| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Biperiden acts as a competitive antagonist at muscarinic acetylcholine receptors in the central nervous system, particularly in the striatum. By blocking the action of acetylcholine at these receptors, it helps to restore the balance between dopaminergic and cholinergic activity in the basal ganglia. This reduces the symptoms of Parkinson's disease and drug-induced movement disorders.
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| ln Vitro |
Biperiden hydrochloride (29.6 μg/ml, 72 hours) can dramatically suppress proliferation and cause apoptosis in human pancreatic ductal adenocarcinoma cells when applied at high concentrations[1].
In vitro, biperiden binds to muscarinic receptors with high affinity, displacing radiolabeled antagonists like [³H]-quinuclidinyl benzilate (QNB) from receptor sites in brain membrane preparations. Its antagonistic activity can be measured by its ability to block acetylcholine-induced responses in isolated tissues or cells expressing muscarinic receptors. |
| ln Vivo |
Biperiden hydrochloride (intraperitoneal injection, 10 mg/kg, everyday, 3 weeks) reduces tumor size by 83% in subcutaneous xenograft mice using Panc-1 human pancreatic ductal adenocarcinoma cells[1].
Biperiden hydrochloride (intraperitoneal injection, 8 mg/kg, every 8 hours, 10 days) can lower extracellular hippocampal glutamate levels and the frequency of spontaneous seizures while permanently lowering hippocampal excitability[2]. In vivo, biperiden is used to treat the symptoms of Parkinson's disease, including tremor, rigidity, and bradykinesia. It is also used to treat extrapyramidal symptoms induced by antipsychotic drugs. It is effective in reducing tremor and rigidity but has less effect on bradykinesia. It is available in oral and injectable forms. |
| Enzyme Assay |
The in vitro receptor binding assay for biperiden involves measuring its affinity for muscarinic acetylcholine receptors. This is typically done using a radioligand binding assay with [³H]-QNB and homogenates from rat brain (which are rich in muscarinic receptors). Competition binding experiments are performed to determine the Ki value of biperiden at the muscarinic receptor.
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| Cell Assay |
Cell Line: Panc-1, Panc-2 and BxPC3 human pancreatic ductal adenocarcinoma cells
Concentration: 29.6 μg/mL Incubation Time: 72 hours Result: Inhibited cell proliferation at 72 hours significantly by reducing nuclear c-Rel translocation. In vitro cellular assays for biperiden are performed on cells expressing muscarinic receptors. The functional antagonism of biperiden is measured by its ability to block acetylcholine-induced calcium mobilization or the activation of downstream signaling pathways. The IC50 for inhibiting the acetylcholine response is determined to quantify its antagonist potency. |
| Animal Protocol |
Subcutaneous xenograft mouse using Panc-1 human pancreatic ductal adenocarcinoma cells[1]
10 mg/kg Intraperitoneal injection; everyday; 3 weeks In vivo animal experiments for biperiden were conducted in animal models of Parkinson's disease. The reserpine-induced catalepsy model in rats or the MPTP-induced parkinsonism model in mice and primates were used to evaluate its efficacy. The reversal of catalepsy or improvement in motor function was measured to assess its antiparkinsonian effect. |
| ADME/Pharmacokinetics |
Biperiden is well-absorbed after oral administration, with peak plasma concentrations reached in 1-2 hours. It is extensively metabolized in the liver and excreted in the urine. Its half-life is approximately 18-24 hours, allowing for multiple daily dosing. It is distributed to the central nervous system and other tissues, consistent with its lipophilic nature.
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| Toxicity/Toxicokinetics |
Biperiden, like other anticholinergic drugs, has a range of potential side effects. Common side effects include dry mouth, blurred vision, constipation, urinary retention, tachycardia, and confusion. CNS effects can include drowsiness, dizziness, and memory impairment, particularly in elderly patients. It should be used with caution in patients with glaucoma or prostatic hypertrophy.
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| References |
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| Additional Infomation |
muscarinic receptor antagonist with effects on both the central and peripheral nervous systems. It has been used to treat atherosclerotic Parkinson's disease, idiopathic Parkinson's disease, and post-encephalitis Parkinson's disease. Additionally, it has been used to relieve extrapyramidal symptoms induced by phenothiazine derivatives and reserpine.
Biperiden hydrochloride is marketed under the brand name Akineton. It was introduced in the 1950s and remains a useful drug for the treatment of Parkinson's disease and drug-induced extrapyramidal symptoms. It is one of the classic anticholinergic drugs used in neurology and psychiatry. Its use has declined with the availability of newer dopaminergic drugs for Parkinson's disease, but it is still used as an adjunctive therapy. |
| Molecular Formula |
C21H30CLNO
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|---|---|
| Molecular Weight |
347.92
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| Exact Mass |
347.201
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| Elemental Analysis |
C, 72.49; H, 8.69; Cl, 10.19; N, 4.03; O, 4.60
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| CAS # |
1235-82-1
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| Related CAS # |
Biperiden; 514-65-8; Biperiden lactate; 7085-45-2; Biperiden-d5 hydrochloride; rel-Biperiden-d5; rel-Biperiden EP impurity A-d5; rel-Biperiden EP impurity B-d5
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| PubChem CID |
92151
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| Appearance |
White to off-white solid powder
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| Boiling Point |
462.1ºC at 760 mmHg
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| Melting Point |
101ºC
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| Flash Point |
224.5ºC
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| Vapour Pressure |
2.45E-09mmHg at 25°C
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| LogP |
4.702
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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 |
24
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| Complexity |
422
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(C1CC2C=CC1C2)(CCN3CCCCC3)C4=CC=CC=C4.[H]Cl
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| InChi Key |
RDNLAULGBSQZMP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H29NO.ClH/c23-21(19-7-3-1-4-8-19,11-14-22-12-5-2-6-13-22)20-16-17-9-10-18(20)15-17;/h1,3-4,7-10,17-18,20,23H,2,5-6,11-16H2;1H
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| Chemical Name |
1-(2-bicyclo[2.2.1]hept-5-enyl)-1-phenyl-3-piperidin-1-ylpropan-1-ol;hydrochloride
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| Synonyms |
Akineton hydrochloride; Akineton; Akinophyl; Biperiden Hydrochloride; Biperiden; Biperiden
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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: ~20 mg/mL (~57.5 mM)
H2O: ~5 mg/mL (~14.4 mM) |
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8742 mL | 14.3711 mL | 28.7422 mL | |
| 5 mM | 0.5748 mL | 2.8742 mL | 5.7484 mL | |
| 10 mM | 0.2874 mL | 1.4371 mL | 2.8742 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 |
| NCT04945213 | Recruiting | Drug: Biperiden Other: Placebo |
Post Traumatic Epilepsy Brain Injury Traumatic Severe |
Hospital Sirio-Libanes | January 10, 2023 | Phase 3 |
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