In all measurements, dicyclomine hydrochloride (ip; 8 mg/kg; daily) increased cognitive impairment. Additionally, compared to the dicyclomine hydrochloride-treated NonTg model, the memory impairment in the 3xTg-AD model was more severe. Mice were given dicyclomine hydrochloride (ip; 2.0, 4.0, and 8.0 mg/kg; 7 days). a notable influence on the model association learning (PAL) task's performance. Small results from systemic treatment at lower doses

Animal/Disease Models: C57Bl/6 mice [1]
Doses: 2.0, 4.0, 8.0 mg/kg
Route of Administration: intraperitoneal (ip) injection; behavioral impairment of mice in spatial tasks [3]. Daily; 7-day
Experimental Results: Damage due to factors outside the hippocampus.

Absorption, Distribution and Excretion
The bioavailability of dicyclohexylamine has not been determined, but it is likely well absorbed due to its primary route of excretion being urine. The time to peak concentration (Tmax) of dicyclohexylamine is 1–1.5 hours. 79.5% of dicyclohexylamine is excreted in urine and 8.4% in feces. The volume of distribution for a 20 mg oral dose is 3.65 L/kg. Data on the clearance of dicyclohexylamine are not yet available. Metabolism/Metabolites Metabolism studies of dicyclohexylamine are insufficient. Biological Half-Life The mean plasma elimination half-life is approximately 1.8 hours.

Hepatotoxicity
As with other anticholinergic drugs, dicyclohexylamine has not been found to be associated with elevated liver enzymes or clinically significant liver injury. The metabolic pathway of dicyclohexylamine is not well understood, but it is likely metabolized in the liver. For references on the safety and potential hepatotoxicity of anticholinergic drugs, please see the "Overview of Anticholinergic Drugs" section. Drug Category: Anticholinergic Drugs

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Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Studies on the use of dicyclohexylamine during lactation are insufficient. However, there has been a report of a nursing infant experiencing apnea, with a response similar to that of an infant who received the drug directly. Dicyclohexylamine should not be used by breastfeeding women. ◉ Effects on Nursing Infants As of the revision date, no relevant published information was found. The manufacturer reported a case of apnea in a breastfed infant while the mother was receiving dicyclohexylamine treatment. Dicyclohexylamine may have been the cause of this reaction.
◉ Effects on Lactation and Breast Milk
As of the revision date, no published information was found regarding lactating women. Anticholinergic drugs can inhibit lactation in animals, possibly by suppressing the secretion of growth hormone and oxytocin. Anticholinergic drugs can also lower serum prolactin levels in non-lactating women. Prolactin levels in established lactating mothers may not affect their ability to breastfeed.

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Protein Binding
There are currently no data on the plasma protein binding of dicyclohexylamine.

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Interactions
...Anticholinergic drugs, such as...dicyclohexylamine...are expected to interact with digoxin...

[1]. Pharmacological Characterization and Distribution of Muscarinic Receptors in Human Placental Syncytiotrophoblast Brush-Border and Basal Plasma Membranes. Eur J Pharmacol. 1997 Feb 12;320(2-3):209-14.

[2]. M1 Receptors Play a Central Role in Modulating AD-like Pathology in Transgenic Mice. 2006 Mar 2;49(5):671-82.doi: 10.1016/j.neuron.2006.01.020.

[3]. A Computer-Automated Touchscreen Paired-Associates Learning (PAL) Task for Mice: Impairments Following Administration of Scopolamine or Dicyclomine and Improvements Following Donepezil.Psychopharmacology (Berl). 2011 Mar;214(2):537-48.

