| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
M1 muscarinic acetylcholine receptor (M1 AChR). Benzhexol HCl is a potent and selective M1 muscarinic receptor antagonist. It partially blocks cholinergic activity in the central nervous system, which is responsible for the symptoms of Parkinson's disease. The compound is also thought to increase the availability of dopamine, a brain chemical critical in the initiation and smooth control of voluntary muscle movement.
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| ln Vitro |
Benzhexol HCl demonstrates anticholinergic activity in vitro with selectivity for M1 muscarinic receptors. The compound binds to M1 receptors and antagonizes acetylcholine-mediated signaling. Its potency and selectivity have been characterized in various receptor binding and functional assays using cell lines expressing different muscarinic receptor subtypes. The compound shows selectivity for M1 receptors over other muscarinic receptor subtypes.
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| ln Vivo |
In vivo, Benzhexol HCl is used clinically for the treatment of Parkinson syndrome, dystonia, and drug-induced extrapyramidal symptoms. It is administered orally and acts centrally to reduce cholinergic overactivity in the striatum, helping to restore the balance between dopamine and acetylcholine. The compound improves motor symptoms such as tremor, rigidity, and bradykinesia in Parkinson's disease patients.
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| Enzyme Assay |
In vitro receptor binding assays for Benzhexol HCl involve competition binding experiments using radiolabeled ligands such as [3H]-N-methylscopolamine or [3H]-QNB. Membranes are prepared from cells expressing the M1 muscarinic receptor or from brain tissue. Benzhexol HCl is incubated at varying concentrations, and bound radioactivity is measured. Ki values are calculated from displacement curves. Functional assays measure inhibition of acetylcholine-induced calcium mobilization or phosphoinositide turnover.
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| Cell Assay |
Cellular assays for Benzhexol HCl involve culturing cells expressing the M1 muscarinic receptor. Cells are treated with Benzhexol HCl at varying concentrations (typically 0.1-100 µM) and stimulated with acetylcholine or a muscarinic agonist. Calcium mobilization is measured using fluorescent indicators. Phosphoinositide turnover is measured by assessing IP3 accumulation. The compound's antagonist activity is assessed by its ability to block agonist-induced responses.
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| Animal Protocol |
In vivo animal studies for Benzhexol HCl are conducted in rodent models of Parkinson's disease or drug-induced catalepsy. The compound is typically administered orally or intraperitoneally. Motor function is assessed using behavioral tests such as the rotarod test, open field test, or catalepsy test. Dosing regimens vary, with typical doses ranging from 1-20 mg/kg depending on the species and study objectives.
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| ADME/Pharmacokinetics |
Benzhexol HCl is administered orally and is well absorbed from the gastrointestinal tract. It is metabolized in the liver and excreted via the renal route. The compound is soluble in DMSO at 8 mg/mL and in water at 4 mg/mL. It has a molecular weight of 337.93 g/mol and a molecular formula of C20H31NO·HCl. Its elimination half-life is approximately 5-10 hours in humans.
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| Toxicity/Toxicokinetics |
Benzhexol HCl is generally well-tolerated at therapeutic doses but can cause side effects typical of anticholinergic agents, including dry mouth, blurred vision, constipation, urinary retention, and cognitive impairment. It is contraindicated in patients with glaucoma, obstructive uropathy, or gastrointestinal obstruction. The compound should be used with caution in elderly patients. It is an FDA-approved medication for Parkinson's disease.
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| References |
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| Additional Infomation |
Trihexyphenidyl hydrochloride is an aralkylamine. Trihexyphenidyl hydrochloride is the hydrochloride salt form of trihexyphenidyl, a synthetic substituted piperidine drug with parasympathetic blocking activity, primarily used to treat Parkinson's disease. Trihexyphenidyl hydrochloride antagonizes the activity of acetylcholine through muscarinic receptors. This balances cholinergic and dopaminergic activity in the basal ganglia, thereby improving typical symptoms of Parkinson's disease, such as rigidity and tremor. Furthermore, Trihexyphenidyl hydrochloride has a direct antispasmodic effect on smooth muscle. It is a centrally acting muscarinic receptor antagonist used to treat Parkinson's disease and drug-induced extrapyramidal motor disorders, and can also be used as an antispasmodic. See also: Trihexyphenidyl (containing the active ingredient).
Benzhexol HCl (Trihexyphenidyl hydrochloride) is a potent and selective M1 muscarinic receptor antagonist used as an antiparkinsonian agent. It is used for the treatment of Parkinson syndrome, dystonia, and drug-induced extrapyramidal symptoms. The compound is an FDA-approved medication and is available as a prescription drug. It is also known by the brand name Artane. |
| Molecular Formula |
C20H32CLNO
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|---|---|
| Molecular Weight |
337.932
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| Exact Mass |
337.217
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| CAS # |
52-49-3
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| Related CAS # |
Trihexyphenidyl;144-11-6
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| PubChem CID |
66007
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| Appearance |
White to off-white solid powder
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| Boiling Point |
447.9ºC at 760mmHg
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| Melting Point |
258.5ºC
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| Flash Point |
211ºC
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| LogP |
5.07
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
314
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QDWJJTJNXAKQKD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H31NO.ClH/c22-20(18-10-4-1-5-11-18,19-12-6-2-7-13-19)14-17-21-15-8-3-9-16-21/h1,4-5,10-11,19,22H,2-3,6-9,12-17H21H
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| Chemical Name |
1-cyclohexyl-1-phenyl-3-piperidin-1-ylpropan-1-ol hydrochloride
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| Synonyms |
TrihexyphenidylBenzhexol ArtaneTrihexPacitane Benzhexol HClApo-TrihexParkin
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~29.59 mM)
H2O : ~5 mg/mL (~14.80 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (2.96 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (2.96 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 10.0 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: ≥ 1 mg/mL (2.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9592 mL | 14.7960 mL | 29.5919 mL | |
| 5 mM | 0.5918 mL | 2.9592 mL | 5.9184 mL | |
| 10 mM | 0.2959 mL | 1.4796 mL | 2.9592 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03430596 | Completed | Drug: Pramipexole Drug: Trihexyphenidyl hydrochloride |
Extrapyramidal Syndrome | Shanghai Mental Health Center | May 1, 2018 | Early Phase 1 |
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