Prubenzin (10 μM-1 mM) 降低膀胱平滑肌对乙酰胆碱的反应性 [1]。

口服预苯苯肼（10-300 mg/kg）可降低因束缚应激导致肠道功能障碍的大鼠的腹泻频率和粪便颗粒量[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

64.79

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

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。