Bicyclohexylamine is an ester formed by the condensation of 1-cyclohexylcyclohexanecarboxylic acid and 2-(diethylamino)ethanol. It is an anticholinergic drug, and its hydrochloride salt is used to treat or prevent gastrointestinal muscle spasms, particularly those associated with irritable bowel syndrome (IBS). It acts as a muscarinic receptor antagonist, antispasmodic, and parasympathetic blocker. It is a tertiary amine and carboxylic acid ester. Its function is related to 2-diethylaminoethanol and 1,1'-bis(cyclohexyl)-1-carboxylic acid. Bicyclohexylamine is a muscarinic M1, M3, and M2 receptor antagonist and a non-competitive inhibitor of histamine and bradykinin, used to treat functional bowel disorders and intestinal spasms caused by IBS. Although dicyclohexylamine is still widely used, its recommendations are likely based on limited evidence, and therefore its prescription rate is declining. Dicyclohexylamine was approved by the U.S. Food and Drug Administration (FDA) on May 11, 1950. Dicyclohexylamine is an anticholinergic drug. Its mechanism of action is as a cholinergic antagonist. Dicyclohexylamine is an anticholinergic drug used to treat gastrointestinal disorders such as acidosis and irritable bowel syndrome. Dicyclohexylamine does not cause elevated liver enzymes or clinically significant acute liver injury. Dicyclohexylamine is a carboxylic acid derivative and a selective anticholinergic drug with antispasmodic effects. Dicyclohexylamine blocks the binding of acetylcholine to muscarinic receptors on smooth muscle. This drug has a direct relaxant effect on smooth muscle, thus preventing gastrointestinal muscle spasms, inhibiting gastrointestinal propulsion, reducing gastric acid secretion, and controlling excessive secretions from the pharynx, trachea, and bronchi. It is a muscarinic receptor antagonist and can be used as an antispasmodic and to treat urinary incontinence. It has minimal effects on glandular secretion or the cardiovascular system. It has some local anesthetic effects and is used to treat spasms of the gastrointestinal tract, biliary tract, and urinary tract. See also: Dicyclohexylamine hydrochloride (salt form). Drug Indications Bicyclic amine is indicated for the treatment of functional bowel disorders and irritable bowel syndrome. FDA Label Mechanism of Action Bicyclic amine's mechanism of action is partly through direct inhibition of the antimuscarinic activity of M1, M3, and M2 receptors, and partly through antagonism of bradykinin and histamine. Bicyclic amine non-competitively inhibits the effects of bradykinin and histamine, thereby acting directly on smooth muscle and reducing the intensity of ileal spasms. Its primary effect appears to be a non-specific, direct relaxation of smooth muscle, rather than competitive antagonism of acetylcholine. Therapeutic Uses Muscarinic antagonist; parasympathetic blocker. Often classified as an "antispasmodic," it is not actually an antimuscarinic drug. ...Bicycloamine hydrochloride, VSP-DECR, relieves spasms of the gastrointestinal tract, biliary tract, ureter, and uterus without producing typical atropine-like effects on the salivary glands, sweat glands, gastric glands, eyes, and cardiovascular system.../HCL/
It reduces intestinal motility but does not inhibit gastric acid secretion. It is used to treat irritable bowel syndrome, spastic constipation, mucinous colitis, spastic colitis, pyloric spasm, and biliary motility disorders. In the treatment of peptic ulcers, it is used to delay gastric emptying. /Hydrochloride/
Anticholinergic/Hydrochloride/

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Drug Warnings
Bicycloamine should be used with caution in patients with benign prostatic hyperplasia, bladder neck obstruction, pyloric obstruction, and pyloric spasm. Although it does not appear to increase intraocular pressure in patients with narrow-angle glaucoma, monitoring of intraocular pressure in such patients is recommended.
The clinical use of phenytoin sodium (Bentyl) has been disappointing. A three-year-old boy suffered a tonic-clonic seizure after accidentally ingesting approximately 100 phenytoin sodium tablets, followed by cardiac arrest. Analysis revealed high levels of doxylamine, bicyclic amine, and pyridoxine. Doxylamine appears to be the toxic component.
Pharmacodynamics
Bicyclic amine is an anticholinergic drug used to relax intestinal smooth muscle. Because it is usually taken four times daily, 20-40 mg orally or 10-20 mg intramuscularly, its duration of action is not particularly long. Bicyclic amine should not be administered intravenously.

C19H35NO2.HCL

345.94764

345.243

67-92-5

Dicyclomine;77-19-0

3042

White to off-white solid powder

399.8ºC at 760 mmHg

164-166ºC

116.5ºC

5.204

0

3

8

22

326

0

CURUTKGFNZGFSE-UHFFFAOYSA-N

InChI=1S/C19H35NO2/c1-3-20(4-2)15-16-22-18(21)19(13-9-6-10-14-19)17-11-7-5-8-12-17/h17H,3-16H2,1-2H3

2-(diethylamino)ethyl 1-cyclohexylcyclohexane-1-carboxylate

2934.99.9001

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.

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

H2O : ~50 mg/mL (~144.53 mM)
DMSO : ~33.33 mg/mL (~96.34 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.23 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.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (7.23 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (7.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.

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Solubility in Formulation 4: 50 mg/mL (144.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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