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, 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/

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

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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.

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Interactions
GI ABSORPTION OF PROPANTHELINE IS INCR BY SODIUM BICARBONATE...
RATE & EXTENT OF ABSORPTION OF.../ORALLY/ DOSED PARACETAMOL IS REDUCED BY...PROPANTHELINE...
CONCURRENT USE OF PROPANTHELINE WITH SLOW-DISSOLVING TABLETS OF DIGOXIN MAY CAUSE INCR SERUM DIGOXIN LEVELS. THIS INTERACTION CAN BE AVOIDED BY USING ONLY THOSE DIGOXIN TABLETS THAT ARE FAST DISSOLVING BY USP STD.
.../TREATMENT WITH/ PROPANTHELINE, INCR /GI/ ABSORPTION /OF PHENOLSULFOPHTHALEIN IN MAN/ UP TO 24% OWING TO DECR GI TRANSIT RATE.
For more Interactions (Complete) data for PROPANTHELINE (14 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 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).

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

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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/

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Therapeutic Uses
Anti-Ulcer Agents; Muscarinic Antagonists; Parasympatholytics
ANTICHOLINERGIC AGENTS (EG ... PROPANTHELINE) ... /IS USED FOR/ ANTISPASMODIC EFFECTS TO TREAT HYPERTONICITY & UNCONTROLLED CONTRACTION OF URINARY BLADDER & TO REDUCE SYMPTOMS OF DYSURIA & URINARY URGENCY & FREQUENCY ASSOC WITH ... NEUROGENIC BLADDER, CYSTITIS, PROSTATITIS, OR URETHRITIS.
BENEFICIAL EFFECTS IN PEPTIC ULCER MOSTLY DERIVED FROM DECR GASTRIC MOTILITY, ALTHOUGH SOME SUPPRESSION OF GASTRIC SECRETION OCCURS AFTER PARENTERAL ADMIN. /PROPANTHELINE BROMIDE/
MEDICATION (VET): /USE AS/ GI SEDATIVE... /BROMIDE/
For more Therapeutic Uses (Complete) data for PROPANTHELINE (9 total), please visit the HSDB record page.

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Drug Warnings
...PRACTITIONER SHOULD BE ALERT FOR SIGNS OF DIGITALIS TOXICITY IN ANY PT RECEIVING DIGOXIN TABLETS & PROPANTHELINE CONCURRENTLY. ... OTHER DRUGS RELATED TO DIGOXIN INCL ACETYLDIGITOXIN DESLANOSIDE, DIGITALIS, GITALIN, LANATOSIDE C & OUABAIN.
There are no clinically significant, clear-cut differences in efficacy among the anticholinergic antispasmodics to aid in drug selection, and, ... no available anticholinergic drug has a particular advantage over others. /Anticholinergic drugs/
In 1 series of patients oral doses of 75 mg/day caused subjective difficulty with vision in only 4/69, presumably from interference with accomodation. In another series 120 mg given orally to 16 normal people 20-35 yr of age had no effect on near point of accomodation. /Propantheline bromide/
...During test period /in tests relating to glaucoma, tension/ rose in 3 chronic simple openangle glaucomatous eyes, in 1 with "chronic congestive", & in 1 with "secondary" glaucoma. Without /adequate/ information ... it is uncertain whether drug was responsible for these tension elevations.
For more Drug Warnings (Complete) data for PROPANTHELINE (9 total), please visit the HSDB record page.

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Pharmacodynamics
Propantheline is an anticholinergic drug, a medication that reduces the effect of acetylcholine, a chemical released from nerves that stimulates muscles, by blocking the receptors for acetylcholine on smooth muscle (a type of muscle). It also has a direct relaxing effect on smooth muscle. Propantheline is used to treat or prevent spasm in the muscles of the gastrointestinal tract in the irritable bowel syndrome. In addition, Propantheline inhibits gastrointestinal propulsive motility and decreases gastric acid secretion and controls excessive pharyngeal, tracheal and bronchial secretions.

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.)