IndraLab

Statements


| 4

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"Further experiments showed caffeine directly blocks hERG in an open state dependent manner."

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"Caffeine dependent inhibition of hERG current is not altered by raising cAMP with forskolin, buffering cytosolic calcium with 1,2-bis (2-aminophenoxy) ethane-N, N, N ', N '-tetraacetic acid, or inhibition of protein kinase C. Thus, the effects of caffeine are unlikely to be mediated by cAMP or intracellular calcium dependent mechanisms."

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"Propoxyphene blocked HERG currents by slowing down channel activation and accelerating channel deactivation kinetics (Ulens et al., 1999)."

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"Thus, caffeine attenuates hERG currents by binding to a drug receptor located within the inner cavity of the channel."