Biperiden
(Synonyms: 比哌立登; 碧卜利旦; KL 373) 目录号 : GC35524
Biperiden(KL 373)有抗帕金森症活性，是中枢M1胆碱受体阻断剂。
Cas No.:514-65-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.Target: M1 receptorsBiperiden is an antiparkinsonian agent of the anticholinergic type. It is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arteriosclerotic)[1]. Biperiden has an atropine-like blocking effect on all peripheral structures which are parasympathetic-innervate. It also has a prominent central blocking effect on M1 receptors [2].Biperiden (0.11 mg/kg), benactyzine (0.3 mg/kg),caramiphen (10 mg/kg), procyclidine (3 mg/kg), and trihexyphenidyl (0.12 mg/kg) separately and each in combination with physostigmine (0.1 mg/kg) is to make a comparative assessment of potential cognitive effects. The results showed that benactyzine, caramiphen, and trihexyphenidyl reduced rats' innate preference for novelty, whereas biperiden and procyclidine did not [3].Clinical indications: parkinsonismFDA Approved Date: Toxicity: Drowsiness; vertigo; headache; dizziness
[1]. Pehl C, et al. Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus. Aliment Pharmacol Ther. 1998 Oct;12(10) [2]. Kornhuber J, et al. Identification of novel functional inhibitors of acid sphingomyelinase. PLoS One. 2011;6(8) [3]. Myhrer T, et al. Antiparkinson drugs used as prophylactics for nerve agents: studies of cognitive side effects in rats. Pharmacol Biochem Behav. 2008 Jun;89(4):633-8.
| Cas No. | 514-65-8 | SDF | |
| 别名 | 比哌立登; 碧卜利旦; KL 373 | ||
| Canonical SMILES | OC([C@H]1C[C@@H]2C=C[C@H]1C2)(CCN3CCCCC3)C4=CC=CC=C4 | ||
| 分子式 | C21H29NO | 分子量 | 311.46 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2107 mL | 16.0534 mL | 32.1069 mL |
| 5 mM | 0.6421 mL | 3.2107 mL | 6.4214 mL |
| 10 mM | 0.3211 mL | 1.6053 mL | 3.2107 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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Biperiden Challenge Model in Healthy Elderly as Proof-of-Pharmacology Tool: A Randomized, Placebo-Controlled Trial
J Clin Pharmacol 2021 Nov;61(11):1466-1478.PMID:34021607DOI:10.1002/jcph.1913.
Selective M1 muscarinic acetylcholine receptor (mAChR) agonists are being developed as symptomatic treatment for neurodegenerative and neuropsychiatric disorders that lead to cognitive dysfunction. Demonstrating cognition-enhancing effects in early-phase clinical development in healthy subjects is difficult. A challenge with the M1 mAChR antagonist Biperiden could be used to demonstrate procognitive and pharmacological effects of selective M1 mAChR agonists. The aim of this study was to develop such a model. To this end, 12 healthy elderly subjects participated in a randomized, placebo-controlled, 3-way crossover study investigating tolerability, pharmacokinetic (PK) and pharmacodynamic (PD) effects of 2 and 4 mg Biperiden. Repeated PD assessments were performed using neurocognitive tasks and electrophysiological measurements. A population PK-PD model was developed. Four milligrams of Biperiden showed significant impairment of sustained attention (-2.1 percentage point in adaptive tracking [95%CI, -3.043 to -1.148], verbal memory (2-3 fewer words recalled [95%CI, -5.9 to -0.2]) and working memory (up to a 50-millisecond increase in the n-back task reaction time [95%CI, 21.854-77.882]) compared with placebo. The PK data were best fitted by a 2-compartment model and showed high interoccasion and intersubject variability. Population PK-PD analysis quantified significant concentration-effect relationships for the n-back reaction time, n-back accuracy, and adaptive tracking. In conclusion, Biperiden caused M1 mAChR-related dose- and concentration-dependent temporary declines in cognitive functioning. Therefore a Biperiden pharmacological challenge model can be used for proof-of-pharmacology studies and to demonstrate cognition-enhancing effects of new cholinergic compounds that are being developed.
Biperiden-Induced Delirium In A Five-Years Old Child
Curr Drug Saf 2019;14(1):48-50.PMID:30370855DOI:10.2174/1574886313666181029101830.
