2-Phenethylbenzimidazole, 2-phenethylbenzoxazole and 2- phenethylbenzothiazole derivatives were synthesized to explore the structural features of the serotonin 5-HT2B receptor antagonists. Those molecules were designed to recognize the 5-HT2B receptor and to discriminate it from the 5-HT2A and 5-HT2c subtypes. All compounds were characterized by binding affinity determination for 5-HT 2A and 5-HT2c subtypes and antagonistic activity for 5-HT2B receptor in rat stomach fundus. None of the new compounds showed affinity for 5-HT2A and 5-HT2c subtypes, but some of them displayed antagonistic activity in rat stomach fundus at micromolar concentrations. © Birkhäuser Boston 2005.
Benzimidazole, benzoxazole and benzothiazole derivatives as 5HT 2B receptor ligands. Synthesis and preliminary pharmacological evaluation
SINISCALCHI, Anna;
2005
Abstract
2-Phenethylbenzimidazole, 2-phenethylbenzoxazole and 2- phenethylbenzothiazole derivatives were synthesized to explore the structural features of the serotonin 5-HT2B receptor antagonists. Those molecules were designed to recognize the 5-HT2B receptor and to discriminate it from the 5-HT2A and 5-HT2c subtypes. All compounds were characterized by binding affinity determination for 5-HT 2A and 5-HT2c subtypes and antagonistic activity for 5-HT2B receptor in rat stomach fundus. None of the new compounds showed affinity for 5-HT2A and 5-HT2c subtypes, but some of them displayed antagonistic activity in rat stomach fundus at micromolar concentrations. © Birkhäuser Boston 2005.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
