Bioactivity | Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine-induced bradycardia in vivo[1][2][3]. |
Target | M2 muscarinic receptor |
Invitro | Methoctramine tetrahydrochloride attenuates Acetylcholine (ACh)- and Arecaidine propargyl ester (APE)-induced increases in PG synthesis in a concentration-dependent manner[1].Methoctramine (0.01-1 μM) tetrahydrochloride causes facilitation of contractions induced by both pre- and postganglionic nerve stimulation in the guinea-pig isolated, innervated tracheal tube preparation[2].Methoctramine (≥10 μM) tetrahydrochloride reduces responses to both nerve stimulation and exogenous 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]. |
Name | Methoctramine tetrahydrochloride |
CAS | 104807-46-7 |
Formula | C36H66Cl4N4O2 |
Molar Mass | 728.75 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Jaiswal N, et, al. Methoctramine, a cardioselective antagonist: muscarinic receptor mediating prostaglandin synthesis in isolated rabbit heart. Eur J Pharmacol. 1991 Jan 3;192(1):63-70. [2]. Watson N, et, al. Actions of methoctramine, a muscarinic M2 receptor antagonist, on muscarinic and nicotinic cholinoceptors in guinea-pig airways in vivo and in vitro. Br J Pharmacol. 1992 Jan;105(1):107-12. [3]. Wess J, et, al. Methoctramine selectively blocks cardiac muscarinic M2 receptors in vivo. Naunyn Schmiedebergs Arch Pharmacol. 1988 Sep;338(3):246-9. |