BW284c51阻断移植到非洲爪蟾卵母细胞中的烟碱型乙酰胆碱受体。
BW284c51 blocks nicotinic acetylcholine receptors transplanted to Xenopus oocytes.
作者信息
Olivera S, Jiménez R, Lax P, Ivorra I, Morales A
机构信息
División de Fisiología, Universidad de Alicante. E-03080 Alicante, Spain.
出版信息
Chem Biol Interact. 2005 Dec 15;157-158:404-6. doi: 10.1016/j.cbi.2005.10.076.
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.
我们研究了BW284c51对移植到非洲爪蟾卵母细胞中的电鳐烟碱型乙酰胆碱（Ach）受体（nAchRs）功能的影响。BW284c51以浓度依赖性方式可逆地抑制Ach诱发电流（IAch），增加IAch脱敏，并将IAch的Ach浓度依赖性从双位点Hill方程改变为单位点Hill方程，而不影响EC50。这些效应仅在超极化电位时出现，表明BW284c51对nAchR的阻断是非竞争性的，可能主要机制是开放通道阻断。
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