PMID: 8584042Sep 1, 1995Paper

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

Naunyn-Schmiedeberg's Archives of Pharmacology
F BorsiniA Donetti

Abstract

In the search for antidepressant agents with a rapid onset of action, we have found that compound BIMT 17 (1-[2-[4-(3-trifluoromethylphenyl)piperazin-1- 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), and antagonized 5-HT-induced phosphatidylinositol turnover (pKi = 6.96) in the cerebral cortex. The effect on cAMP accumulation was blocked by the 5-HT1A receptor antagonist tertatolol. Buspirone, 8-OH-DPAT and S 14671 (1-[2-(2-thenoylamino)ethyl]- 4[1-(7-methoxynaphtyl)]-piperazine), claimed to be 5-HT1A receptor agonists, did not reduce forskolin-stimulated cAMP formation in the cerebral cortex. On the basis of these data, it was concluded that BIMT 17 was the only compound that behaved as a full agonist with respect to the cAMP response in the cortex, while exerting concurrent agonism at 5-HT1A receptors and antagonism at 5-HT2A receptors. These characteristics might explain the peculiar behavior of BIMT 17 in mimicking the inhibit...Continue Reading

Citations

May 3, 2007·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Jesper EkelundMarc Laruelle
Jan 5, 2002·European Journal of Pharmacology·F Borsini, R Cesana
Jan 26, 2000·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·A BrambillaF Borsini
Nov 19, 2013·Pharmacology, Biochemistry, and Behavior·Lynda Uphouse
Feb 2, 2010·Social Science & Medicine·Annemarie Jutel
Nov 2, 2005·The Journal of Pharmacy and Pharmacology·Roberto PerroneVincenzo Tortorella
Nov 18, 2005·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Llorenç Díaz-MataixPau Celada
Mar 10, 2004·The Journal of Pharmacy and Pharmacology·Marcello LeopoldoVincenzo Tortorella
Jul 3, 2007·Neurochemistry International·Gino GiannacciniAntonio Lucacchini

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