| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| Other Sizes |
|
| ln Vitro |
The reactivity of bladder smooth muscle to cervical choline is lowered by brachpropantheline (10 μM–1 mM) [1].
|
|---|---|
| ln Vivo |
In patients with restrictive intestinal dysfunction, propantheline bromide (powder formulation, 10-300 mg/kg) lowers the incidence of diarrhea and the count of matrix particles [3].
|
| Animal Protocol |
Animal/Disease Models: Rat restraint stress intestinal dysfunction model [3]
Doses: 10-300 mg/kg Route of Administration: Oral Experimental Results:diminished fecal particle count, ED50 value is 41 mg/kg. The incidence of diarrhea was dose-dependently diminished, with an ED50 value of 64 mg/kg. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Approximately 70% of the dose is excreted in the urine, mostly as metabolites. AFTER 95 HR HUMANS EXCRETED IN URINE 5% OF DOSE (0.03 G) OF PROPANTHELINE BROMIDE GIVEN ORALLY. /PROPANTHELINE BROMIDE, FROM TABLE/ The quarternary ammonium derivatives of the belladonna alkaloids are poorly absorbed after an oral dose; nevertheless, some of these compounds applied locally to the eye can cause mydriasis and cycloplegia. /Quarternary ammonium derivatives of belladonna alkaloids/ |
| Toxicity/Toxicokinetics |
Hepatotoxicity
Like other anticholinergic agents, propantheline has not been linked to episodes of liver enzyme elevations or clinically apparent liver injury. It is metabolized at least partially in the liver. A reason for its safety may relate to the low daily dose. References on the safety and potential hepatotoxicity of anticholinergics are given together after the Overview section on Anticholinergic Agents. Drug Class: Anticholinergic Agents Effects During Pregnancy and Lactation ◉ Summary of Use during Lactation No information is available on the use of propantheline during breastfeeding. Because propantheline is a quaternary ammonium compound, it is not likely to be absorbed and reach the bloodstream of the infant. Long-term use of propantheline might reduce milk production or milk letdown. During long-term use, observe for signs of decreased lactation (e.g., insatiety, poor weight gain). ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Anticholinergics can inhibit lactation in animals, apparently by inhibiting growth hormone and oxytocin secretion. Anticholinergic drugs can also reduce serum prolactin in nonnursing women. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. |
| References | |
| Additional Infomation |
Propantheline is a member of xanthenes.
A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking. Propantheline is an Anticholinergic. The mechanism of action of propantheline is as a Cholinergic Antagonist. Propantheline is an anticholinergic agent used to treat gastrointestinal conditions associated with intestinal spasm and to decrease secretions during anesthesia. Propantheline has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury. A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking. See also: Propantheline Bromide (has salt form). Drug Indication For the treatment of enuresis. It has also been used for hyperhidrosis, and cramps or spasms of the stomach, intestines or bladder. Mechanism of Action Action is achieved via a dual mechanism: (1) a specific anticholinergic effect (antimuscarinic) at the acetylcholine-receptor sites and (2) a direct effect upon smooth muscle (musculotropic). ANTICHOLINERGIC DRUGS BLOCK THE ACTION OF ACETYLCHOLINE AT POSTGANGLIONIC CHOLINERGIC SITES, THEREBY INCREASING BLADDER CAPACITY BY REDUCING THE NUMBER OF MOTOR IMPULSES REACHING THE DETRUSOR MUSCLE. /ANTICHOLINERGIC DRUGS/ |
| Molecular Formula |
C23H30BRNO3
|
|---|---|
| Molecular Weight |
448.39
|
| Exact Mass |
447.14
|
| CAS # |
50-34-0
|
| Related CAS # |
Propantheline-d3 bromide;64717-35-7;Propantheline;298-50-0
|
| PubChem CID |
4934
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
159-161°C
|
| LogP |
1.734
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
27
|
| Complexity |
474
|
| Defined Atom Stereocenter Count |
0
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~223.02 mM)
H2O : ~50 mg/mL (~111.51 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.58 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 25.0 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: ≥ 2.5 mg/mL (5.58 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 25.0 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: ≥ 2.5 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 130 mg/mL (289.93 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2302 mL | 11.1510 mL | 22.3020 mL | |
| 5 mM | 0.4460 mL | 2.2302 mL | 4.4604 mL | |
| 10 mM | 0.2230 mL | 1.1151 mL | 2.2302 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
