Benzimidazole, Benzoxazole and Benzothiazole Derivatives as 5HT2B Receptor Ligands. Synthesis and Preliminary Pharmacological Evaluation

被引：0
|
作者：
G. Giorgioni
B. Accorroni
A. Di Stefano
G. Marucci
A. Siniscalchi
F. Claudi
机构：
[1] Università di Camerino,Dipartimento di Scienze Chimiche
[2] Università G. D'Annunzio,Dipartimento di Scienze del Farmaco
[3] Università di Ferrara,Dipartimento di Medicina Sperimentale e Clinica, Sezione di Farmacologia
来源：
Medicinal Chemistry Research | 2005年 / 14卷
关键词：
Serotonin; Receptor Antagonist; Structural Feature; Binding Affinity; Benzimidazole;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
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-HT2A 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.
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页码：57 / 73
页数：16
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