Pancuronium bromide. A Potent�nAChR Antagonist.
nAChRs are members of the Cys-Loop ligand-gated ion channel superfamily, located both in the peripheral and central nervous systems (PNS and CNS, respectively). They mediate rapid synaptic transmission by increasing the conductance of the postsynaptic cell membrane in response to nerve-released acetyl choline (ACh) and are validated therapeutic targets for various CNS pathologies.
Pancuronium bromide is a competitive neuromuscular blocking agent and a skeletal muscle relaxant. It is a bulky molecule of Bovet's pachycurare type and therefore has a nondepolarising mechanism of action.
Neuromuscular blocking agents have been used routinely to provide skeletal muscle relaxation during surgical procedures allowing access to body cavities without hindrance from voluntary or reflex muscle movement.
Pancuronium remains one of few drugs logically and successfully designed on the drawing board and after about 40 years, it is still used in surgical anaesthesia. It blocks the nAChR current with an IC50 of 5.5 nM in BC3H-1 cells expressing embryonic mouse muscle nAChR and its Ki value for the receptor is 0.9.
Ion Channel Modulators; Nicotinic Acetylcholine Receptor Blockers
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