Morphine sulfate (MS) stimulates mesangial cell (MC) proliferation, a process central to development of glomerular disease. The purpose of this study was to examine whether specific opioid receptors (OR) and signal transducer and activators of transcription 3 (STAT3) signaling are associated with MS-induced MC proliferation. C57Bl/6J and OR-specific knockout (KO) mice were treated for up to 6 w...

Exposure to stress is associated with adverse emotional and behavioral responses. Whereas the κ-opioid receptor (KOR) system is known to mediate some of the effects, it is unclear whether and how stress affects epigenetic regulation of this gene. Because the KOR gene can use two promoters (Pr1 and Pr2) and two polyadenylation signals (PA1 and PA2), it is also interesting whether and how these d...

Genetic and pharmacological approaches were used to examine kappa-opioid receptor (KOR-1) regulation of dopamine (DA) dynamics in the nucleus accumbens and vulnerability to cocaine. Microdialysis revealed that basal DA release and DA extraction fraction (Ed), an indirect measure of DA uptake, are enhanced in KOR-1 knock-out mice. Analysis of DA uptake revealed a decreased Km but unchanged Vmax ...

mu-, delta- and kappa-opioid receptors are widely expressed in the central nervous system where they mediate the strong analgesic and mood-altering actions of opioids, and modulate numerous endogenous functions. To investigate the contribution of the kappa-opioid receptor (KOR) to opioid function in vivo, we have generated KOR-deficient mice by gene targeting. We show that absence of KOR does n...

The purpose of the study was to compare the binding energy of pharmacophores of different classes targeting to kappa opioid receptor (KOR) with ketazocine and pentazocine which are having good activity on the KOR. The 3D structure of KOR receptor was built by Homology modeling; pharmacophores were characterized by using Ligand scout. Docking studies for the KOR agonists were performed in Autodo...

abstract in current study, an irrigation examination and acquisition of environmental water in kor-river fields, that is dominated from doroudzan dam to bakhtegan lake, was done by an integrated economy-environmental model. the model was considered by economic, hydrologic and agronomic components. in the economic component, an optimal harvesting of water was done using non-linear programming in...

In opioid signaling in the brain and -opioid receptors (MOR and KOR) are like the yin and yang principles in Chinese philosophy, they always act as an opposing pair. The antagonistic interactions between MOR and KOR are widespread in the CNS. In few receptor families, two closely related members with such overlapping expression in the brain produce such opposite behavioral effects. In humans, M...

The macrocyclic tetrapeptide natural product CJ-15,208 (cyclo[Phe-d-Pro-Phe-Trp]) exhibited both dose-dependent antinociception and kappa opioid receptor (KOR) antagonist activity after oral administration. CJ-15,208 antagonized a centrally administered KOR selective agonist, providing strong evidence it crosses the blood-brain barrier to reach KOR in the CNS. Orally administered CJ-15,208 also...

Cocaine abuse has been implicated as a cofactor in human immunodeficiency virus (HIV)-1-associated dementia (HAD). In this study, we tested the hypothesis that exposure of microglial cells, the resident macrophages of the brain, to cocaine would potentiate HIV-1 expression. Because kappa-opioid receptor (KOR) agonists have been shown to suppress neurochemical and neurobehavioral responses to co...