Abstract
The serotonin system exerts its effects on the CNS and many peripheral systems. Of the 14 serotonin receptors, the 5-HT7 receptor is the most recently discovered. The 5-HT7 receptor has been shown to be involved in stress reduction, depression, and nociceptive control. Despite the 20 years since the discovery of 5-HT7R, there are still few truly selective ligands. Two of the common scaffolds for 5-HT7R ligands are long chain arylpiperazines (LCAPs) and sulfonamide containing compounds. This review focuses on recently developed (2014-2016) 5-HT7R ligands, their selectivity for the receptor, and suggests the possible new pharmacophore models for these ligands.
Keywords: Arylpiperazine, CNS, drug design, 5-HT7, pharmacophore, serotonin.
Mini-Reviews in Medicinal Chemistry
Title:Pharmacophore Comparison and Development of Recently Discovered Long Chain Arylpiperazine and Sulfonamide Based 5-HT7 Ligands
Volume: 18 Issue: 7
Author(s): Andrea Rague and Kevin Tidgewell*
Affiliation:
- Division of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, School of Pharmacy, Duquesne University, Pittsburgh, Pennsylvania,United States
Keywords: Arylpiperazine, CNS, drug design, 5-HT7, pharmacophore, serotonin.
Abstract: The serotonin system exerts its effects on the CNS and many peripheral systems. Of the 14 serotonin receptors, the 5-HT7 receptor is the most recently discovered. The 5-HT7 receptor has been shown to be involved in stress reduction, depression, and nociceptive control. Despite the 20 years since the discovery of 5-HT7R, there are still few truly selective ligands. Two of the common scaffolds for 5-HT7R ligands are long chain arylpiperazines (LCAPs) and sulfonamide containing compounds. This review focuses on recently developed (2014-2016) 5-HT7R ligands, their selectivity for the receptor, and suggests the possible new pharmacophore models for these ligands.
Export Options
About this article
Cite this article as:
Rague Andrea and Tidgewell Kevin *, Pharmacophore Comparison and Development of Recently Discovered Long Chain Arylpiperazine and Sulfonamide Based 5-HT7 Ligands, Mini-Reviews in Medicinal Chemistry 2018; 18 (7) . https://dx.doi.org/10.2174/1389557517666170913111533
DOI https://dx.doi.org/10.2174/1389557517666170913111533 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
Related Articles
-
Adenosine and the Auditory System
Current Neuropharmacology Platelet-Derived Secreted Amyloid-Precursor Protein-β as a Marker for Diagnosing Alzheimer’s Disease
Current Neurovascular Research Patient-Controlled Analgesia
Current Drug Targets Meet Our Editorial Board Member
Current Neuropharmacology Current Drug Managements of Wilson’s Disease: From West to East
Current Neuropharmacology Conformation as the Therapeutic Target for Neurodegenerative Diseases
Current Alzheimer Research GABAB Receptors as Potential Therapeutic Targets
Current Drug Targets - CNS & Neurological Disorders Endogenous Cardioprotective Agents: Role in Pre and Postconditioning
Current Drug Targets Patient-Tailored Treatments with Anti-EGFR Monoclonal Antibodies in Advanced Colorectal Cancer: KRAS and Beyond
Current Cancer Drug Targets AVN-322 is a Safe Orally Bio-Available Potent and Highly Selective Antagonist of 5-HT6R with Demonstrated Ability to Improve Impaired Memory in Animal Models
Current Alzheimer Research Left Anterior Temporal Lobe Sustains Naming in Alzheimers Dementia and Mild Cognitive Impairment
Current Alzheimer Research Meet Our Editorial Board Member
Current Molecular Pharmacology Functional Role of Lipoprotein Receptors in Alzheimers Disease
Current Alzheimer Research Synthesis and In Silico Molecular Docking Studies on Substituted Piperic Acid Derivatives as Inhibitors of Bacterial DNA Gyrase
Current Computer-Aided Drug Design Emerging Biologics in the Treatment of Inflammatory Bowel Disease: What is Around the Corner?
Current Drug Targets HIV-1 Integrase Binding to its Cellular Partners: A Perspective from Computational Biology
Current Pharmaceutical Design Mobile Phone Text Message Interventions in Psychiatry - What are the Possibilities?
Current Psychiatry Reviews Editorial: Multi-Target in Computer-Aided Drug Design Studies
Current Drug Targets The Bovine Basic Pancreatic Trypsin Inhibitor (Kunitz Inhibitor): A Milestone Protein
Current Protein & Peptide Science Ocular Biomarkers of Alzheimer’s Disease
Central Nervous System Agents in Medicinal Chemistry