Rapacuronium bromide (Org 9487) 是一种非去极化神经肌肉阻滞剂，是毒蕈碱乙酰胆碱受体 (mAChR) 的变构调节剂。

Rapacuronium bromide (Org 9487), a non-depolarizing neuromuscular blocker, is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).

Solid

Muscarinic receptor

Rapacuronium binds to all muscarinic receptor subtypes at physiologically relevant concentrations and displays micromolar affinity and slight selectivity towards M2 receptor. Rapacuronium exhibits complex effects on the kinetics of ACh binding and subsequent receptor activation estimated from stimulation of [S]GTPγS binding. Rapacuronium alone concentration dependently lowers [S]GTPγS binding to membranes with a maximal effect of approximately 25% at odd-numbered subtypes and 15% at even-numbered subtypes, with EC50 ranging from 28 μM at M2 receptors to 76 μM at M3 receptors. While the EC50 values of Rapacuronium in inhibiting [S]GTPγS binding at individual subtypes correlated with affinities measured in binding experiments with [H]ACh (R = 0.76) they are lower (4- to 12-fold) at all subtypes. Measurements of ACh-stimulate

Time course of the neuromuscular effects of Rapacuronium following the administration of the 2×ED 90 doses to rats and guinea-pigs with ED 90 of 5953±199 and 187±16 μg/kg in rat and guinea pig, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Jakubík J, et al. Divergence of allosteric effects of Rapacuronium on binding and function of muscarinic receptors. BMC Pharmacol. 2009 Dec 28;9:15.
[2]. Vizi ES, et al. A new short-acting non-depolarizing muscle relaxant (SZ1677) without cardiovascular side-effects. Acta Anaesthesiol Scand. 2003 Mar;47(3):291-300.

In Vitro: DMSO : ≥ 125 mg/mL (184.42 mM)配制储备液