Showing 1-30 of 37 results for "U103"
Bing Cao et al.
Molecular brain, 5, 19-19 (2012-06-12)
Pain contains both sensory and affective dimensions. Using a rodent visceral pain assay that combines the colorectal distension (CRD) model with the conditioned place avoidance (CPA) paradigms, we measured a learned behavior that directly reflects the affective component of visceral...
Lisa E Baker et al.
Psychopharmacology, 203(2), 203-211 (2009-01-21)
Research interests regarding the psychopharmacology of salvinorin A have been motivated by the recreational use and widespread media focus on the hallucinogenic plant, Salvia divinorum. Additionally, kappa opioid (KOP) receptor ligands may have therapeutic potential in the treatment of some...
Sarah A Kissiwaa et al.
British journal of pharmacology, 177(2), 420-431 (2019-10-10)
Pain is a subjective experience involving sensory discriminative and emotionally aversive components. Consistent with its role in pain processing and emotions, the amygdala modulates the aversive component of pain. The laterocapsular region of the central nucleus of the amygdala (CeLC)...
Xu Zhang et al.
Behavioural brain research, 236(1), 8-15 (2012-09-04)
Within a biopsychosocial model of pain, pain is seen as a conscious experience modulated by mental, emotional and sensory mechanisms. Recently, using a rodent visceral pain assay that combines the colorectal distension (CRD) model with the conditioned place avoidance (CPA)...
A P Piras et al.
Neuroscience, 169(2), 751-757 (2010-05-11)
There is evidence that the kappa opioid system plays an important role in cocaine addiction and that chronic cocaine administration and withdrawal from chronic cocaine alter kappa opioid receptor (KOPr) density. The present study employed in situ [(35)S]guanosine 5'-O-[gamma-thio]triphosphate acid...
Reagan L Pennock et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 31(1), 281-288 (2011-01-07)
Hypothalamic proopiomelanocortin (POMC) neurons release the endogenous opioid beta-endorphin and POMC neuron activity is inhibited by opioids, leading to the proposal that beta-endorphin acts to provide feedback inhibition. However, both intrinsic properties and synaptic inputs contribute to the regulation of...
Sara M Thomasy et al.
Journal of analytical toxicology, 32(9), 754-759 (2008-11-22)
This study evaluated the validity of measuring fentanyl concentrations in equine plasma using radioimmunoassay (RIA) by comparing it to the established technique of liquid chromatography-mass spectrometry (LC-MS). Equine plasma samples were analyzed using a solid-phase Coat-A-Count fentanyl RIA and a...
Kristina Cechova et al.
Journal of neuroimmunology, 321, 12-23 (2018-06-30)
Regulation of μ-, δ- and κ-opioid receptor protein level in spleen lymphocytes when stimulated by mitogen is not known. To answer the question whether these cells do express opioid receptor (OR) proteins, primary, fresh rat spleen lymphocytes were prepared and...
Kurt K Sladky et al.
American journal of veterinary research, 70(9), 1072-1078 (2009-09-02)
To determine the effects of mu-, delta-, and kappa-opioid receptor (MOR, DOR, and KOR, respectively) activation on thermal antinociception in red-eared slider turtles Trachemys scripta. 51 adult turtles. Infrared heat stimuli were applied to the plantar surface of turtle hind...
Michael A Ansonoff et al.
Frontiers in bioscience (Scholar edition), 2, 772-780 (2009-12-29)
Over the past several years substantial evidence has documented that opioid receptor homo- and heterodimers form in cell lines expressing one or more of the opioid receptors. We used opioid receptor knockout mice to determine whether in vivo pharmacological characteristics...
Aashish S Morani et al.
Pharmacology, biochemistry, and behavior, 94(2), 244-249 (2009-09-15)
Our previous work indicated that pretreatment with the selective kappa-opioid receptor (KOPr) agonist, U69593, attenuated the ability of priming injections of cocaine to reinstate extinguished cocaine-seeking behavior. The present study expanded these initial tests to include other traditional KOPr agonists...
S Schenk et al.
Psychopharmacology, 151(1), 85-90 (2000-08-25)
Results of a previous study indicated that prior administration of the kappa-opioid receptor agonist, U69593, blocked the ability of cocaine to reinstate extinguished cocaine-taking behavior. In order to determine whether the effect of U69593 was specific to cocaine or was...
Zi-long Wang et al.
PloS one, 9(8), e103773-e103773 (2014-08-05)
Neuropeptide FF (NPFF) is known to be an endogenous opioid-modulating peptide. Nevertheless, very few researches focused on the interaction between NPFF and endogenous opioid peptides. In the present study, we have investigated the effects of NPFF system on the supraspinal...
Ajay S Yekkirala et al.
ACS chemical neuroscience, 1(2), 146-154 (2010-02-17)
Research in the opioid field has relied heavily on the use of standard agonist ligands such as morphine, [d-Ala(2)-MePhe(4)-Glyol(5)]enkephalin (DAMGO), U69593, bremazocine, [d-Pen(2)d-Pen(5)]enkephalin (DPDPE), and deltorphin-II as tools for investigating the three major types of opioid receptors, MOP (μ), KOP...
Miriam Stoeber et al.
eLife, 9 (2020-02-26)
G protein-coupled receptors (GPCRs) signal through allostery, and it is increasingly clear that chemically distinct agonists can produce different receptor-based effects. It has been proposed that agonists selectively promote receptors to recruit one cellular interacting partner over another, introducing allosteric...
Kshitij A Patkar et al.
