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.
|Titolo:||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|
SPARATORE, ANNA CONCETTINA (Primo)
|Parole Chiave:||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 Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
|Data di pubblicazione:||30-apr-1999|
|Digital Object Identifier (DOI):||10.1016/S0014-827X(99)00025-7|
|Appare nelle tipologie:||01 - Articolo su periodico|