Abstract
Inhibition of serotonin (5-HT) reuptake has been a central theme in the therapy of depression for half a century. Through the years these therapies have improved, particularly with regard to side effects, and todays selective serotonin reuptake inhibitors (SSRIs) constitute a reasonably effective offer for the patients. However, there is still room for major improvement and considering that almost 20%of the population in the western world will experience a depressive period in their lifetime, there is a large need for improved therapies. A large spectrum of targets and strategies are currently being pursued, but so far none of these new approaches have been successful, mainly due to lack of a deeper understanding of the disease biology. Since inhibition of 5-HT reuptake ensures a certain degree of antidepressant efficacy, there has been a large interest in various combinations with serotonin reuptake inhibitors (SRIs) in order to improve on the shortcomings of treatment with SSRIs. Some of these approaches have resulted in marketed antidepressants, eg combinations of SRI with norepinephrine (NE) reuptake inhibition, whereas other approaches are still at an experimental stage. This review attempts to present the current status of these add-on/combination approaches with particular focus on the medicinal chemistry aspects.
Keywords: Serotonin, norepinephrine, dopamine, SERT, DAT, NET, SSRI, 5-HT1A, 5-HT2C, 5-HT2A
Current Topics in Medicinal Chemistry
Title: Serotonin Reuptake Inhibitors: The Corner Stone in Treatment of Depression for Half a Century – A Medicinal Chemistry Survey
Volume: 6 Issue: 17
Author(s): Ejner K. Moltzen and Benny Bang-Andersen
Affiliation:
Keywords: Serotonin, norepinephrine, dopamine, SERT, DAT, NET, SSRI, 5-HT1A, 5-HT2C, 5-HT2A
Abstract: Inhibition of serotonin (5-HT) reuptake has been a central theme in the therapy of depression for half a century. Through the years these therapies have improved, particularly with regard to side effects, and todays selective serotonin reuptake inhibitors (SSRIs) constitute a reasonably effective offer for the patients. However, there is still room for major improvement and considering that almost 20%of the population in the western world will experience a depressive period in their lifetime, there is a large need for improved therapies. A large spectrum of targets and strategies are currently being pursued, but so far none of these new approaches have been successful, mainly due to lack of a deeper understanding of the disease biology. Since inhibition of 5-HT reuptake ensures a certain degree of antidepressant efficacy, there has been a large interest in various combinations with serotonin reuptake inhibitors (SRIs) in order to improve on the shortcomings of treatment with SSRIs. Some of these approaches have resulted in marketed antidepressants, eg combinations of SRI with norepinephrine (NE) reuptake inhibition, whereas other approaches are still at an experimental stage. This review attempts to present the current status of these add-on/combination approaches with particular focus on the medicinal chemistry aspects.
Export Options
About this article
Cite this article as:
Moltzen K. Ejner and Bang-Andersen Benny, Serotonin Reuptake Inhibitors: The Corner Stone in Treatment of Depression for Half a Century – A Medicinal Chemistry Survey, Current Topics in Medicinal Chemistry 2006; 6 (17) . https://dx.doi.org/10.2174/156802606778249810
DOI https://dx.doi.org/10.2174/156802606778249810 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Current Therapy and Computational Drug Designing Approaches for Neurodegenerative Diseases -with Focus on Alzheimer’s and Parkinson’s.
Current Signal Transduction Therapy Aminochrome as New Preclinical Model to Find New Pharmacological Treatment that Stop the Development of Parkinson’s Disease
Current Medicinal Chemistry Gene Frequency of <i>CYP2D6*4</i> and <i>*10</i> Variants in Karachi Population
Current Pharmacogenomics and Personalized Medicine 5'-Nucleotidases, Nucleosides and their Distribution in the Brain: Pathological and Therapeutic Implications
Current Medicinal Chemistry Central Nervous System Depressants and Risk of Hospitalization due to Community-Acquired Pneumonia in very Old Patients
Current Drug Safety Antipsychotics in Obsessive-Compulsive Disorder
Current Psychiatry Reviews HTR2A Gene Variants and Psychiatric Disorders: A Review of Current Literature and Selection of SNPs for Future Studies
Current Medicinal Chemistry L-DOPA and Serotonergic Neurons: Functional Implication and Therapeutic Perspectives in Parkinson's Disease
Central Nervous System Agents in Medicinal Chemistry Pharmacological Treatments for Attention-Deficit/Hyperactivity Disorder (ADHD) in Adults
Current Psychiatry Reviews Application of Current Diagnostic Criteria for Arrhythmogenic Right Ventricular Cardiomyopathy in Every Day Clinical Practice
Current Pharmaceutical Design Borna Disease Virus (BDV): Neuropharmacological Effects of a CNS Viral Infection
Current Neuropharmacology Induced Pluripotent Stem Cell-Based Studies of Parkinson's Disease: Challenges and Promises
CNS & Neurological Disorders - Drug Targets Levodopa Therapy for Parkinson's Disease: History, Current Status and Perspectives
CNS & Neurological Disorders - Drug Targets Glutamate mGlu5-Adenosine A2A-Dopamine D2 Receptor Interactions in the Striatum. Implications for Drug Therapy in Neuro-psychiatric Disorders and Drug Abuse
Current Medicinal Chemistry - Central Nervous System Agents Oestrogen-A Protective Factor in Schizophrenia?
Current Psychiatry Reviews Randomized Placebo-Controlled Trials of Omega-3 Polyunsaturated Fatty Acids in Psychiatric Disorders: A Review of the Current Literature
Current Drug Discovery Technologies Comparison of Mono-dopaminergic and Multi-target Pharmacotherapies in Primary Parkinson Syndrome and Assessment Tools to Evaluate Motor and Non-motor Symptoms
Current Drug Therapy Artificial Neural Network (ANN) Based Modelling for D1 Like and D2 Like Dopamine Receptor Affinity and Selectivity
Medicinal Chemistry GABAB Receptors as Potential Therapeutic Targets
Current Drug Targets - CNS & Neurological Disorders The Applications of Pharmacogenomics to Neurological Disorders
Current Molecular Medicine