Designing Safer Analgesics via μ-Opioid Receptor Pathways

Opioid Analgesics

Intensive research on the neurobiology of pain over the past two decades has revealed many receptors, ion channels and enzymes with potential as novel targets for development of a new generation of analgesic agents. However, despite large investment in preclinical and clinical development of small molecules and biologics as potential novel pain therapeutics, very few have reached the clinic. He...

Evidence of morphine like substance and μ-opioid receptor expression in Toxacara canis (Nematoda: Ascaridae)

Toxocara canis (Nematoda: Ascaridae) is an intestinal nematode parasite of dogs, which can also cause disease in humans. Transmission to humans usually occurs because of direct contact with T. canis eggs present in soil contaminated with the feces of infected dogs. This nematode has extraordinary abilities to survive for many years in different tissues of vertebrates, and deve...

Replacement of Serine363 and Serine375 Codons by Alanine in Rat μ-Opioid Receptor cDNA

     The aim of this study was to use site directed mutagenesis technique to construct a vector in which serine363 and serine375 residues of the COOH-terminal portion of the μ-opioid receptor (MOR) were substituted by alanine. These constructs are essential in studying G-protein coupled receptor kinase-mediated MOR desensiti-zation. The nested PCR carried out for conversio...

Opioid and Nonopioid Analgesics

μ-Opioid receptor desensitization: homologous or heterologous?

There is considerable controversy over whether μ-opioid receptor (MOPr) desensitization is homologous or heterologous and over the mechanisms underlying such desensitization. In different cell types MOPr desensitization has been reported to involve receptor phosphorylation by various kinases, including G-protein-coupled receptor kinases (GRKs), second messenger and other kinases as well as pert...