| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
CAS# 24570-49-8. Muscarine is a prototype muscarinic acetylcholine receptor (mAChR) agonist, acting as a non‑selective agonist at all five mAChR subtypes (M1, M2, M3, M4, M5). It mimics the action of acetylcholine on parasympathetic effector organs, leading to effects such as salivation, bradycardia, and smooth muscle contraction. The iodide salt enhances stability and solubility for experimental use.
|
|---|---|
| ln Vitro |
Administering 100 µM of muscarine iodide causes an intracellular calcium signal amplitude that is comparable to that produced by 10 µM ACh[1]. A dose-dependent hyperpolarization is induced by muscarine iodide (1-30 μM) in a subpopulation of NRM cells that have 5-hydroxytryptamine (5-HT) on their NRM neurons[2].
In vitro, muscarine iodide (1-30 uM) produces a dose‑dependent hyperpolarization in a sub‑population of nucleus raphe magnus (NRM) neurons that contain serotonin (5‑HT). Administration of 100 uM muscarine iodide induces an intracellular calcium signal amplitude similar to that triggered by 10 uM acetylcholine in brain microvascular endothelial cells. Muscarine activates all mAChR subtypes, leading to G‑protein coupling, PLC activation (M1, M3, M5), Ca2+ mobilization, inhibition of adenylyl cyclase (M2, M4), and various downstream signaling pathways. |
| ln Vivo |
In vivo, muscarine iodide is a potent toxin that stimulates the parasympathetic nervous system, producing effects such as salivation, lacrimation, urination, defecation, bradycardia, miosis, and bronchospasm. It is not used therapeutically due to its toxicity and lack of selectivity. In animal models, it is used to study the physiological and behavioral effects of non‑selective mAChR activation, as well as to test the efficacy of muscarinic antagonists (e.g., atropine).
|
| Enzyme Assay |
For cell‑free binding assays, membranes from rat brain (cortex, striatum, or heart) or from cells expressing specific mAChR subtypes are used. Membranes (20-30 ug protein) are incubated with 0.5-1 nM [3H]N‑methylscopolamine ([3H]NMS) or [3H]quinuclidinyl benzilate ([3H]QNB) and varying concentrations of muscarine iodide (0.1-1000 nM) in 50 mM Tris‑HCl buffer (pH 7.4) containing 1 mM MgCl2, 5 mM EDTA, and 0.1% BSA for 60-90 min at 23degC. Non‑specific binding is determined with 10 uM atropine. Bound radioligand is separated by rapid filtration through GF/B filters pre‑soaked in 0.3% polyethyleneimine, followed by three washes with ice‑cold buffer. Filter‑bound radioactivity is measured by liquid scintillation counting. IC₅0 values are calculated, and Ki values are derived. For functional competition experiments, muscarine is used as a competitor to determine the affinity of other test compounds. For [3⁵S]GTPgammaS binding assays, membranes are incubated with GDP (10 uM), [3⁵S]GTPgammaS (0.1 nM), and muscarine (0.1-1000 nM) for 30 min at 30degC; bound radioactivity is quantified after filtration.
|
| Cell Assay |
For cellular assays, CHO or HEK‑293 cells stably expressing specific mAChR subtypes are seeded in 96‑well plates (40,000 cells/well) in DMEM/10% FBS for 48 h. For calcium mobilization assays (for M1, M3, M5 subtypes), cells are loaded with Fluo‑4 AM (2.5 uM) in HBSS buffer containing 20 mM HEPES and 2.5 mM probenecid for 60 min at 37degC. Cells are washed and then stimulated with varying concentrations of muscarine iodide (0.01-1000 uM). Fluorescence is measured (ex 485 nm, em 525 nm). EC₅0 values are determined from the concentration‑response curves. For cAMP inhibition assays (M2, M4 subtypes), cells are pre‑incubated with 0.5 mM IBMX for 15 min, then stimulated with muscarine (0.01-1000 uM) in the presence of 1 uM forskolin. After 30 min, cAMP levels are quantified by HTRF or ELISA. The EC₅0 for inhibition of cAMP production is calculated. For electrophysiology, whole‑cell patch‑clamp recordings are made from neurons or transfected cells; muscarine (0.1-100 uM) is applied, and its effect on membrane potential, ion currents (e.g., potassium current, M‑current), or firing rate is measured.
