DESIGN AND SYNTHESIS OF A PIPERAZINE DERIVATIVE AS A HIGH AFFINITY 5-HTIA RECEPTOR LIGAND

Document Type : Original Article

Author

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt

Abstract

Serotonin (5-HT) 1A receptors have been shown to have physiological, biochemical pharmacological and clinical values. The piperazino derivative 1 was rationally designed as a bulky, lipophilic N4-substituted arylpiperazine. Radioligand binding assay of 1 at 5-HT1A receptors indicates that it binds at these receptors with higher affinity than the famous 5-HT1A, ligand, buspirone (Ki = 15 nM). Buspirone is currently used to treat anxiety.