Abstract
Methods for addressing sigma receptor affinity and activity have been explored and although several protocols have been employed, only few procedures resulted reliable. Sigma-1 receptor affinity protocol using guinea-pig brain and (+)-[3H]-pentazocine and sigma-2 receptor affinity protocol employing rat liver and [3H]-DTG are usually reported by authors as standard procedures. By contrast, the intrinsic activity evaluation of sigma ligands has been performed in several manners: tumor cell lines, isolated organ bath, in vivo animal model. The last is not considered in the present paper because this method studied the physiological role of sigma receptors. The studies carried out in tumor cell lines involved the role of sigma receptors in tumors progression while, although isolated organ bath experiment employed physiological samples, the pharmacokinetic properties of ligands, a strictly requirement for the in vivo assays, did not affect the pharmacodynamic properties of tested compounds. The advances in the above mentioned assays have been reported.
Keywords: Sigma-1 receptors, sigma-2 receptors, sigma receptor agonists and antagonists, autophagy
Central Nervous System Agents in Medicinal Chemistry
Title: In Vitro and Ex Vivo Characterization of Sigma-1 and Sigma-2 Receptors: Agonists and Antagonists in Biological Assays
Volume: 9 Issue: 3
Author(s): Nicola Antonio Colabufo, Marialessandra Contino, Carmela Inglese, Mauro Niso, Roberto Perrone, Sante Roperto and Franco Roperto
Affiliation:
Keywords: Sigma-1 receptors, sigma-2 receptors, sigma receptor agonists and antagonists, autophagy
Abstract: Methods for addressing sigma receptor affinity and activity have been explored and although several protocols have been employed, only few procedures resulted reliable. Sigma-1 receptor affinity protocol using guinea-pig brain and (+)-[3H]-pentazocine and sigma-2 receptor affinity protocol employing rat liver and [3H]-DTG are usually reported by authors as standard procedures. By contrast, the intrinsic activity evaluation of sigma ligands has been performed in several manners: tumor cell lines, isolated organ bath, in vivo animal model. The last is not considered in the present paper because this method studied the physiological role of sigma receptors. The studies carried out in tumor cell lines involved the role of sigma receptors in tumors progression while, although isolated organ bath experiment employed physiological samples, the pharmacokinetic properties of ligands, a strictly requirement for the in vivo assays, did not affect the pharmacodynamic properties of tested compounds. The advances in the above mentioned assays have been reported.
Export Options
About this article
Cite this article as:
Colabufo Antonio Nicola, Contino Marialessandra, Inglese Carmela, Niso Mauro, Perrone Roberto, Roperto Sante and Roperto Franco, In Vitro and Ex Vivo Characterization of Sigma-1 and Sigma-2 Receptors: Agonists and Antagonists in Biological Assays, Central Nervous System Agents in Medicinal Chemistry 2009; 9 (3) . https://dx.doi.org/10.2174/1871524910909030161
DOI https://dx.doi.org/10.2174/1871524910909030161 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
- 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
-
Correlation of Alzheimer-like Tau Hyperphosphorylation and fMRI Bold Intensity
Current Alzheimer Research Calpains: Attractive Targets for the Development of Synthetic Inhibitors
Current Topics in Medicinal Chemistry Application of In Vivo Animal Models to Characterize the Pharmacokinetic and Pharmacodynamic Properties of Drug Candidates in Discovery Settings
Combinatorial Chemistry & High Throughput Screening Visual Sexual Stimulation and Erection, a Brief Review with New fMRI Data
Current Medicinal Chemistry Molecular Mechanisms in Rheumatic Diseases: Rationale for Novel Drug Development – Introduction
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Animal Models of Depressive Illness: The Importance of Chronic Drug Treatment
Current Pharmaceutical Design The Interaction of Zinc Oxide/Green Tea Extract Complex Nanoparticles and its Effect on Monosodium Glutamate Toxicity in Liver of Rats
Current Pharmaceutical Biotechnology Development of Platform Technology for Oral Controlled Delivery of Highly Water Soluble Drugs Using Milnacipran HCl as a Model Drug
Drug Delivery Letters Hypertension in Pregnancy: Clinical Manifestations and Treatment
Current Hypertension Reviews Brain Senescence and Neuroprotective Dietary Components
Central Nervous System Agents in Medicinal Chemistry Exploiting Anti-Inflammation Effects of Flavonoids in Chronic Inflammatory Diseases
Current Pharmaceutical Design Clinical Applications of Autoimmunity to Citrullinated Proteins in Rheumatoid Arthritis, from Improving Diagnostics to Future Therapies
Recent Patents on Inflammation & Allergy Drug Discovery Molecular Biology of T-Type Calcium Channels
CNS & Neurological Disorders - Drug Targets Fc-fusion Proteins in Therapy: An Updated View
Current Medicinal Chemistry Intracranial Atherosclerotic Stenosis is Related to Post-stroke Cognitive Impairment: A Cross-sectional Study of Minor Stroke
Current Alzheimer Research Interleukin-7: a key Mediator in T Cell-driven Autoimmunity, Inflammation, and Tissue Destruction
Current Pharmaceutical Design Lab-on-Chip for Pharmacogenomics: An Embedded System Organization
Micro and Nanosystems Modulation of the Cannabinoid System: A New Perspective for the Treatment of the Alzheimer’s Disease
Current Neuropharmacology Cellular Functions of RNA-Binding Motif Protein 3 (RBM3): Clues in Hypothermia, Cancer Biology and Apoptosis
Protein & Peptide Letters Urinary Albumin to Creatinine Ratio as Potential Biomarker for Cerebral Microvascular Disease
Current Neurovascular Research