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| 500mg |
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Butylscopolamine bromide is a potent antimuscarinic quaternary ammonium analogue acting as a competitive antagonist of mAChR (IC50: 55.3 ± 4.3 nM). Scopolamine inhibits parasympathetic-cholinergic system.
| Targets |
Muscarinic acetylcholine receptors
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|---|---|
| ln Vitro |
Action mechanism：It is a quaternary ammonium antimuscarinic drug. In addition to having a spasmolytic effect on smooth muscles, it can also block ganglia and neuromuscular junctions, but it has a weak effect on the central nervous system [2]
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| ln Vivo |
- Effect on colonoscopy polyp detection：Hyoscine butylbromide was used in colonoscopy. Meta - analysis of 5 RCTs involving 1998 patients showed that it did not significantly improve the polyp detection rate, with an odds ratio (OR) of 1.09 (95% CI: 0.91 - 1.31, p = 0.33). In 4 RCTs with 1882 patients, it also did not significantly improve the adenoma detection rate, with an OR of 1.13 (95% CI: 0.92 - 1.38, p = 0.24). Its possible mechanism is to inhibit smooth muscle activity, flatten colon folds, and theoretically improve mucosal visualization, but the actual effect on detection rate is not significant [2]
- Treatment of acute ureteral colic：It can be used for the treatment of acute ureteral colic, but the literature does not elaborate on the specific effect and action mechanism [3] |
| Toxicity/Toxicokinetics |
6852391 Rats Oral LD50 1040 mg/kg Archives Internationales de Pharmacodynamie et de Therapie., 180(155), 1969 [PMID:5357002]
6852391 Rats Subcutaneous LD50 450 mg/kg Arzneimittel-Forschung. Drug Research., 4(341), 1954 [PMID:13172124] 6852391 Rats Intravenous LD50 24 mg/kg Sensory organs and special senses: Pupil dilation: eye; Autonomic nervous system: smooth muscle relaxant (mechanism unclear, antispasmodic) Oyo Yakuri. Pharmacometrics, 23(461), 1982 6852391 Rats Duodenal LD50 180 mg/kg International Archives of Pharmacodynamics and Therapeutics, 180(155), 1969 [PMID:5357002] 6852391 Oral LD50 in mice 1170 mg/kg Behavioral: Seizures or Effects on Seizure Threshold Therapeutics, 14(1096), 1959 [PMID:14435525] |
| References |
[1]. Effect of hyoscine N-butylbromide on adenoma detection rate: meta-analysis of randomized clinical trials. Dig Endosc. 2015 Mar;27(3):354-60.
[2]. Does hyoscine butylbromide really improve polyp detection during colonoscopy? A meta-analysis of randomized controlled trials. World J Gastroenterol. 2014 Jun 14;20(22):7034-9. [3]. Hyoscine N-butylbromide (Buscopan®) in the treatment of acute ureteral colic: what is the evidence? Urol Int. 2014;92(3):253-7. |
| Additional Infomation |
Indications: Can be used to relieve visceral colic. Can also be used in colonoscopy, CT colonography and barium enema to reduce colonic peristalsis and facilitate mucosal exploration [2][3]. Butylscopolamine bromide is an organic bromide salt of butylscopolamine. It is an antispasmodic that relieves gastric spasms (including spasms associated with irritable bowel syndrome), bladder spasms and dysmenorrhea. It has the effects of a muscarinic receptor antagonist and an antispasmodic. It is an organic bromide salt and a quaternary ammonium salt. It contains butylscopolamine.
An antimuscarinic quaternary ammonium derivative of scopolamine is used to treat spasms of the gastrointestinal tract, urinary tract, uterus and biliary tract and helps with radiographic imaging of the gastrointestinal tract. See also: Butylscopolamine bromide (note moved to); N-butylscopolamine bromide (note moved to). |
| Molecular Formula |
C21H30BRNO4
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|---|---|
| Molecular Weight |
440.37
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| Exact Mass |
439.135
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| Elemental Analysis |
C, 57.28; H, 6.87; Br, 18.14; N, 3.18; O, 14.53
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| CAS # |
149-64-4
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| Related CAS # |
Scopolamine;51-34-3;Scopolamine hydrobromide;114-49-8;Scopolamine hydrochloride;55-16-3
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| PubChem CID |
6852391
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| Appearance |
White to off-white solid powder
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| Melting Point |
142-1440C
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
|
| Heavy Atom Count |
27
|
| Complexity |
500
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
CCCC[N+]1([C@@H]2CC(C[C@H]1[C@H]3[C@@H]2O3)OC(=O)[C@H](CO)C4=CC=CC=C4)C.[Br-]
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| InChi Key |
HOZOZZFCZRXYEK-HNHWXVNLSA-M
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| InChi Code |
InChI=1S/C21H30NO4.BrH/c1-3-4-10-22(2)17-11-15(12-18(22)20-19(17)26-20)25-21(24)16(13-23)14-8-6-5-7-9-14;/h5-9,15-20,23H,3-4,10-13H2,1-2H3;1H/q+1;/p-1/t15?,16-,17-,18+,19-,20+,22?;/m1./s1
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| Chemical Name |
[(1S,2S,4R,5R)-9-butyl-9-methyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-7-yl] (2S)-3-hydroxy-2-phenylpropanoate;bromide
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| Synonyms |
Hyoscine butobromide; N-Butylscopolammonium bromide; Buscopan Injectable Solution; scopolamine butylbromide; 149-64-4; Hyoscine butylbromide; EINECS 205-744-1; Butylscopolamine bromide
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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) |
DMSO : ≥ 90 mg/mL (~204.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.11 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 22.5 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: ≥ 2.25 mg/mL (5.11 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 22.5 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: ≥ 2.25 mg/mL (5.11 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 | 2.2708 mL | 11.3541 mL | 22.7082 mL | |
| 5 mM | 0.4542 mL | 2.2708 mL | 4.5416 mL | |
| 10 mM | 0.2271 mL | 1.1354 mL | 2.2708 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.
Reclassifying Constipation Using Imaging and Manometry
CTID: NCT03226145
Phase: N/A Status: Unknown status
Date: 2020-07-07
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