Prubenzin (10 μM-1 mM) decreases the smooth muscle in the bladder's reactivity to acetylcholine [1].

Oral prebenebenzine (10–300 mg/kg) decreases the frequency of diarrhea and the amount of fecal pellets in rats suffering from intestinal dysfunction brought on by restraint stress [3].

Animal/Disease Models: Rat intestinal dysfunction model induced by restraint stress [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.

Absorption, Distribution and Excretion
Approximately 70% of the dose is excreted in the urine, primarily as metabolites. 95 hours after oral administration of propylthiocyanate bromide, 5% (0.03 g) is excreted in the urine. /propylthiocyanate bromide, from table/ Quaternary ammonium derivatives of belladonna alkaloids are poorly absorbed orally; however, when applied topically to the eyes, some compounds can cause mydriasis and ciliary muscle paralysis. /Quaternary ammonium derivatives of belladonna alkaloids/

Hepatotoxicity
As with other anticholinergic drugs, propylthioline has not been found to be associated with elevated liver enzymes or clinically significant liver injury. It is at least partially metabolized in the liver. Its safety may be related to its low daily dose. References on the safety and potential hepatotoxicity of anticholinergic drugs are listed after the "Overview of Anticholinergic Drugs" section. Drug Category: Anticholinergic Drugs

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Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation There is currently no information regarding the use of propylthioline during lactation. Because propylthioline is a quaternary ammonium compound, it is unlikely to be absorbed by the infant and enter the bloodstream. Long-term use of propylthioline may reduce milk production or inhibit the milk ejection reflex. With long-term use, signs of reduced milk production (e.g., dissatisfaction, poor weight gain) should be observed. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found.
◉ Effects on Lactation and Breast Milk
Anticholinergic drugs can inhibit lactation in animals, possibly by suppressing the secretion of growth hormone and oxytocin. Anticholinergic drugs can also reduce serum prolactin levels in non-lactating women. For mothers who have established lactation, prolactin levels may not affect their ability to breastfeed.

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Drug Interactions
Sodium bicarbonate can increase the gastrointestinal absorption of propylthiophene…
Propylthiophene can reduce the rate and extent of absorption of oral acetaminophen…
Concomitant use of propylthiophene and sustained-release digoxin tablets may lead to elevated serum digoxin levels. This interaction can be avoided by using only fast-dissolving digoxin tablets conforming to the United States Pharmacopeia.
…/Use/propylthiophene treatment can increase/the/gastrointestinal/absorption/of/phenolsulfonphthalein/by up to 24% due to reduced gastrointestinal transit rate.
For more (complete) interaction data on propylthiophene (14 in total), please visit the HSDB record page.

[1]. J Mokry, et al. Propantheline and in vitro reactivity of urinary bladder smooth muscle in guinea pigs. Bratisl Lek Listy. 2005;106(4-5):151-4.
[2]. Richard Jewell, et al. Propantheline. xPharm: The Comprehensive Pharmacology Reference. 2007, Pages 1-5.
[3]. S Kobayashi, et al. Effects of YM905, a novel muscarinic M3-receptor antagonist, on experimental models of bowel dysfunction in vivo. Jpn J Pharmacol. 2001 Jul;86(3):281-8.

Propantheline belongs to the xaxidine class of drugs. It is a muscarinic receptor antagonist used as an antispasmodic to treat rhinitis, urinary incontinence, and ulcers. At high doses, it has nicotine-like effects, leading to neuromuscular blockade. Propantheline is an anticholinergic drug. Its mechanism of action is as a cholinergic antagonist. Propantheline is an anticholinergic drug used to treat gastrointestinal disorders associated with intestinal spasms and to reduce secretions during anesthesia. Propantheline has not been shown to cause elevated liver enzymes or clinically significant acute liver injury. It is a muscarinic receptor antagonist used as an antispasmodic to treat rhinitis, urinary incontinence, and ulcers. At high doses, it has nicotine-like effects, leading to neuromuscular blockade. See also: Propantheline bromide (salt form).

