title: BW284c51 blocks nicotinic acetylcholine receptors transplanted to Xenopus oocytes.
abstract: 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.
authors.affiliation: División de Fisiología, Universidad de Alicante. E-03080 Alicante, Spain.
authors.forename: S
authors.initials: S
authors.lastname: Olivera
authors.forename: R
authors.initials: R
authors.lastname: Jiménez
authors.forename: P
authors.initials: P
authors.lastname: Lax
authors.forename: I
authors.initials: I
authors.lastname: Ivorra
authors.forename: A
authors.initials: A
authors.lastname: Morales
mesh_terms: 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
chemical_list: D011978:Receptors, Nicotinic; D002093:Benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(N,N-dimethyl-N-2-propenyl-), Dibromide