| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
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| Targets |
Muscarine chloride targets muscarinic acetylcholine receptors (mAChRs). There are five subtypes of muscarinic receptors (M1-M5), which are widely distributed in the central and peripheral nervous systems and in various peripheral tissues. Muscarine acts as a non-selective agonist, activating all five subtypes. This leads to a variety of physiological effects, including decreased heart rate, increased glandular secretions, and smooth muscle contraction.
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| ln Vitro |
The amplitude of the intracellular induced signal caused by muscarine chloride (100 µM) in brain microvascular endothelial cells and simulated brain microvascular endothelial cells was lower than that activated by 10 µM cardiac choline [1]. Simulated supramaximal maxima are produced in a subpopulation of NRM cells expressing 5-responsive tryptamine (5-HT) in the nucleus raphe magnum (NRM) neurons by muscarine chloride (1-30 μM; 2 min). the value of EC50 is 2.7 µM[2].
In vitro, muscarine chloride is used as a standard agonist to study muscarinic receptor function. It is used in receptor binding assays to determine the affinity of other compounds for muscarinic receptors. In functional assays, muscarine is used to activate muscarinic receptors and measure downstream signaling events, such as the accumulation of inositol phosphates or the inhibition of adenylyl cyclase. Its effects are blocked by muscarinic antagonists like atropine. |
| ln Vivo |
In vivo, muscarine chloride produces a range of effects characteristic of muscarinic receptor activation. These include bradycardia (slowed heart rate), hypotension, salivation, lacrimation, urination, defecation, and gastrointestinal distress. These effects are due to the stimulation of the parasympathetic nervous system. Muscarine is a potent toxin, and its ingestion can be dangerous. It is used in research to study the physiological roles of muscarinic receptors.
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| Enzyme Assay |
In vitro receptor binding assays for muscarine chloride are performed using membrane preparations from tissues or cells expressing muscarinic receptors. A radiolabeled antagonist, such as [³H]-N-methylscopolamine or [³H]-quinuclidinyl benzilate (QNB), is used as a tracer. Membranes are incubated with the radioligand and varying concentrations of muscarine. The amount of bound radioligand is measured, and the compound's affinity (Ki) is determined. Functional assays measure the activation of muscarinic receptors.
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| Cell Assay |
For cell-based assays, cells expressing muscarinic receptors are cultured in standard media. Cells are seeded in multi-well plates and treated with muscarine chloride at various concentrations. The activation of muscarinic receptors is measured by assessing downstream signaling events, such as calcium mobilization (for M1, M3, M5 subtypes) or inhibition of forskolin-stimulated cAMP accumulation (for M2, M4 subtypes). Cell viability is assessed using standard assays. All experiments include appropriate controls.
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| Animal Protocol |
In vivo studies with muscarine chloride are typically conducted in animal models to study the physiological effects of muscarinic receptor activation. The compound is administered via routes such as intravenous (IV) or intraperitoneal (IP) injection. Physiological parameters such as heart rate, blood pressure, and salivation are measured. The effects of muscarine can be blocked by pre-treatment with atropine, a muscarinic antagonist, to confirm receptor specificity. All procedures must be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
...Very poor absorption in the gastrointestinal tract... /Mucor/ Muscarine chloride is a quaternary ammonium compound and is therefore charged and poorly absorbed from the gastrointestinal tract. When administered parenterally, it is rapidly distributed and metabolized. The compound is typically used in research settings. Its pharmacokinetic properties are well-characterized in pharmacological literature. |
| Toxicity/Toxicokinetics |
Toxicity Summary
Muscarinic acetylcholine is a competitive inhibitor. It mimics the action of the neurotransmitter acetylcholine on acetylcholine receptors. (L1011) Muscarine chloride is a potent toxin. Its toxic effects are due to excessive activation of muscarinic receptors, leading to parasympathetic overstimulation. Symptoms of poisoning include salivation, lacrimation, urination, defecation, gastrointestinal distress, and respiratory failure. There is no specific antidote, but atropine can be used to block the effects. The compound is for research use only and is not for human consumption. |
| References |
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| Additional Infomation |
Mechanism of Action
Muscarinic alkaloids act almost exclusively on muscarinic receptors… Muscarinic alkaloids stimulate intestinal smooth muscle… Increased tone and peristalsis of the ureter, bladder, gallbladder, and bile ducts… Muscarinic alkaloids are a potent diuretic. After systemic administration, it more realistically mimics parasympathetic excitation than the true parasympathetic agonist acetylcholine. For this reason, and due to its temporal priority, muscarinic alkaloids have been the classic prototype of parasympathomimetic drugs, and the neurological effects of parasympathomimetic drugs are also known as muscarinic-like effects. /Muscarinic Acid/ Muscarine chloride is a classical pharmacological tool, and its primary application is in the study of the cholinergic nervous system. It is a potent and selective agonist of muscarinic acetylcholine receptors. The compound is not an approved drug and is not used therapeutically. It is commercially available from various chemical suppliers for research purposes only. Its discovery and use have been fundamental to our understanding of cholinergic signaling. |
| Molecular Formula |
C9H20CLNO2
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|---|---|
| Molecular Weight |
209.71
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| Exact Mass |
209.118
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| CAS # |
2303-35-7
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| Related CAS # |
Muscarine iodide;24570-49-8;Muscarine;300-54-9
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| PubChem CID |
16817
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| Appearance |
White to off-white solid powder
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| Melting Point |
180-181 °C
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| LogP |
1.032
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
13
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| Complexity |
153
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C[C@H]1[C@@H](C[C@H](O1)C[N+](C)(C)C)O.[Cl-]
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| InChi Key |
WUFRNEJYZWHXLC-CTERPIQNSA-M
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| InChi Code |
InChI=1S/C9H20NO2.ClH/c1-7-9(11)5-8(12-7)6-10(2,3)4;/h7-9,11H,5-6H2,1-4H3;1H/q+1;/p-1/t7-,8-,9+;/m0./s1
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| Chemical Name |
[(2S,4R,5S)-4-hydroxy-5-methyloxolan-2-yl]methyl-trimethylazanium;chloride
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| Synonyms |
(+)-Muscarine chloride; L-(+)-Muscarine chloride; Muscarine chloride
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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) |
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
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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 | 4.7685 mL | 23.8424 mL | 47.6849 mL | |
| 5 mM | 0.9537 mL | 4.7685 mL | 9.5370 mL | |
| 10 mM | 0.4768 mL | 2.3842 mL | 4.7685 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.
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