| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Cycrimine targets the muscarinic acetylcholine receptor M1. It functions as an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist. By binding to and blocking these receptors, Cycrimine reduces the levels of acetylcholine in the central nervous system. This antagonism helps to restore the balance between dopamine and acetylcholine in the brain, which is disrupted in Parkinson's disease.
|
|---|---|
| ln Vitro |
In vitro, Cycrimine acts as a muscarinic receptor antagonist. Its anticholinergic activity is characterized by its ability to block the effects of acetylcholine at muscarinic receptors. This activity is responsible for its pharmacological effects, including reducing tremors and muscle rigidity in Parkinson's disease.
|
| ln Vivo |
In vivo, Cycrimine is effective in reducing the symptoms of Parkinson's disease, including tremors, rigidity, and bradykinesia. It is administered orally and is used as an adjunctive therapy to levodopa or other dopaminergic agents. Its central anticholinergic action helps to improve motor function and reduce extrapyramidal symptoms.
|
| Enzyme Assay |
In cell-free receptor binding assays, Cycrimine's activity is evaluated by measuring its affinity for muscarinic acetylcholine receptors. Membrane preparations from tissues or cells expressing the M1 receptor are incubated with a radiolabeled antagonist (e.g., [3H]N-methylscopolamine or [3H]quinuclidinyl benzilate) and varying concentrations of Cycrimine. The displacement of the radioligand is measured, and the Ki is calculated from the competition curve.
|
| Cell Assay |
In vitro cell-based experiments with Cycrimine typically involve cell lines expressing muscarinic receptors, such as CHO cells transfected with M1 receptors. Cells are treated with the compound in the presence of a muscarinic agonist (e.g., carbachol), and the inhibition of agonist-induced intracellular calcium mobilization or inositol phosphate accumulation is measured. The IC50 for antagonism is determined from the concentration-response curve.
|
| Animal Protocol |
In vivo animal experiments with Cycrimine have been conducted in animal models of Parkinson's disease, such as the reserpine-induced catalepsy model or the 6-hydroxydopamine (6-OHDA) lesioned rat model. Animals are administered Cycrimine orally or intraperitoneally, and motor function is assessed using behavioral tests such as the rotarod test or the open field test. The compound's ability to reverse catalepsy or improve motor function is measured.
|
| ADME/Pharmacokinetics |
Cycrimine is an orally active anticholinergic agent. Its pharmacokinetic properties include good oral absorption and distribution to the central nervous system, which is necessary for its therapeutic effect in Parkinson's disease. The compound is metabolized in the liver and excreted primarily via the kidneys. No specific PK parameters (e.g., half-life, Cmax) are provided in the search results.
|
| Toxicity/Toxicokinetics |
Protein Binding
14-21% Cycrimine is generally well-tolerated at therapeutic doses. Common adverse effects associated with anticholinergic drugs include dry mouth, blurred vision, constipation, urinary retention, and cognitive impairment. Due to its central anticholinergic activity, it may cause confusion or hallucinations, particularly in elderly patients. The compound is for research use only. |
| References | |
| Additional Infomation |
Cycrimine, a piperidine derivative, is chemically named 3-(piperidin-1-yl)prop-1-ol, where one hydrogen atom at position 1 is replaced by a cyclopentyl group and the other by a phenyl group. It is a centrally acting anticholinergic drug, and its hydrochloride salt is commonly used in the treatment and management of Parkinson's disease. Cycrimine possesses pharmacological effects against Parkinson's disease, muscarinic receptor antagonism, and motor dysfunction. It is a tertiary alcohol, belonging to the piperidine class and also a tertiary amine. Cycrimine is a drug used to lower acetylcholine levels to restore its balance with dopamine, and is used to treat and control Parkinson's disease. Drug Indications: Used for the treatment and control of Parkinson's disease. Mechanism of Action: Cycrimine binds to the muscarinic acetylcholine receptor M1, effectively inhibiting acetylcholine. The reduction in acetylcholine levels restores the normal dopamine-acetylcholine balance, thereby alleviating Parkinson's disease symptoms.
Pharmacodynamics Cyclohexylamine is a centrally acting anticholinergic drug used to treat symptoms of Parkinson's disease. It is a drug used to lower acetylcholine levels. Acetylcholine normally maintains a balance with the neurotransmitter dopamine; however, dopamine levels are low in the brains of Parkinson's patients. It is believed that lowering acetylcholine levels may restore this balance. Cycrimine is a centrally acting anticholinergic drug with a molecular formula of C19H29NO and a molecular weight of 287.44. It is also known as 1-cyclopentyl-1-phenyl-3-piperidin-1-ylpropan-1-ol. It is typically used as its hydrochloride salt in the treatment of Parkinson's disease. The compound is available for research purposes only and is not intended for clinical use outside of approved indications. |
| Molecular Formula |
C19H29NO
|
|---|---|
| Molecular Weight |
287.44
|
| Exact Mass |
287.225
|
| CAS # |
77-39-4
|
| PubChem CID |
2911
|
| Appearance |
White to off-white solid powder
|
| Density |
1.057g/cm3
|
| Boiling Point |
433.5ºC at 760 mmHg
|
| Melting Point |
112-113
|
| Flash Point |
205.7ºC
|
| Index of Refraction |
1.554
|
| LogP |
3.878
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
21
|
| Complexity |
301
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
SWRUZBWLEWHWRI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H29NO/c21-19(18-11-5-6-12-18,17-9-3-1-4-10-17)13-16-20-14-7-2-8-15-20/h1,3-4,9-10,18,21H,2,5-8,11-16H2
|
| Chemical Name |
1-cyclopentyl-1-phenyl-3-piperidin-1-ylpropan-1-ol
|
| Synonyms |
Cicrimina; Pagitane; Cycrimine
|
| HS Tariff Code |
2934.99.9001
|
| 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 (e.g. under nitrogen), 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)
|
| Solubility (In Vitro) |
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
|
|---|---|
| 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 | 3.4790 mL | 17.3949 mL | 34.7899 mL | |
| 5 mM | 0.6958 mL | 3.4790 mL | 6.9580 mL | |
| 10 mM | 0.3479 mL | 1.7395 mL | 3.4790 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
