| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
| Targets |
Biochemical
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|---|---|
| ln Vitro |
MAJOR ACTION OF ANTIMUSCARINIC AGENTS IS COMPETITIVE OR SURMOUNTABLE ANTAGONISM TO ACETYLCHOLINE AND OTHER MUSCARINIC AGONISTS
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| Toxicity/Toxicokinetics |
Human Toxicity Excerpt
In normal individuals, subcutaneous injection of 1 mg causes mydriasis and ciliary muscle paralysis lasting for several hours; however, subcutaneous or intramuscular injection of 0.5 mg has almost no effect on accommodation, and oral administration of 16 mg has no effect either. Grant, WM, Ocular Toxicology, 2nd ed., Springfield, Illinois: Charles C. Thomas, 1974, p. 16. 901 Non-Human Toxicity Excerpt Intraperitoneal injection of 1 mg/kg of methyl nitrate scopolamine (which does not readily cross the blood-brain barrier) into rats did not significantly impair the acquisition of conditioned inhibitory responses. This suggests that the interference of scopolamine on the acquisition of conditioned inhibitory responses is due to central effects. PMID: 5389067 Rats were trained to retrieve food particles from the end of each arm of an 8-arm radial maze. Baseline performance was characterized by very little entry into arms where food particles had already been retrieved. Intraperitoneal injection of dextroamphetamine sulfate (0.1–3.0 mg/kg) or sodium pentobarbital (1.0–10.0 mg/kg) did not affect selection accuracy, although arm entry rate increased after dextroamphetamine and decreased after sodium pentobarbital. Scopolamine hydrochloride (0.1–1.0 mg/kg) reduced selection accuracy and arm entry rate. Methoscopamine nitrate (0.17, 1.0 mg/kg) had almost no effect on experimental performance. Long-term administration of methoscopamine nitrate to female rats at doses far exceeding those required to block vagal nerve-mediated insulin secretion only reduced resting ventromedial hypothalamic obesity by 31%. Even with an 8-fold increase in the initial effective dose (0.15 mg/kg, four times daily), at least 59% of obesity persisted. Even with large doses of scopolamine, treatment initiated before the injury occurred failed to prevent damage to the ventromedial hypothalamus and weight gain. Ten days after the injury, decreased gastrointestinal motility appeared to prevent further weight gain. PMID:523552 |
| References |
[1]. https://pubchem.ncbi.nlm.nih.gov/compound/11957694
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| Additional Infomation |
Mechanism of Action
The main action of anticholinergic drugs is the competitive or reversible antagonism of acetylcholine and other muscarinic receptor agonists. /Anticholinergic Drugs/ Therapeutic Uses Parasympathetic blockers Anticholinergic drugs for treating functional diarrhea Anticholinergic drugs for treating hypermotility Anticholinergic drugs for treating peptic ulcers Anticholinergic, antispasmodic, and acid-suppressing agents |
| Molecular Formula |
C18H24N2O7
|
|---|---|
| Molecular Weight |
380.39
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| Exact Mass |
380.158
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| Elemental Analysis |
C, 56.83; H, 6.36; N, 7.36; O, 29.44
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| CAS # |
6106-46-3
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| PubChem CID |
11957694
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| Appearance |
White to off-white solid powder
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| Density |
1.31 g/cm3
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| Boiling Point |
460.3ºC at 760 mmHg
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| Melting Point |
199ºC
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| Flash Point |
232.2ºC
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| Index of Refraction |
-25 ° (C=1, H2O)
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| LogP |
1.305
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
27
|
| Complexity |
472
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C[N+]1(C2CC(CC1C3C2O3)OC(=O)[C@H](CO)C4=CC=CC=C4)C.[N+](=O)([O-])[O-]
|
| InChi Key |
BSQIVYOSLFLSGE-UXXRHRDBSA-N
|
| InChi Code |
InChI=1S/C18H24NO4.NO3/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;2-1(3)4/h3-7,12-17,20H,8-10H2,1-2H3;/q+1;-1/t12?,13-,14?,15?,16?,17?;/m1./s1
|
| Chemical Name |
(9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-7-yl) (2S)-3-hydroxy-2-phenylpropanoate;nitrate
|
| Synonyms |
(-)Scopolamine methyl nitrate; (-)-Scopolamine methyl nitrate; Hyoscine methyl nitrate; 6106-46-3; SCOPOLAMINE METHYL NITRATE;
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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. |
| 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) |
H2O: 250 mg/mL (657.22 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 | 2.6289 mL | 13.1444 mL | 26.2888 mL | |
| 5 mM | 0.5258 mL | 2.6289 mL | 5.2578 mL | |
| 10 mM | 0.2629 mL | 1.3144 mL | 2.6289 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.
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