BW284c51 blocks nicotinic acetylcholine receptors transplanted to Xenopus oocytes.
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.
Olivera
S
S
División de Fisiología, Universidad de Alicante. E-03080 Alicante, Spain.
Jiménez
R
R
Lax
P
P
Ivorra
I
I
Morales
A
A
D000818:Animals; D002093:Benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(N,N-dimethyl-N-2-propenyl-), Dibromide / Q000737:chemistry / Q000494:pharmacology*; D004594:Electrophysiology; D015394:Molecular Structure; D009865:Oocytes / Q000187:drug effects* / Q000378:metabolism*; D018408:Patch-Clamp Techniques; D011978:Receptors, Nicotinic / Q000235:genetics / Q000378:metabolism*; D014101:Torpedo; D014982:Xenopus laevis
D011978:Receptors, Nicotinic; D002093:Benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(N,N-dimethyl-N-2-propenyl-), Dibromide