| Title : Blockade of nicotinic currents in hippocampal neurons defines methyllycaconitine as a potent and specific receptor antagonist - Alkondon_1992_Mol.Pharmacol_41_802 |
| Author(s) : Alkondon M , Pereira EF , Wonnacott S , Albuquerque EX |
| Ref : Molecular Pharmacology , 41 :802 , 1992 |
| Abstract : Methyllycaconitine, a toxin isolated from the seeds of Delphinium brownii, inhibited acetylcholine- and anatoxin-induced whole-cell currents in cultured fetal rat hippocampal neurons, at picomolar concentrations. This antagonism was specific, concentration dependent, reversible, and voltage independent. Furthermore, methyllycaconitine inhibited 125I-alpha-bungarotoxin binding to adult rat hippocampal membranes, protected against the alpha-bungarotoxin-induced pseudoirreversible blockade of nicotinic currents, and shifted the concentration-response curve of acetylcholine to the right in fetal rat hippocampal neurons, suggesting a possible competitive mode of action for this toxin. Remarkably low concentrations of methyllycaconitine (1-1000 fM) decreased the frequency of anatoxin-induced single-channel openings, with no detectable decrease in the mean channel open time. These actions of methyllycaconitine commend this neurotoxin for the characterization of the alpha-bungarotoxin-sensitive subclass of neuronal nicotinic receptors, which has hitherto eluded functional demonstration. |
| ESTHER : Alkondon_1992_Mol.Pharmacol_41_802 |
| PubMedSearch : Alkondon_1992_Mol.Pharmacol_41_802 |
| PubMedID: 1569927 |
Alkondon M, Pereira EF, Wonnacott S, Albuquerque EX (1992)
Blockade of nicotinic currents in hippocampal neurons defines methyllycaconitine as a potent and specific receptor antagonist
Molecular Pharmacology
41 :802
Alkondon M, Pereira EF, Wonnacott S, Albuquerque EX (1992)
Molecular Pharmacology
41 :802