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Methoctramine tetrahydrochloride is a potent and cardioselective antagonist of the M2 muscarinic receptor, capable of inhibiting muscarine-induced bradycardia in vivo.


| Description | Methoctramine tetrahydrochloride is a potent and cardioselective antagonist of the M2 muscarinic receptor, capable of inhibiting muscarine-induced bradycardia in vivo. |
| In vitro | Methoctramine tetrahydrochloride effectively inhibits the increase in PG synthesis triggered by Acetylcholine (ACh) and Arecaidine propargyl ester (APE) in a dose-dependent manner[1]. At concentrations ranging from 0.01 to 1 μM, it enhances the contractions resulting from both pre- and postganglionic nerve stimulations in guinea-pig tracheal tubes that are isolated and innervated[2]. Moreover, when the concentration of Methoctramine tetrahydrochloride reaches or exceeds 10 μM, it diminishes the reactions to nerve stimulation as well as to exogenously applied ACh[2]. |
| In vivo | Methoctramine (300 μg/kg; i.v.) tetrahydrochloride strongly inhibits the Methacholine- and Muscarine-induced bradycardia in the anaesthetized rat, respectively[3]. |
| Molecular Weight | 619.38 |
| Formula | C36H63ClN4O2 |
| Cas No. | 104807-46-7 |
| Smiles | Cl.COc1ccccc1CNCCCCCCNCCCCCCCCNCCCCCCNCc1ccccc1OC |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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