Muscarinic acetylcholine receptors.

大鼠被束缚 30 小时后，胃体出现溃疡，同时胃液量、胃酸和用于估计粘液含量的己糖胺也显著减少。甲基东莨菪碱 (Pamine) 是一种抗乙酰胆碱药物，可防止溃疡形成，进一步减少体积和酸排出，但使己糖胺浓度增加 3-4 倍。组织（胃体和胃窦）的己糖胺因束缚而适度减少。在胃体中，甲基东莨菪碱 可抵消这种影响，但胃窦己糖胺不受此药影响。甲基东莨菪碱 的抗溃疡特性可能不仅归因于其对酸分泌的影响，还归因于其产生的胃粘液浓度升高。[1]

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在大鼠中，30小时束缚可导致胃体出现溃疡，同时胃液体积、胃酸和己糖胺（用于估算黏液含量）显著减少。溴甲东莨菪碱可预防溃疡形成，进一步减少胃液体积和胃酸分泌，并使己糖胺浓度增加3至4倍。该药物可抵消束缚引起的胃体己糖胺减少，但对胃窦的己糖胺无影响。其抗溃疡作用可能不仅与抑制胃酸分泌有关，还与胃黏液浓度升高有关[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)

59.06

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)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。