5-HT₃ Receptor ( IC50 = 2.09 μM ); mAChR

东莨菪碱阻断烟碱型乙酰胆碱受体 (IC50=928 μM) 并增加 α7 nACh 受体的表达。东莨菪碱与 0.6 nM [3H]格拉司琼呈浓度依赖性竞争，平均 pKi 为 5.17±0.24 (Ki=6.76 μM)。荧光标记形式的格拉司琼 (G-FL) 与东莨菪碱的浓度依赖性竞争产生的平均 pKi 为 5.31±0.09 (Ki=4.90 μM)。东莨菪碱会阻断毒蕈碱受体并诱导认知缺陷[1]。东莨菪碱（0.1-3 mM；持续 24 小时）诱导 SH-SY5Y 细胞的细胞毒性、ROS 生成和凋亡[2]。细胞活力测定[2] 细胞系：人神经母细胞瘤 SH-SY5Y 细胞系 浓度：0.1-3 mM（通常为 2 mM） 孵育时间：24 小时 结果：暴露于 1-3 mM 24 小时显着降低人神经母细胞瘤 SH-SY5Y细胞活力呈剂量依赖性。在所有后续实验中，2 M 导致细胞活力损失 50.6±2.2%。

东莨菪碱会导致与胆碱能神经传递减弱相关的记忆障碍，以及与大脑氧化应激相关的过程增加[3]。动物模型：体重 20-25[3] 的幼稚雄性瑞士小鼠 剂量：1 mg/kg 给药方式：腹膜内 (ip) 给药；为了测量记忆获取过程，在预测试前 20 分钟服用东莨菪碱；为了测量记忆巩固过程，在预测试后立即给予东莨菪碱结果：在东莨菪碱治疗组中，与盐水治疗组相比，潜伏期指数（IL）值显着下降，表明东莨菪碱在使用的剂量会损害记忆和学习的获得。

为了测量饱和结合（8 点）曲线，0.5 mL 孵育液含有 10 mM HEPES 缓冲液（pH 7.4）、0.1-1 nM [³H]格拉司琼或 1-10 nM [^{将 3}H]N-甲基东莨菪碱与稳定表达 5-HT₃ 受体的 HEK 293 细胞的粗提物或豚鼠膜制剂一起孵育。将相同的受体制剂在含有 0.6 nM [³H]格拉司琼或 0.6 nM [³H]N-甲基东莨菪碱以及不同浓度的 0.5 mL HEPES 缓冲液中孵育竞争配体，以确定竞争结合（10 分）。可以分别使用 1 mM 的喹嗪或 10 μM 的东莨菪碱来测量非特异性结合。过滤到用 HEPES 缓冲液 + 0.3% 聚乙烯亚胺润湿的 Whatman GF/B 过滤器上以结束孵育。然后用冰冷的 HEPES 缓冲液快速洗涤两次。使用牛血清白蛋白的标准品，使用 Lowry 蛋白质测定来确定蛋白质浓度。 Tri-Carb 2100 TR 闪烁计数器用于测量放射性[1]。

Mice: After the mice are weighed, labeled, and divided into seven groups of five animals each, 3 mg/kg of Scopolamine is pre-injected intraperitoneally into each group. For three days in a row, groups 1-3 receive 0.2 mL equivalent doses of 4 mg/kg, 6 mg/kg, and 8 mg/kg of the Morinda lucida extract, groups 4-6 receive the same doses of Peltophorum pterocarpum extract, and group 7 receives 0.2 mL of distilled water (negative control).
Rats: In this work, healthy male Wistar rats, 12 months of age, weighing 180–200 g, are employed. Group I comprises of six rats; Group II is for disease control (Scopolamine hydrobromide 3 mg/kg, i.p. ); Group III is for Scopolamine+Quercetin (25 mg/kg, p.o. ); Group IV is for standard treatment (Scopolamine+Donepezil hydrochloride 3 mg/kg, p.o. ); and Group V is for Scopolamine+Quercetin (25 mg/kg, p.o.)+Donepezil (3 mg/kg, p.o.). For a period of 14 days, the rats in groups III, IV, and V receive their prescribed doses of medication every 24 hours. The 14^th day is dedicated to the acquisition trail for the Morris water maze, elevated plus maze, and passive avoidance paradigm. Following the acquisition trail, all groups—aside from the normal control group—receive an injection of scopolamine (3 mg/kg, i.p.) on the same day, which causes cognitive impairment in rats. The fifteenth day is dedicated to testing memory retention; on the same day, rats are killed and brain tissues are removed in order to measure the levels of the enzyme acetylcholinesterase (AchE) and markers of brain oxidative stress, such as reduced glutathione (GSH) and lipid peroxidase (LPO). To estimate the level of β amyloid (Aβ_1-42), an ELISA kit is utilized. Rat brains are used to dissect the hippocampus and examine any histopathological abnormalities.

[1]. The muscarinic antagonists Scopolamine and atropine are competitive antagonists at 5-HT3 receptors. Neuropharmacology. 2016 Sep;108:220-8.

[2]. COGNITIVE-ENHANCING PROPERTIES OF MORINDA LUCIDA (RUBIACEAE) AND PELTOPHORUM PTEROCARPUM (FABACEAE) IN SCOPOLAMINE-INDUCED AMNESIC MICE. Afr J Tradit Complement Altern Med. 2017 Mar 1;14(3):136-141.

[3]. Evaluation of neuroprotective effect of Quercetin with Donepezil in Scopolamine-induced amnesia in rats. Indian J Pharmacol. 2017 Jan-Feb;49(1):60-64.

C17H22CLNO4

339.81388

339.12

C, 60.09; H, 6.53; Cl, 10.43; N, 4.12; O, 18.83

55-16-3

Scopolamine; 51-34-3; Scopolamine hydrobromide; 114-49-8; Scopolamine butylbromide; 149-64-4; Scopolamine hydrobromide trihydrate; 6533-68-2

Solid powder

CN1[C@@H]2CC(C[C@H]1[C@H]3[C@@H]2O3)OC(=O)[C@H](CO)C4=CC=CC=C4.Cl

KXPXJGYSEPEXMF-WYHSTMEOSA-N

InChI=1S/C17H21NO4.ClH/c1-18-13-7-11(8-14(18)16-15(13)22-16)21-17(20)12(9-19)10-5-3-2-4-6-10;/h2-6,11-16,19H,7-9H2,1H3;1H/t11?,12-,13-,14+,15-,16+;/m1./s1

[(1S,2S,4R,5R)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] (2S)-3-hydroxy-2-phenylpropanoate;hydrochloride

Hyoscine hydrochloride; Scopolamine hydrochloride

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)

DMSO: ~250 mg/mL (~650.6 mM)
H2O: ≥ 100 mg/mL (~260.2 mM)

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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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。