Background Opioid receptors belong to the rhodopsin subclass within the superfamily of G protein-coupled receptors (GPCR), which are characterized by the presence of seven transmembrane (7TM) helices. They interact with morphine and related opioid alkaloids as well as with endogenous opioid peptides. There are three main types of opioid receptors (μ, δ, ), which are differently implicated in op...

We have examined the endocytic trafficking of epitope-tagged delta and mu opioid receptors expressed in human embryonic kidney (HEK) 293 cells. These receptors are activated by peptide agonists (enkephalins) as well as by the alkaloid agonist drugs etorphine and morphine. Enkephalins and etorphine cause opioid receptors to internalize rapidly (t1/2 approximately 6 min) by a mechanism similar to...

Opioid agonistic and antagonistic peptides which are inactive within the sequence of the precursor milk proteins can be released and thus activated by enzymatic proteolysis, for example during gastrointestinal digestion or during food processing. Activated opioid peptides are potential modulators of various regulatory processes in the body. Opioid peptides can interact with subepithelial opioid...

Tricyclic antidepressants (TCAs) have been reported to interact with the opioid system, but their pharmacological activity at opioid receptors has not yet been elucidated. In the present study, we investigated the actions of amoxapine, amitriptyline, nortriptyline, desipramine, and imipramine at distinct cloned and native opioid receptors. In Chinese hamster ovary (CHO) cells expressing delta-o...

In this study, the effects of subcutaneous (SC) injection of pilocarpine (a cholinomimetic agent) and atropine (a muscarinic receptors antagonist) were investigated on a tonic model of orofacial pain in rats. The contribution of the endogenous analgesic opioid system was assessed using naloxone (an opioid receptors antagonist). Tonic orofacial pain was induced by SC injection of a diluted forma...

In experiments to evaluate responses to the activation of cerebral delta-opioid receptors, repeated daily injection of the selective delta-opioid agonist Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 ([D-Ala2]deltorphin II) into rat brain resulted in the development of tolerance, whereas repeated daily injection or continuous infusion of morphine resulted in sensitization to the behavioral activating effec...

Activation of micro-opioid receptors makes animals hyperphagic and increases their preference for a high-fat diet. Previous studies have suggested that this receptor population plays a role in mediating the hyperphagia that is associated with food deprivation. In this paper, we tested the hypothesis that food deprivation will increase the expression of micro-opioid receptors in the ventral medi...

objective(s): morphine dependence (md) potently protects heart against ischemia reperfusion (ir) injury through specific signaling mechanisms, which are different from the pathways involved in acute morphine treatment or classical preconditioning. since opioid receptor density changes post cerebral ischemia strongly correlated with brain histological damage, in the present study, we tried to el...

The present study investigated the effects of intra-dentate gyrus microinjection of naloxone (an opioid antagonist) and thioperamide (an antagonist of histamine H3 receptors) in the formalin test in rats. Subcutaneous injection of formalin (50 μl, 2.5 %) in the ventral surface of right hind paw produced a biphasic pattern (first phase: 0-5 min and second phase: 15 - 60 min) of licking/biting an...

The purpose of the current study is to investigate the effect of opioid-independent, heterologous activation of protein kinase C (PKC) on the responsiveness of opioid receptor and the underlying molecular mechanisms. Our result showed that removing the C terminus of d opioid receptor (DOR) containing six Ser/Thr residues abolished both DPDPEand phorbol 12-myristate 13acetate (PMA)-induced DOR p...