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Drug Indications
For the treatment of enuresis.
It has also been used to treat hyperhidrosis and spasms or cramps of the stomach, intestines or bladder.

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Mechanism of Action
Its mechanism of action is a dual mechanism: (1) it exerts a specific anticholinergic effect at the acetylcholine receptor site (antimuscarinic effect); (2) it has a direct effect on smooth muscle (muscotropic effect).
Anticholinergic drugs block the action of acetylcholine at postganglionic cholinergic sites, thereby reducing the number of motor impulses reaching the detrusor muscle and increasing bladder capacity. /Anticholinergic Drugs/

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Therapeutic Uses
Antiulous drugs; muscarinic receptor antagonists; parasympathetic nerve blockers
Anticholinergic drugs (e.g., propylthiophene)...are used to treat bladder hypertonia and uncontrolled contractions, and to relieve symptoms of dysuria, urgency and frequency associated with neurogenic bladder, cystitis, prostatitis or urethritis.
The benefit for peptic ulcers mainly comes from reduced gastric motility, although gastric secretion inhibition also occurs after parenteral administration. /Propamiline bromide/
Drug (Veterinary):/Used as/a gastrointestinal sedative... /Bromide/
For more complete data on the therapeutic uses of propamiline (9 types), please visit the HSDB record page.

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Drug Warnings
...Physicians should be alert to signs of digitalis toxicity in patients taking digoxin tablets and propamiline concurrently. ……Other drugs associated with digoxin include acetyldigoxin, dilanoside, digitalis, gentamicin, lananoside C, and ouabain.
Currently, there are no clinically significant, clear differences in the efficacy of anticholinergic antispasmodics for drug selection, and...currently, no single anticholinergic drug has a particular advantage over other drugs. /Anticholinergic Drugs/
In a patient series study, a daily oral dose of 75 mg of anticholinergic drugs resulted in subjective visual disturbances in only 4 out of 69 patients, presumably due to interference with accommodation. In another study, oral administration of 120 mg of an anticholinergic drug to 16 healthy subjects aged 20–35 years showed no effect on near-point accommodation. Propantheline bromide…During trials, intraocular pressure increased in 3 patients with chronic simple open-angle glaucoma, 1 patient with chronic congestive glaucoma, and 1 patient with secondary glaucoma in glaucoma-related trials. Due to insufficient information, it is uncertain whether these increases in intraocular pressure were caused by the drug. For more complete data on drug warnings for Propantheline (9 of 9), please visit the HSDB record page. Pharmacodynamics: Propantheline is an anticholinergic drug that reduces the effect of acetylcholine (a neurotransmitter that stimulates muscles) by blocking acetylcholine receptors on smooth muscle. It also has a direct relaxant effect on smooth muscle. Propantheline is used to treat or prevent gastrointestinal muscle spasms caused by irritable bowel syndrome. In addition, propylthiophene can inhibit gastrointestinal motility, reduce gastric acid secretion, and control excessive secretion in the pharynx, trachea, and bronchi.

C23H30NO3+.BR-

448.3932

294.194

298-50-0

Propantheline bromide;50-34-0

4934

Typically exists as solid at room temperature

3.137

0

3

7

27

474

0

CC(C)[N+](C)(CCOC(=O)C1C2=CC=CC=C2OC3=CC=CC=C31)C(C)C

VVWYOYDLCMFIEM-UHFFFAOYSA-N

InChI=1S/C23H30NO3/c1-16(2)24(5,17(3)4)14-15-26-23(25)22-18-10-6-8-12-20(18)27-21-13-9-7-11-19(21)22/h6-13,16-17,22H,14-15H2,1-5H3/q+1

methyl-di(propan-2-yl)-[2-(9H-xanthene-9-carbonyloxy)ethyl]azanium

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)