Mu opioid receptor regulation and opiate responsiveness
Journal Title: The AAPS Journal - Year 2005, Vol 7, Issue 3
Abstract
Opiate drugs such as morphine are well known for their ability to produce potent analgesia as well as such unwanted side effects as tolerance, physical dependence, respiratory suppression and constipation. Opiates act at opioid receptors, which belong to the family of G protein-coupled receptors. The mechanisms governing mu opioid receptor (μOR) regulation are of particular interest since morphine and other clinically important analgesics produce their pharmacological effects through this receptor. Here we review recent advances in understanding how opioid receptor regulation can impart differential agonist efficacy produced in vivo.
Authors and Affiliations
Kirsten M. Raehal, Laura M. Bohn
Keywords
Related Articles
- EP ID EP681892
- DOI 10.1208/aapsj070360
- Views 59
- Downloads 0
Evaluating and Reporting the Immunogenicity Impacts for Biological Products—a Clinical Pharmacology Perspective
Immunogenicity assessment is important for biological products due to potential impacts of immunogenicity on safety and efficacy. We reviewed the prescribing information and the FDA’s clinical pharmacology review...
Neural retina limits the nonviral gene transfer to retinal pigment epithelium in an in vitro bovine eye model
We investigated the permeation of liposomal and polymeric gene delivery systems through neural retina into retinal pigment epithelium (RPE) and determined the roles of various factors in permeation and subsequent uptake...
Antibody Drug Conjugates: Preclinical Considerations
The development path for antibody drug conjugates (ADCs) is more complex and challenging than for unmodified antibodies. While many of the preclinical considerations for both unmodified and antibody drug conjugates are s...
Evaluation of the Microcentrifuge Dissolution Method as a Tool for Spray-Dried Dispersion
Although using spray-dried dispersions (SDDs) to improve the bioavailability of poorly water-soluble compounds has become a common practice in supporting the early phases of clinical studies, their performance evaluation...
Pharmacokinetics in mice implanted with xenografted tumors after intravenous administration of tasidotin (ILX651) or its carboxylate metabolite
The pharmacokinetics of tasidotin (ILX651), a depsipeptide currently in phase II for the treatment of advanced solid tumors, and tasidotin-C-carboxylate, the main metabolite, were characterized in male nude mice implante...