Pub. Date : 2014 Apr
PMID : 24417241
8 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Allosteric effects of erythromycin pretreatment on thioridazine block of hERG potassium channels. | Erythromycin | ETS transcription factor ERG | Homo sapiens |
| 2 | Experiments were conducted to determine if concomitant exposure to two potent pore hERG blockers, thioridazine and terfenadine and a weak hERG blocker, erythromycin, would result in an additive, synergistic or inhibitory effect. | Erythromycin | ETS transcription factor ERG | Homo sapiens |
| 3 | KEY RESULTS: Pre-exposure of cells to erythromycin resulted in an approximately 14-22-fold rightward shift in the hERG concentration-response curve for thioridazine and terfenadine respectively. | Erythromycin | ETS transcription factor ERG | Homo sapiens |
| 4 | CONCLUSIONS AND IMPLICATIONS: Pretreatment with erythromycin induced an approximately 14-22-fold reduction in hERG affinity for pore-binding drugs at concentrations of erythromycin, which by themselves only block hERG by 10% or less. | Erythromycin | ETS transcription factor ERG | Homo sapiens |
| 5 | CONCLUSIONS AND IMPLICATIONS: Pretreatment with erythromycin induced an approximately 14-22-fold reduction in hERG affinity for pore-binding drugs at concentrations of erythromycin, which by themselves only block hERG by 10% or less. | Erythromycin | ETS transcription factor ERG | Homo sapiens |
| 6 | CONCLUSIONS AND IMPLICATIONS: Pretreatment with erythromycin induced an approximately 14-22-fold reduction in hERG affinity for pore-binding drugs at concentrations of erythromycin, which by themselves only block hERG by 10% or less. | Erythromycin | ETS transcription factor ERG | Homo sapiens |
| 7 | CONCLUSIONS AND IMPLICATIONS: Pretreatment with erythromycin induced an approximately 14-22-fold reduction in hERG affinity for pore-binding drugs at concentrations of erythromycin, which by themselves only block hERG by 10% or less. | Erythromycin | ETS transcription factor ERG | Homo sapiens |
| 8 | Furthermore, these results suggest that co-administration of erythromycin may provide some reduction in cardiac liability of potent hERG-blocking drugs. | Erythromycin | ETS transcription factor ERG | Homo sapiens |