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XB-ART-796
Chem Biol Interact 2005 Dec 15;157-158:404-6. doi: 10.1016/j.cbi.2005.10.076.
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BW284c51 blocks nicotinic acetylcholine receptors transplanted to Xenopus oocytes.

Olivera S , Jiménez R , Lax P , Ivorra I , Morales A .


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We have studied the effects of BW284c51 on the function of Torpedo nicotinic acetylcholine (Ach) receptors (nAchRs) transplanted to Xenopus laevis oocytes. BW284c51 reversible inhibited Ach-elicited currents (IAch) in a concentration-dependent manner, increased IAch desensitisation and changed the Ach concentration-dependence of the IAch from a two-site to a single-site Hill equation, without affecting the EC50. These effects were only present at hyperpolarising potentials, suggesting that nAchR blockade by BW284c51 is non-competitive and likely due to an open channel block as the principal mechanism.

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