DESIGN AND SYNTHESIS OF A PIPERAZINE DERIVATIVE AS A HIGH AFFINITY 5-HTIA RECEPTOR LIGAND | ||||
Zagazig Journal of Pharmaceutical Sciences | ||||
Article 9, Volume 2, Issue 2, December 1993, Page 103-110 PDF (3.61 MB) | ||||
Document Type: Original Article | ||||
DOI: 10.21608/zjps.1993.187356 | ||||
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Author | ||||
Mohamed El-Bermawy | ||||
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. | ||||
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