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Scopolamine:Chem Biodivers. 2021 Sep 12. doi: 10.1002/cbdv.202100341.
"]Scopolamine HCl (Hyoscine), the hydrochloride salt of Scopolamine, is a drug approved for the treatment of motion sickness and postoperative nausea and vomiting. It functions as a non-selective and competitive antagonist of the muscarinic acetylcholine receptor with an IC50 of 55.3 nM.
| Targets |
5-HT3 Receptor ( IC50 = 2.09 μM ); mAChR
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|---|---|
| ln Vitro |
When applied alone to oocytes expressing 5-HT3 receptors, Scopolamine does not elicit a response. However, when 2 μM 5-HT is also applied concurrently, the response is concentration-dependently inhibited. With a Hill Slope of 1.06 ± 0.05, the pIC50 value for Scopolamine is 5.68±0.05 (IC50=2.09 μM, n=6). As a result, 3.23 μM was the Kb. Applying Scopolamine concurrently with the 5-HT application results in the same concentration-dependent effect. In order to investigate the possibility of a competitive binding at the 5-HT3 receptor, [3H]granisetron, a well-known high-affinity competitive antagonist at these receptors, is used to measure the competition of unlabelled Scopolamine. A concentration-dependent competition is seen with 0.6 nM [3H]granisetron (~Kd) for scopopolamine, resulting in an average pKi of 5.17±0.24 (Ki=6.76 μM, n=3)[1].
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| ln Vivo |
The histology of the brain shows no discernible changes in the histopathology study. On the other hand, it is noted that the control mice given Scopolamine and given only distilled water showed a decrease in cell density in their hippocampus[2]. When compared to the normal group's 3.06±0.296 activity, the administration of Scopolamine alone significantly increases the activity of the Acetylcholinesterase enzyme (AchE) (7.98±0.065; P<0.001). In comparison to the normal group (12.82±2.86), the animals treated with Scopolamine report significantly higher levels of malondialdehyde (MDA) (34.61±4.85; P<0.01). In comparison to the normal group (0.3906±0.02), the scopolamine-treated group exhibits a significant decrease in reduced glutathione (GSH) levels (P<0.001; 0.1504±0.03). The concentration of β amyloid (Aβ1-42) in the rats treated with Scopolamine is significantly higher (P<0.001; 146.2±1.74) than in the control group (43.21±3.46)[3].
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| Enzyme Assay |
In order to measure saturation binding (8 point) curves, 0.5 mL incubations containing 10 mM HEPES buffer (pH 7.4), 0.1-1 nM [3H]granisetron or 1-10 nM [3H]N-methylScopolamine are incubated with either crude extracts of HEK 293 cells stably expressing 5-HT3 receptors or Guinea pig membrane preparations. The same receptor preparations are incubated in 0.5 mL HEPES buffer containing either 0.6 nM [3H]granisetron or 0.6 nM [3H]N-methylScopolamine, as well as varying concentrations of competing ligands, in order to determine competition binding (10 point). One can measure non-specific binding using quipazine at 1 mM or Scopolamine at 10 μM, respectively. Filtration onto Whatman GF/B filters wetted with HEPES buffer + 0.3% polyethyleneimine is used to end the incubations. This is followed by two quick washes with ice-cold HEPES buffer. Using standards for bovine serum albumin, a Lowry protein assay is used to determine the protein concentration. Tri-Carb 2100 TR scintillation counters are used to measure radioactivity[1].
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| Animal Protocol |
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 14th 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 (Aβ1-42), an ELISA kit is utilized. Rat brains are used to dissect the hippocampus and examine any histopathological abnormalities. |
| References |
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| Molecular Formula |
C17H22CLNO4
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|---|---|
| Molecular Weight |
339.81388
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| Exact Mass |
339.123
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| Elemental Analysis |
C, 60.09; H, 6.53; Cl, 10.43; N, 4.12; O, 18.83
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| CAS # |
55-16-3
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| Related CAS # |
Scopolamine; 51-34-3; Scopolamine hydrobromide; 114-49-8; Scopolamine butylbromide; 149-64-4; Scopolamine hydrobromide trihydrate; 6533-68-2
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| PubChem CID |
6852406
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| Appearance |
Solid powder
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| Boiling Point |
460.3ºC at 760mmHg
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| Flash Point |
232.2ºC
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| LogP |
1.658
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
418
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CN1[C@@H]2CC(C[C@H]1[C@H]3[C@@H]2O3)OC(=O)[C@H](CO)C4=CC=CC=C4.Cl
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| InChi Key |
KXPXJGYSEPEXMF-WYHSTMEOSA-N
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| InChi Code |
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
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| Chemical Name |
[(1S,2S,4R,5R)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] (2S)-3-hydroxy-2-phenylpropanoate;hydrochloride
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| Synonyms |
Hyoscine hydrochloride; Scopolamine hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~250 mg/mL (~650.6 mM)
H2O: ≥ 100 mg/mL (~260.2 mM) |
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9428 mL | 14.7141 mL | 29.4282 mL | |
| 5 mM | 0.5886 mL | 2.9428 mL | 5.8856 mL | |
| 10 mM | 0.2943 mL | 1.4714 mL | 2.9428 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03616067 | Recruiting | Drug: Botox® injection Drug: Scopoderm® patches arm |
Cerebral Palsy | Hospices Civils de Lyon | April 27, 2022 | Phase 3 |
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