Abstract
Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT 1A subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT 1A R sites. Among these, arylpiperazine derivatives represent one of the most important classes of 5-HT 1A R ligands. This article will review the development of arylpiperazine derivatives acting at 5-HT 1A Rs with an emphasis on structure-affinity relationships of agonists and antagonists, ligand-receptor interactions and pharmacological applications.
Keywords: Arylpiperazine Derivatives, 5-hydroxytryptamine, aryloxyalkylamines and arylpiperazines, Antagonist Pharmacophore, postsynaptic receptor sites, alpha-carbon coordinate
Current Medicinal Chemistry
Title: Arylpiperazine Derivatives Acting at 5-HT1A Receptors
Volume: 9 Issue: 4
Author(s): M. L. Lopez-Rodriguez, D. Ayala, B. Benhamu, M. J. Morcillo and A. Viso
Affiliation:
Keywords: Arylpiperazine Derivatives, 5-hydroxytryptamine, aryloxyalkylamines and arylpiperazines, Antagonist Pharmacophore, postsynaptic receptor sites, alpha-carbon coordinate
Abstract: Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT 1A subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT 1A R sites. Among these, arylpiperazine derivatives represent one of the most important classes of 5-HT 1A R ligands. This article will review the development of arylpiperazine derivatives acting at 5-HT 1A Rs with an emphasis on structure-affinity relationships of agonists and antagonists, ligand-receptor interactions and pharmacological applications.
Export Options
About this article
Cite this article as:
Lopez-Rodriguez L. M., Ayala D., Benhamu B., Morcillo J. M. and Viso A., Arylpiperazine Derivatives Acting at 5-HT1A Receptors, Current Medicinal Chemistry 2002; 9 (4) . https://dx.doi.org/10.2174/0929867023371030
DOI https://dx.doi.org/10.2174/0929867023371030 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Resveratrol: A Therapeutic Approach to Neurodegenerative Diseases and Aging
Mini-Reviews in Organic Chemistry The Human Leukocyte Antigen Class III Haplotype Approach: New Insight in Alzheimer's Disease Inflammation Hypothesis
Current Alzheimer Research Meet Our Regional Editor
Central Nervous System Agents in Medicinal Chemistry Mitochondrial Metabolism Modulation: A New Therapeutic Approach for Parkinsons Disease
CNS & Neurological Disorders - Drug Targets Targeting the BH3 Domain of Bcl-2 Family Proteins. A Brief History From Natural Products to Foldamers As Promising Cancer Therapeutic Avenues
Current Medicinal Chemistry Antioxidant Therapy in Critically Septic Patients
Current Drug Targets Recent Development in Applications of Important Biopolymer Chitosan in Biomedicine, Pharmaceuticals and Personal Care Products
Current Tissue Engineering (Discontinued) Anti-tumor Effects of Curcuminoids in Glioblastoma Multiforme: An Updated Literature Review
Current Medicinal Chemistry Advantages of Structure-Based Drug Design Approaches in Neurological Disorders
Current Neuropharmacology Synthesis of Oligopeptides Through O-acyl Isopeptide Method
Protein & Peptide Letters Drug Interactions between Nine Antifungal Agents and Drugs Metabolized by Human Cytochromes P450
Current Drug Metabolism The Role of Coagulation and Fibrinolysis in the Pathogenesis of Acute Lung Injury
Current Respiratory Medicine Reviews Prodrugs of Non-steroidal Anti-inflammatory Drugs (NSAIDs): A Long March Towards Synthesis of Safer NSAIDs
Mini-Reviews in Medicinal Chemistry Beyond the Obvious: Smoking and Respiratory Infection Implications on Alzheimer's Disease
CNS & Neurological Disorders - Drug Targets Old Weapons for New Wars: Bioactive Molecules From Cnidarian Internal Defense Systems
Central Nervous System Agents in Medicinal Chemistry Effects of the KIBRA Single Nucleotide Polymorphism on Synaptic Plasticity and Memory: A Review of the Literature
Current Neuropharmacology Use of Angiotensin Receptor Blockers and Risk of Alzheimer’s Disease: A Class Effect?
Current Reviews in Clinical and Experimental Pharmacology Tumor-Intrinsic and Tumor-Extrinsic Factors Impacting Hsp90- Targeted Therapy
Current Molecular Medicine Methods for Detection of Speech Impairment Using Mobile Devices
Recent Patents on Signal Processing (Discontinued) Possible Involvement of Advanced Glycation End-Products (AGEs) in the Pathogenesis of Alzheimers Disease
Current Pharmaceutical Design