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Exploratory drug safety: a discovery strategy to reduce attrition in development.
Pre-clinical toxicological investigations in discovery serve the important objective of identifying the most promising candidates to progress into development and onto registration. Expand
Assessment of seizure liability of Org 306039, a 5-HT2c agonist, using hippocampal brain slice and rodent EEG telemetry.
In vitro and in vivo models complement each other in the characterization of the seizure potential of CNS-targeted compounds such as the 5-HT2c agonist Org 306039, indicating seizure-genic potential. Expand
Removal of hERG potassium channel affinity through introduction of an oxygen atom: Molecular insights from structure‐activity relationships of strychnine and its analogs
This study suggests that introduction of an oxygen to compensate for the N+ − charge could be a useful strategy for reducing hERG potency and increasing the safety margin of alkaloid‐type compounds in drug development. Expand