The Journal of pharmacology and experimental therapeutics, 346(3), 545-554 (2013-07-16)
In the mouse 55°C warm-water tail-withdrawal assay, a single administration of nor-binaltorphimine (nor-BNI; 10 mg/kg i.p.) antagonized κ-opioid receptor (KOR) agonist-induced antinociception up to 14 days, whereas naloxone (10 mg/kg i.p.)-mediated antagonism lasted less than 1 day. In saturation binding...
Carmel M McDermott et al.
The Journal of physiology, 589(Pt 14), 3517-3532 (2011-05-25)
The dentate gyrus of the hippocampus is thought to control information flow into the rest of the hippocampus. Under pathological conditions, such as epilepsy, this protective feature is circumvented and uninhibited activity flows throughout the hippocampus. Many factors can modulate...
C A Heidbreder et al.
Neuroreport, 5(14), 1797-1800 (1994-09-08)
Repeated intermittent administration of cocaine (20 mg kg-1, i.p.) for 3 days dramatically increased basal dopamine (DA) overflow in the nucleus accumbens (ACB) 48 h after the final daily injection. This cocaine pretreatment also produced a significant increase in stereotypy...
Ferenc Zádor et al.
Molecules (Basel, Switzerland), 25(6) (2020-03-21)
The present work represents the in vitro (potency, affinity, efficacy) and in vivo (antinociception, constipation) opioid pharmacology of the novel compound 14-methoxycodeine-6-O-sulfate (14-OMeC6SU), compared to the reference compounds codeine-6-O-sulfate (C6SU), codeine and morphine. Based on in vitro tests (mouse and...
S Stevens Negus et al.
Experimental and clinical psychopharmacology, 16(5), 386-399 (2008-10-08)
Micro opioid receptor agonists are clinically valuable as analgesics; however, their use is limited by high abuse liability. Kappa opioid agonists also produce antinociception, but they do not produce micro agonist-like abuse-related effects, suggesting that they may enhance the antinociceptive...
Gregory P McLennan et al.
Journal of neurochemistry, 107(6), 1753-1765 (2008-11-19)
GTP binding regulatory protein (G protein)-coupled receptors can activate MAPK pathways via G protein-dependent and -independent mechanisms. However, the physiological outcomes correlated with the cellular signaling events are not as well characterized. In this study, we examine the involvement of...
Ricardo Mario Arida et al.
Journal of neurochemistry, 132(2), 206-217 (2014-10-21)
Physical exercise stimulates the release of endogenous opioid peptides supposed to be responsible for changes in mood, anxiety, and performance. Exercise alters sensitivity to these effects that modify the efficacy at the opioid receptor. Although there is evidence that relates...
Jason W Hahn et al.
Journal of neurochemistry, 112(6), 1431-1441 (2009-11-10)
As embryonic stem cell-derived neural progenitors (NPs) have the potential to be used in cell replacement therapy, an understanding of the signaling mechanisms that regulate their terminal differentiation is imperative. In previous studies, we discovered the presence of functional mu...
Bassil Hassan et al.
Regional anesthesia and pain medicine, 38(1), 21-27 (2012-12-12)
κ-Opioid receptor (κ-OR) activation is known to play a role in analgesia and central sedation. The purpose of the present study was to examine the effect of the κ-OR agonist, U-50488 (an arylacetamide), on Ca channel currents and the signaling...
S Stevens Negus et al.
Psychopharmacology, 210(2), 149-159 (2010-01-27)
Selective, centrally acting kappa opioid agonists produce antinociception in a wide range of preclinical assays, but these compounds perform poorly as analgesics in humans. This discrepancy may be related to the behavioral depressant effects of kappa agonists. Kappa antagonists do...
A Menozzi et al.
Equine veterinary journal, 44(3), 368-370 (2011-09-03)
The effects of preferential µ (morphine), selective µ (fentanyl), selective κ (compound U69593) opioid receptor agonists, and nonselective (naloxone) and selective µ (naloxonazine) antagonists on equine small intestinal motility were evaluated in vitro. Samples of circular muscle from equine jejunum...
Michael J McCarthy et al.
Psychopharmacology, 210(2), 221-229 (2009-10-07)
The synthesis and release of dynorphin are increased in the caudate/putamen (CPU) and nucleus accumbens (NAc) of nicotine-withdrawn mice, suggesting a role in the nicotine abstinence syndrome. This study aims to investigate the consequences of enhanced dynorphinergic activity on kappa-opioid...
José Antonio Fuentealba et al.
Synapse (New York, N.Y.), 64(12), 898-904 (2010-10-13)
Acute activation of κ-opioid receptors (KOR) decreases dopamine (DA) extracellular levels in both the medial prefrontal cortex (mPFC) and the nucleus accumbens (NAc). Also, the acute activation of KOR prevents alterations in behavior and neurochemistry occurring after repeated use of...
Ferenc Zádor et al.
European journal of pharmacology, 814, 264-273 (2017-09-03)
14-O-methyl (14-O-Me) group in morphine-6-O-sulfate (M6SU) or oxymorphone has been reported to be essential for enhanced affinity, potency and antinociceptive effect of these opioids. Herein we report on the pharmacological properties (potency, affinity and efficacy) of the new compound, 14-O-methylmorphine...
Philemon Kipkemoi Towett et al.
Pharmacology, biochemistry, and behavior, 91(4), 566-572 (2008-10-22)
Data available on the role of the opioid systems of the naked mole-rat in nociception is scanty and unique compared to that of other rodents. In the current study, the effect of DAMGO, DPDPE and U-50488 and U-69593 on formalin-induced...

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