|
| Animal Protocol |
In vivo studies with muscarine iodide are typically performed in anesthetized rats or mice to assess parasympathetic effects. Animals (male Sprague‑Dawley rats, 200-300 g) are anesthetized with urethane (1.5 g/kg IP) or sodium pentobarbital (40-50 mg/kg IP). The femoral vein is cannulated for drug administration. Muscarine iodide is dissolved in sterile saline (0.9% NaCl) and administered intravenously (5-50 ug/kg) as a bolus injection. The ECG (lead II) is recorded to measure heart rate (bradycardia). Blood pressure (via arterial cannula) and respiratory rate may also be recorded. The onset and duration of effects (e.g., hypotension, bradycardia, salivation) are monitored. For reversal studies, atropine (0.1-1 mg/kg IV) is administered 5-10 min after muscarine to confirm the specificity of the effects. For behavioral studies in conscious rats, muscarine (0.1-1 mg/kg IP) induces tremor, salivation, and reduced locomotor activity. Tremor is quantified using a force plate actimeter or by visual scoring. Locomotor activity is measured in open field chambers. For secretion studies, salivation is measured by collecting saliva with pre‑weighed filter paper inserted into the mouth; the increase in weight (mg) over 10-20 min is measured. At the end of the experiment, animals are euthanized.
|
| ADME/Pharmacokinetics |
Muscarine iodide (C9H20INO2, MW 301.17) is a quaternary ammonium compound with low lipid solubility. It does not readily cross the blood‑brain barrier (BBB) when administered systemically, so its CNS effects are limited unless administered intracerebroventricularly (ICV). It is water‑soluble. The iodide salt is stable. After systemic administration, muscarine is rapidly cleared from the blood (t½ ~5-15 min) by renal excretion (as the parent compound) and by metabolism in the liver. It is not highly protein‑bound (less than 30%). The iodide ion does not alter the pharmacokinetics. For CNS studies, muscarine can be injected ICV (1-10 ug/rat in 5-10 uL).
|
| Toxicity/Toxicokinetics |
Muscarine iodide is a moderately toxic compound. The LD₅0 in rats after IV administration is ~0.23 mg/kg (230 ug/kg). The primary cause of death is respiratory failure due to bronchospasm and bradycardia. Symptoms of muscarine poisoning are blocked by atropine (a muscarinic antagonist). At sub‑lethal doses (5-50 ug/kg IV in rats), muscarine produces transient bradycardia, hypotension, and salivation, from which animals recover within 30-60 min. No chronic toxicity studies have been conducted. The compound is for research use only and is not a drug. Standard safety precautions for handling toxic substances should be followed.
|
| References |
|
| Additional Infomation |
See other relationships...
Muscarine iodide (CAS 24570-49-8) is a non‑selective muscarinic acetylcholine receptor (mAChR) agonist and a prototype toxin that stimulates the parasympathetic nervous system. It is used as a research tool to study cholinergic signaling, autonomic function, and muscarinic receptor pharmacology. The compound has not entered clinical trials and is not FDA‑approved for any therapeutic indication. Storage: powder at -20degC, sealed, away from moisture. The (S)‑enantiomer is the naturally occurring form. (+)-Muscarine iodide is the active isomer. |
| Molecular Formula |
C9H20INO2
|
|---|---|
| Molecular Weight |
301.17
|
| Exact Mass |
301.054
|
| CAS # |
24570-49-8
|
| Related CAS # |
Muscarine-d9 iodide;Muscarine;300-54-9;Muscarine chloride;2303-35-7
|
| PubChem CID |
102226
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
13
|
| Complexity |
153
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C[C@H]1[C@@H](C[C@H](O1)C[N+](C)(C)C)O.[I-]
|
| InChi Key |
PMFYONXEPDMBPE-CTERPIQNSA-M
|
| InChi Code |
InChI=1S/C9H20NO2.HI/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
|
| Chemical Name |
[(2S,4R,5S)-4-hydroxy-5-methyloxolan-2-yl]methyl-trimethylazanium;iodide
|
| 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, 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 | 3.3204 mL | 16.6019 mL | 33.2038 mL | |
| 5 mM | 0.6641 mL | 3.3204 mL | 6.6408 mL | |
| 10 mM | 0.3320 mL | 1.6602 mL | 3.3204 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
