Pub. Date : 2014 Feb
PMID : 24307198
6 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Mechanism of hERG channel block by the psychoactive indole alkaloid ibogaine. | Ibogaine | ETS transcription factor ERG | Homo sapiens |
| 2 | Therefore, we studied in detail the interaction of ibogaine with hERG channels heterologously expressed in mammalian kidney tsA-201 cells. | Ibogaine | ETS transcription factor ERG | Homo sapiens |
| 3 | Currents through hERG channels were blocked regardless of whether ibogaine was applied via the extracellular or intracellular solution. | Ibogaine | ETS transcription factor ERG | Homo sapiens |
| 4 | Mutations in the binding site reported for other hERG channel blockers (Y652A and F656A) reduced the potency of ibogaine, whereas an inactivation-deficient double mutant (G628C/S631C) was as sensitive as wild-type channels. | Ibogaine | ETS transcription factor ERG | Homo sapiens |
| 5 | Experimental current traces were fit to a kinetic model of hERG channel gating, revealing preferential binding of ibogaine to the open and inactivated state. | Ibogaine | ETS transcription factor ERG | Homo sapiens |
| 6 | Taken together, these findings show that ibogaine blocks hERG channels from the cytosolic side either in its charged form alone or in company with its uncharged form and alters the currents by changing the relative contribution of channel states over time. | Ibogaine | ETS transcription factor ERG | Homo sapiens |