillary dilation: long-term health effects of short-term exposure to chemicals, National Research Council, Vol. 3, Washington, D.C., National Academy of Sciences Press, 1982-85, 1(L1), 1982
5459110 Rat LD50 42500 ug/kg IV Behavior: somnolence (general activity inhibition); Behavior: ataxia; Lung, pleural or respiratory: respiratory depression, Toxicology and Applied Pharmacology, 1(391), 1959; 5459110 Rat duodenal LD50 870 mg/kg, Archives of International Pharmacodynamics and Therapeutics, 180(155), 1969 [PMID:5357002]; 5459110 Mouse oral LD50 619 mg/kg; Behavior: Seizures or Effects on Epilepsy Threshold, Therapeutics, 14(1096), 1959 [PMID:14435525]; 5459110 Intraperitoneal LD50 in mice 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 produced by the reaction of the amino group of scopolamine with bromomethane. It has the effects of muscarinic receptor antagonist, antiemetic, antispasmodic and parasympathetic nerve blocker. It is a quaternary ammonium salt and bromide salt that is functionally related to scopolamine.
A muscarinic receptor antagonist used to study the binding characteristics of muscarinic cholinergic receptors.
See also: sconibromoscopolamine (note moved to).

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The literature mainly discusses the effects of sconibromoscopolamine on ulcer formation and gastric mucus, indicating that it has a protective effect on the gastric mucosa, and its mechanism may be related to reducing gastric acid secretion and increasing mucus concentration[1]. Pharmacodynamics: Methionine bromide is a muscarinic receptor antagonist with a structure similar to the neurotransmitter acetylcholine. It works by blocking muscarinic acetylcholine receptors and is therefore classified as an anticholinergic drug. Methionine bromide has a wide range of uses, including the prevention of motion sickness. It is currently unclear how methionine bromide prevents nausea and vomiting caused by motion sickness. The vestibular system of the ear is crucial for balance. When a person loses their sense of direction due to movement, the vestibular system sends signals to the vomiting center in the brain via nerves, triggering vomiting. Acetylcholine is the chemical substance that transmits information between nerves. It is believed that methionine bromide blocks the action of acetylcholine, thus preventing the transmission of information between the vestibular nerve and the vomiting center in the brain. Methionine bromide may also act directly on the vomiting center. Methionine bromide must be taken before the onset of motion sickness to be effective. Mechanism of action: Methionine bromide exerts its effect by interfering with the transmission of acetylcholine nerve impulses in the parasympathetic nervous system, particularly the vomiting center. It achieves this effect by acting as a muscarinic receptor 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.)