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Scopolamine:Chem Biodivers. 2021 Sep 12. doi: 10.1002/cbdv.202100341.
Purity: ≥98%
Scopolamine HBr, also known as Hyoscine, is the hydrobromide salt of scopolamine which is a competitive and non-selective antagonist of muscarinic acetylcholine receptor with an IC50 of 55.3 nM. Scopolamine is an approved medication used to treat motion sickness and postoperative nausea and vomiting. It is also occasionally used before surgery to decrease saliva. When used by injection effects begin after about 20 minutes and last for up to 8 hours. It may also be used by mouth and as a skin patch.
ln Vitro |
When applied alone, scopolane does not elicit a response from oocytes expressing 5-HT3 receptors. However, when 2 μM 5-HT is also applied concurrently, the reaction is concentration-dependently inhibited. Scopolamine's pIC50 value is 5.68±0.05 (IC50=2.09 μM, n=6), and its hill slope is 1.06 ± 0.05. The resulting Kb was 3.23 μM. When Scopolamine is delivered during the 5-HT administration, the same concentration-dependent impact is observed. The competitiveness of unlabeled Scopolamine is evaluated with [3H]granisetron, a proven high-affinity competitive antagonist at these receptors, in order to further investigate a potential competitive binding to the 5-HT3 receptor. With 0.6 nM [3H]granisetron (~ Kd), scopolamine exhibits concentration-dependent competition, 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 has not changed much in the histopathology investigation. 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 hippocampal regions[2]. When compared to the normal group (3.06±0.296), the administration of Scopolamine alone significantly enhances the activity of the Acetylcholinesterase enzyme (AchE) (7.98±0.065; P<0.001). Malondialdehyde (MDA) levels in the Scopolamine-treated rats are significantly higher (34.61±4.85; P<0.01) than in the control group (12.82±2.86). Compared to the normal group (0.3906±0.02), the scopolamine-treated group exhibits a significant drop 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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Animal Protocol |
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References |
[1]. Lochner M, et al. The muscarinic antagonists Scopolamine and atropine are competitive antagonists at 5-HT3 receptors. Neuropharmacology. 2016 Sep;108:220-8.
[2]. O ET, et al. 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]. Pattanashetti LA, et al. Evaluation of neuroprotective effect of Quercetin with Donepezil in Scopolamine-induced amnesia in rats. Indian J Pharmacol. 2017 Jan-Feb;49(1):60-64 |
Molecular Formula |
C17H21NO4.HBR
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Molecular Weight |
384.26
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CAS # |
114-49-8
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SMILES |
Br[H].O1[C@]2([H])[C@@]3([H])C([H])([H])C([H])(C([H])([H])[C@@]([H])([C@]12[H])N3C([H])([H])[H])OC([C@@]([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C([H])([H])O[H])=O
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6024 mL | 13.0120 mL | 26.0240 mL | |
5 mM | 0.5205 mL | 2.6024 mL | 5.2048 mL | |
10 mM | 0.2602 mL | 1.3012 mL | 2.6024 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.