Size | Price | Stock | Qty |
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5mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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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 |
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Additional Infomation |
Scopolamine hydrobromide appears as colorless crystals or white powder or solid. Has no odor. pH (of 5% solution): 4-5.5. Slightly efflorescent in dry air. Bitter, acrid taste. (NTP, 1992)
Scopolamine hydrobromide (anhydrous) is a hydrobromide that is obtained by reaction of scopolamine with hydrogen bromide. It has a role as a muscarinic antagonist. It contains a scopolamine(1+). Scopolamine Hydrobromide is the hydrobromide salt form of scopolamine, a tropane alkaloid derived from plants of the nightshade family (Solanaceae), specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic and antivertigo properties. Structurally similar to acetylcholine, scopolamine antagonizes acetylcholine activity mediated by muscarinic receptors located on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. The agent is used to cause mydriasis, cycloplegia, to control the secretion of saliva and gastric acid, to slow gut motility, and prevent vomiting. An alkaloid from SOLANACEAE, especially DATURA and SCOPOLIA. Scopolamine and its quaternary derivatives act as antimuscarinics like ATROPINE, but may have more central nervous system effects. Its many uses include an anesthetic premedication, the treatment of URINARY INCONTINENCE and MOTION SICKNESS, an antispasmodic, and a mydriatic and cycloplegic. |
Molecular Formula |
C17H21NO4.HBR
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Molecular Weight |
384.26
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Exact Mass |
383.073
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CAS # |
114-49-8
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Related CAS # |
Scopolamine;51-34-3;Scopolamine butylbromide;149-64-4;Scopolamine hydrobromide trihydrate;6533-68-2;Scopolamine hydrochloride;55-16-3
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PubChem CID |
6603108
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Appearance |
White to off-white solid powder
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Boiling Point |
460.3ºC at 760 mmHg
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Melting Point |
195-199 °C (dry matter)(lit.)
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Vapour Pressure |
2.51E-10mmHg at 25°C
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LogP |
1.814
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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.Br
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InChi Key |
WTGQALLALWYDJH-WYHSTMEOSA-N
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InChi Code |
InChI=1S/C17H21NO4.BrH/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;hydrobromide
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Synonyms |
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.