Five 2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylic acid derivatives of lupinine, epi-lupinine and lupinylamine, together with two 1-homolupinanoyl benzimidazolones were prepared and investigated for their ability to displace specific radioligands from 5-HT3 and 5-HT4 receptors. The synthesized compounds were only moderately active, with IC50 in the micromolar range. The compound with the highest affinity for 5-HT4 receptor was tested for the enhancement of intestinal transit rate but was inactive at the oral dose of 100 mg/kg.

Quinolizidinyl derivatives of 2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylic acid and 1-homolupinanoyl benzimidazolones as ligands for 5-HT3 and 5-HT4 receptors / A. Sparatore, A. Cagnotto, F. Sparatore. - In: IL FARMACO. - ISSN 0014-827X. - 54:4(1999 Apr 30), pp. 248-254.

Quinolizidinyl derivatives of 2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylic acid and 1-homolupinanoyl benzimidazolones as ligands for 5-HT3 and 5-HT4 receptors

A. Sparatore
Primo
;
1999

Abstract

Five 2,3-dihydro-2-oxo-1H-benzimidazole-1-carboxylic acid derivatives of lupinine, epi-lupinine and lupinylamine, together with two 1-homolupinanoyl benzimidazolones were prepared and investigated for their ability to displace specific radioligands from 5-HT3 and 5-HT4 receptors. The synthesized compounds were only moderately active, with IC50 in the micromolar range. The compound with the highest affinity for 5-HT4 receptor was tested for the enhancement of intestinal transit rate but was inactive at the oral dose of 100 mg/kg.
Animals; Mice, Inbred ICR; Guinea Pigs; Brain Chemistry; Receptors, Serotonin; Mice; Quinolizines; Receptors, Serotonin, 5-HT4; Receptors, Serotonin, 5-HT3; Magnetic Resonance Spectroscopy; Spectrophotometry, Infrared; Rats, Inbred Strains; Benzimidazoles; Rats; Serotonin Agents; Binding, Competitive; Gastrointestinal Transit; Ligands; Male
Settore CHIM/08 - Chimica Farmaceutica
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/181698
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