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
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
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
Establishment of Cell-Based Neuroglobin Promoter Reporter Assay for Neuroprotective Compounds Screening
CNS & Neurological Disorders - Drug Targets Hypocholesterolemia
Current Vascular Pharmacology Bioactive Cyclohexenones: A Mini Review
Current Bioactive Compounds Methotrexate-Induced Pneumonitis: Heterogeneity of Bronchoalveolar Lavage and Differences between Cancer and Rheumatoid Arthritis
Inflammation & Allergy - Drug Targets (Discontinued) The Therapeutic Potential of the Wnt Signaling Pathway in Bone Disorders
Current Molecular Pharmacology Neuroimaging Studies of Acute Effects of THC and CBD in Humans and Animals: a Systematic Review
Current Pharmaceutical Design Molecular Mechanisms Determining Opposed Functional States of Microglia
Current Neuropharmacology Is Galanin a Promising Therapeutic Resource for Neural and Nonneural Diseases?
Current Drug Targets Study of Protein Amyloid-Like Aggregates by Solid-State Circular Dichroism Spectroscopy
Current Protein & Peptide Science Theoretical Study of Monoamine Oxidase B Inhibitors as Drug Candidates for Treatment of Parkinson’s Disease
Central Nervous System Agents in Medicinal Chemistry Predicting Progression from Cognitive Impairment to Alzheimer’s Disease with the Disease State Index
Current Alzheimer Research Molecular Approach to Targeted Therapy for Multiple Sclerosis
CNS & Neurological Disorders - Drug Targets The Economic Translation of Paradigm-Changing Innovation: A Short History of Biotechnology
Technology Transfer and Entrepreneurship (Discontinued) Vitamin D in Acute Kidney Injury
Inflammation & Allergy - Drug Targets (Discontinued) Natural Products as Promising Drug Candidates for the Treatment of Alzheimer’s Disease: Molecular Mechanism Aspect
Current Neuropharmacology New Trends in the Development of Oral Antidiabetic Drugs
Current Medicinal Chemistry Anesthetics Act in Quantum Channels in Brain Microtubules to Prevent Consciousness
Current Topics in Medicinal Chemistry Exosomes: The Messengers of Health and Disease
Current Neuropharmacology Kaiso Protein in the Regulation of Brain and Behavior
Current Protein & Peptide Science Non-Suicidal Self-Injury in an Adolescent: A Case Report and Discussion of Treatment
Adolescent Psychiatry