Objective: Extrapyramidal adverse effects of antipsychotic drugs are more reported in children. Biperiden is an anticholinergic agent to treat the adverse effects of antipsychotic drugs. The drug has the potential to induce delirium at toxic doses. However, data are scarce about delirium associated with Biperiden in children. Thus far, a case of delirium has been associated with Biperiden in an adolescent patient. We report the first case of delirium associated with the use of Biperiden in a preadolescent patient. Case report: A boy aged five years and weighing 20 kilograms had been diagnosed as having oppositional defiant disorder and separation anxiety disorder in the previous treatment center. Ten milligrams fluoxetine and 0.25 milligrams risperidone had been initiated. On the third day of treatment, dystonia developed and he was administered with Biperiden. An hour later, he was brought to our emergency clinic due to disorganized speech and behavior. His vital signs were stable. There were no findings in blood and urine tests. No electrolyte imbalance, liver, kidney, and thyroid dysfunction have been observed. His neurologic examination was unremarkable and no abnormal findings were shown on cranial magnetic resonance imaging. No other system findings or findings pointing out to infectious diseases have been observed. One milligram physostigmine was administered with intravenous infusion. However, symptoms did not resolve and he was diagnosed with delirium. Naranjo Adverse Drug Reaction Probability Scale score was seven, indicating a "Probable" Adverse Drug Reaction. Half milligram haloperidol was administered bid for three days and he was discharged with complete recovery. Conclusion: Clinicians must be aware of the risk of delirium when using non-toxic doses of Biperiden in young children.
The antimuscarinic agent Biperiden selectively impairs recognition of abstract figures without affecting the processing of non-words
Hum Psychopharmacol 2022 Mar;37(2):e2819.PMID:34533841DOI:10.1002/hup.2819.
Objectives: The present study investigated the effects of Biperiden, a muscarinic type 1 antagonist, on the recognition performance of pre-experimentally unfamiliar abstract figures and non-words in healthy young volunteers. The aim was to examine whether 4 mg Biperiden could model the recognition memory impairment seen in healthy aging. Methods: A double-blind, placebo-controlled, two-way crossover study was conducted. We used a three-phase (deep memorization, shallow memorization, and recognition) old/new discrimination paradigm in which memory strength was manipulated. Strong memories were induced by deep encoding and repetition. Deep encoding was encouraged by redrawing the abstract figures and mentioning existing rhyme words for the non-words (semantic processing). Weak memories were created by merely instructing the participants to study the stimuli (shallow memorization). Results: Biperiden impaired recognition accuracy and prolonged reaction times of the drawn and the studied abstract figures. However, participants were biased towards "old" responses in the placebo condition. The recognition of the new abstract figures was unaffected by the drug. Biperiden did not affect the recognition of the non-words. Conclusions: Although Biperiden may model age-related deficits in episodic memory, the current findings indicate that Biperiden does not mimic age-related deficits in recognition performance.
Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase
Biomed Res Int 2017;2017:2532764.PMID:28785576DOI:10.1155/2017/2532764.
Biperiden is a drug used in Parkinson disease treatment and it serves also as an antiseizures compound in organophosphates poisoning. It acts as antagonist of muscarinic receptor activated by acetylcholine while the enzyme acetylcholinesterase (AChE) cleaves acetylcholine in synaptic junction into choline and acetic acid. This enzyme is inhibited by various compounds; however there has not been proposed evidence about interaction with Biperiden molecule. We investigated this interaction using standard Ellman's assay and experimental findings were critically completed with an in silico prediction by SwissDock docking software. Uncompetitive mechanism of action was revealed from Dixon plot and inhibition constant (Ki ) was calculated to be 1.11 mmol/l. The lowest predicted binding energy was -7.84 kcal/mol corresponding to H-bond between Biperiden molecule and Tyr 341 residuum in protein structure of AChE. This interaction seems to be further stabilized by π-π interaction with Tyr 72, Trp 286, and Tyr 341. In conclusion, Biperiden appears as a very weak inhibitor but it can serve as a lead structure in a pharmacological research.
Effects of Biperiden (cholinergic muscarinic m1/m4 receptor antagonist) on ethanol conditioned place preference in mice
Neurosci Lett 2021 Feb 6;745:135551.PMID:33346074DOI:10.1016/j.neulet.2020.135551.
Background: Previous studies suggest that muscarinic cholinergic receptors might act upon the dopamine release in the mesolimbic system and alter drug-reinforcing values related to drug craving. Aims: We examined the effects of systemic Biperiden administration, a muscarinic cholinergic (M1/M4) receptor antagonist, on ethanol (dose of 2 g/Kg) conditioned place preference (CPP), neuronal activation, dopamine and its metabolites levels in the nucleus accumbens. Methods: Thirty minutes before the ethanol-induced CPP test, mice received saline or Biperiden at doses of 1.0, 5.0, or 10.0 mg/kg. The time spent in each compartment was recorded for 15 min. After the CPP protocol, animals were euthanized, and we investigated the activation of the nucleus accumbens by immunohistochemistry for Fos. We also quantified dopamine, homovanillic acid (HVA), and dihydroxyphenylacetic acid (DOPAC) levels in the nucleus accumbens by high-performance liquid chromatography (HPLC). Additionally, the rotarod was employed to evaluate the effects of Biperiden on motor coordination. Results: Biperiden at different doses (1.0, 5.0, and 10.0 mg/kg) blocked the expression of ethanol-induced CPP. These Biperiden doses increased the number of Fos-positive cells and the dopamine turnover in the nucleus accumbens. None of the doses affected the motor coordination evaluated by the rotarod. Conclusions: Our results show that Biperiden can modulate the effect of alcohol reward, and its mechanism of action may involve a change in dopamine and cholinergic mesolimbic neurotransmission.