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</script>pmid: 7678947
AbstractThe efficacy of decamethonium as an agonist at the nicotinic acetylcholine receptor has never been determined. Here, we demonstrate how patch clamp recording during rapid perfusion of agonists to outside‐out patches from BC3H‐1 cells can be used to provide an unambiguous estimate of the efficacy of decamethonium. First, we obtain the decamethonium concentration‐response relationship between 10 and 1,000 μM decamethonium. The maximum channel open probability is small (<0.02) and occurs at about 100 μM. This suggests two alternative explanations: decamethonium is a poor agonist or decamethonium is an efficacious agonist but a potent channel blocker. To distinguish between these alternatives, we perfuse mixtures of decamethonium and acetylcholine to generate acetylcholine concentration‐response curves in the presence of 30, 100, and 1,000 μM decamethonium. We use a model for activation and block of the acetylcholine receptor by both agonists to fit these data and determine the binding affinity, efficacy, and blocking affinity of decamethonium. We conclude that the efficacy of decamethonium is low 0.016. Decamethonium is a true partial agonist. © 1993 Wiley‐Liss, Inc.
Electrophysiology, Perfusion, Mice, Decamethonium Compounds, Animals, Receptors, Nicotinic, Acetylcholine, Ion Channels, Clone Cells
Electrophysiology, Perfusion, Mice, Decamethonium Compounds, Animals, Receptors, Nicotinic, Acetylcholine, Ion Channels, Clone Cells
| citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically). | 26 | |
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| influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically). | Top 10% | |
| impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network. | Average |
