BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex

@article{Borsini2004BIMT1A,
  title={BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex},
  author={Franco Borsini and Ettore Giraldo and Eugenia Monferini and Giovanni Antonini and Marco Daniele Parenti and Giuseppe Bietti and Arturo Donetti},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2004},
  volume={352},
  pages={276-282}
}
In the search for antidepressant agents with a rapid onset of action, we have found that compound BIMT 17 (1-[2-[4-(3-trifluoromethylphenyl)piperazin1-yl]ethyl]benzimidazol-[1H]-2-one) shows a good affinity for cerebral cortical 5-HT1A (pKi = 7.72) and 5-HT2A (pKi = 6.90) receptors, with no appreciable affinity for the other 5-HT receptor subtypes, including 5-HT2C. BIMT 17 reduced forskolin-stimulated cAMP accumulation in the cerebral cortex (pEC50 = 6.09) and in the hippocampus (pEC50 = 6.50… Expand
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