Abstract
Sigma receptors have been implicated in a myriad of cellular functions, biological processes and diseases. While the precise biological functions of sigma receptors have not been elucidated, recent work has shed some light on to these enigmatic systems. Sigma receptors have recently been a target of drug development related to psychiatric and neurological disorders. Sigma ligands have also been shown to modulate endothelial cell proliferation and can control angiogenesis which makes them a promising target for oncology applications. Other areas currently being investigated include treatment of gastrointestinal, cardiovascular, endocrine and immune system disorders. Of interest is that the human sigma-1 receptor gene contains a steroid binding component, and several gonadal steroids, including progesterone, testosterone and dehydroepiandrosterone (DHEA), interact with sigma-1 receptors. Of the steroids examined thus far, progesterone binds with the highest affinity to human sigma-1 receptors, with a reported affinity (Ki) as high as 30 nM while the other steroids exhibit lower affinity. For this and other reasons, sigma-1 receptors have been proposed as a link between the central nervous system and the endocrine and reproductive systems. Taken together, the above information highlights an important yet largely unexplored but promising area of research to examine the biological function and therapeutic potential of sigma receptors. This review provides an overview of the current knowledge of these sites with a focus on specific areas where in vivo sigma receptor imaging is currently being investigated.
Keywords: Sigma Receptors, PET, SPECT, Drug Development, Radiotracer, Radioligand
Current Pharmaceutical Design
Title: Imaging Sigma Receptors: Applications in Drug Development
Volume: 13 Issue: 1
Author(s): Thomas Lee Collier, Rikki N. Waterhouse and Michael Kassiou
Affiliation:
Keywords: Sigma Receptors, PET, SPECT, Drug Development, Radiotracer, Radioligand
Abstract: Sigma receptors have been implicated in a myriad of cellular functions, biological processes and diseases. While the precise biological functions of sigma receptors have not been elucidated, recent work has shed some light on to these enigmatic systems. Sigma receptors have recently been a target of drug development related to psychiatric and neurological disorders. Sigma ligands have also been shown to modulate endothelial cell proliferation and can control angiogenesis which makes them a promising target for oncology applications. Other areas currently being investigated include treatment of gastrointestinal, cardiovascular, endocrine and immune system disorders. Of interest is that the human sigma-1 receptor gene contains a steroid binding component, and several gonadal steroids, including progesterone, testosterone and dehydroepiandrosterone (DHEA), interact with sigma-1 receptors. Of the steroids examined thus far, progesterone binds with the highest affinity to human sigma-1 receptors, with a reported affinity (Ki) as high as 30 nM while the other steroids exhibit lower affinity. For this and other reasons, sigma-1 receptors have been proposed as a link between the central nervous system and the endocrine and reproductive systems. Taken together, the above information highlights an important yet largely unexplored but promising area of research to examine the biological function and therapeutic potential of sigma receptors. This review provides an overview of the current knowledge of these sites with a focus on specific areas where in vivo sigma receptor imaging is currently being investigated.
Export Options
About this article
Cite this article as:
Lee Collier Thomas, Waterhouse N. Rikki and Kassiou Michael, Imaging Sigma Receptors: Applications in Drug Development, Current Pharmaceutical Design 2007; 13 (1) . https://dx.doi.org/10.2174/138161207779313740
DOI https://dx.doi.org/10.2174/138161207779313740 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
The “Big Five” Phytochemicals Targeting Cancer Stem Cells: Curcumin, EGCG, Sulforaphane, Resveratrol and Genistein
Current Medicinal Chemistry Tolerance Induction by Gene Transfer to Lymphocytes
Current Gene Therapy Converging Pathways in the Occurrence of Endoplasmic Reticulum (ER) Stress in Huntingtons Disease
Current Molecular Medicine Sodium Glucose Cotransporter-2 Inhibitor Treatment and the Risk of Diabetic Ketoacidosis in Denmark: A Retrospective Cohort Study of Five Years of Use
Current Drug Safety Competency of Prefilled Insulin Pen Usage Among Diabetes Patients in Saudi Arabia: A Cross-sectional Study
Current Diabetes Reviews Targeted Anti-leukemic Therapy as Disease-stabilizing Treatment for Acute Myeloid Leukemia Relapse after Allogeneic Stem Cell Transplantation: Will it be Possible to Combine these Strategies with Retransplantation or Donor Lymphocyte Infusions?
Current Cancer Drug Targets Prognostic Significance of Hypertriglyceridemia in Patients at High and Very High Cardiovascular Risk Depending on the Concentration of Highsensitivity C-reactive Protein
Endocrine, Metabolic & Immune Disorders - Drug Targets Protein Tyrosine Phosphatases, New Targets for Cancer Therapy
Current Cancer Drug Targets Molecularly Imprinted Polymer of Colocynthin, An Effective Tool for Quality Control of <i>Citrullus colocynthis</i> Extracts
Current Drug Discovery Technologies Therapeutic Targeting of Epigenetic Components in Amyotrophic Lateral Sclerosis (ALS)
Current Medicinal Chemistry A Novel Combined Pharmacophore Mapping and Quantitative Structure Selectivity Relationship Analysis for the Development of Potent and Selective Human Aldose Reductase Inhibitors
Current Computer-Aided Drug Design Myocardial Insulin Resistance and Cardiac Complications of Diabetes
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Targeting Protein Tyrosine Phosphatases for Anticancer Drug Discovery
Current Pharmaceutical Design Somatostatin and its Analogs
Current Drug Targets Chemical Senses Affecting Cough and Swallowing
Current Pharmaceutical Design Anti-diabetic Activity of Rosmarinic Acid Rich Fractions from Orthosiphon stamineus
Current Enzyme Inhibition Selective Thyroid Hormone Receptor Modulators
Current Topics in Medicinal Chemistry Aging and DNA Methylation
Current Chemical Biology Peroxisome Proliferator-Activated Receptors as New Molecular Targets in Psoriasis
Current Drug Targets - Inflammation & Allergy Synthesis, Molecular Docking and PTP1B Inhibitory Activity of Functionalized 4,5-Dihydronaphthofurans and Dibenzofurans
Medicinal Chemistry