Overview
- Buckett, W.R. et al. (1968) Br.J. Pharmacol. 32, 671.
- Wenningmann, I. et al. (2001) Mol. Pharmacol. 60, 790.
- Filatov, G.N. et al. (1993) Mol. Pharmacol. 44, 237.
Alomone Labs Pancuronium bromide inhibits α7 nAChR heterologously expressed in Xenopus oocytes.A. Current traces of α7 nAChR activity at -60 mV holding potential. Currents were elicited by applications of 100 μM acetylcholine every 100 seconds. Inhibition of these induced currents was achieved upon perfusion of 0.2, 2 or 20 μM Pancuronium bromide (#P-130) (indicated by the horizontal bars). B. Superimposed traces of α7 nicotinic ACh channel current in the absence or presence of 0.2, 2 or 20 μM Pancuronium bromide, as indicated (taken from the experiment described in A).
- Kombo, D.C. et al. (2011) Eur. J. Med. Chem.46, 5625.
- Buckett, W.R. et al. (1968) Br.J. Pharmacol. 32, 671.
- Tuba, Z. et al. (2002) Curr. Med. Chem. 9, 1507.
- Bowman, W.C. et al. (2006) Br. J. Pharmacol. 1, S277.
- Wenningmann, I. et al. (2001) Mol. Pharmacol. 60, 790.
- Filatov, G.N. et al. (1993) Mol. Pharmacol. 44, 237.
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 acetylcholine (ACh) and are validated therapeutic targets for various CNS pathologies1.
Pancuronium bromide is a competitive neuromuscular blocking agent and a skeletal muscle relaxant2. It is a bulky molecule of Bovet's pachycurare type and therefore has a nondepolarising mechanism of action2.
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 movement3. 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 anaesthesia4. It blocks the nAChR current with an IC50 of 5.5 nM in BC3H-1 cells expressing embryonic mouse muscle nAChR5 and its Ki value for the receptor is 0.96.
Pancuronium bromide (#P-130) is a highly pure, synthetic, and biologically active compound.
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