Abstract
Among serotonin receptors (5-HTRs), the 5-HT4 subtype is of considerable interest because it is involved in (patho)physiological processes both in peripheral and central nervous systems. In addition to the clinical use of 5-HT4R agonists in the treatment of gastrointestinal motility disorders, the potential use of antagonists in the treatment of irritable bowel syndrome, arrhythmias and micturition disturbances are currently under investigation. This article will review the development of the most important classes of 5- HT4R antagonists with an emphasis on benzimidazole derivatives, their structure-affinity relationships, ligand-receptor interactions and pharmacological applications.
Keywords: 5-HT4 Receptor Antagonists, Benzamides
Current Topics in Medicinal Chemistry
Title: 5-HT4 Receptor Antagonists: Structure-Affinity Relationships and Ligand- Receptor Interactions
Volume: 2 Issue: 6
Author(s): M. L. Lopez-Rodriguez, B. Benhamu, M. J. Morcillo, M. Murcia, A. Viso, M. Campillo and L. Pardo
Affiliation:
Keywords: 5-HT4 Receptor Antagonists, Benzamides
Abstract: Among serotonin receptors (5-HTRs), the 5-HT4 subtype is of considerable interest because it is involved in (patho)physiological processes both in peripheral and central nervous systems. In addition to the clinical use of 5-HT4R agonists in the treatment of gastrointestinal motility disorders, the potential use of antagonists in the treatment of irritable bowel syndrome, arrhythmias and micturition disturbances are currently under investigation. This article will review the development of the most important classes of 5- HT4R antagonists with an emphasis on benzimidazole derivatives, their structure-affinity relationships, ligand-receptor interactions and pharmacological applications.
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Cite this article as:
Lopez-Rodriguez L. M., Benhamu B., Morcillo J. M., Murcia M., Viso A., Campillo M. and Pardo L., 5-HT4 Receptor Antagonists: Structure-Affinity Relationships and Ligand- Receptor Interactions, Current Topics in Medicinal Chemistry 2002; 2 (6) . https://dx.doi.org/10.2174/1568026023393769
DOI https://dx.doi.org/10.2174/1568026023393769 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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