T0675

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Showing 1-26 of 26 results for "T0675" within Papers

Behavioral consequences of delta-opioid receptor activation in the periaqueductal gray of morphine tolerant rats.

Michael M Morgan et al.

Neural plasticity, 2009, 516328-516328 (2009-03-07)

Chronic morphine administration shifts delta-opioid receptors (DORs) from the cytoplasm to the plasma membrane. Given that microinjection of morphine into the PAG produces antinociception, it is hypothesized that the movement of DORs to the membrane will allow antinociception to the

Comparison with naloxone of two dynorphin A analogues with K- and delta-opioid antagonist activity.

A Capasso

Medicinal chemistry (Shariqah (United Arab Emirates)), 5(1), 1-6 (2009-01-20)

Recently, we have demonstrated that substitution of 1,2,3,4 tetrahyidroisoquinoline-3- carboxylic acid (Tic) in place of Gly2 in dynorphin A-(1-13)-NH2 (DYN) analogue (A) decreased the affinity to the kappa, delta, and micro receptors, and kappa selectivity. The doubly substituted analogue [2',6'-dimethyl-L-tyrosine

Consequences of opioid receptor mutation on actions of univalent and bivalent kappa and delta ligands.

Michael A Ansonoff et al.

Psychopharmacology, 210(2), 161-168 (2010-03-25)

During the past decade, substantial evidence has documented that opioid receptor heterodimers form in cell lines expressing one or more opioid receptors. More recent studies have begun to investigate whether heterodimer formation also occurs in vivo. We have used opioid

Protein kinase C mediates the synergistic interaction between agonists acting at alpha2-adrenergic and delta-opioid receptors in spinal cord.

Aaron C Overland et al.

The Journal of neuroscience : the official journal of the Society for Neuroscience, 29(42), 13264-13273 (2009-10-23)

Coactivation of spinal alpha(2)-adrenergic receptors (ARs) and opioid receptors produces antinociceptive synergy. Antinociceptive synergy between intrathecally administered alpha(2)AR and opioid agonists is well documented, but the mechanism underlying this synergy remains unclear. The delta-opioid receptor (DOP) and the alpha(2A)ARs are

Activation of peripheral delta2 opioid receptors increases cardiac tolerance to ischemia/reperfusion injury Involvement of protein kinase C, NO-synthase, KATP channels and the autonomic nervous system.

Leonid N Maslov et al.

Life sciences, 84(19-20), 657-663 (2009-02-28)

This study aims to investigate the role of peripheral delta(2) opioid receptors in cardiac tolerance to ischemia/reperfusion injury and to examine the contribution of PKC, TK, K(ATP) channels and the autonomic nervous system in delta(2) cardioprotection. Deltorphin II and various

Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ₂-opioid receptors, protein kinase C, and K(ATP) channels.

L N Maslov et al.

Bulletin of experimental biology and medicine, 149(5), 591-593 (2010-12-18)

The cardioprotective properties of a δ₂-opioid receptor agonist deltorphin II were studied in rats with coronary occlusion and reperfusion. Opioid receptor ligands and inhibitors (glybenclamide, chelerythrine, and 5-hydroxydecanoate) were injected intravenously before ischemia and reperfusion. A δ₂-opioid receptor agonist deltorphin

Regulation of interleukin-1beta and interleukin-8 production by agonists of mu and delta opiate receptors in vitro.

S V Gein et al.

Neuroscience and behavioral physiology, 39(6), 591-595 (2009-06-11)

The studies reported here showed that beta-endorphin at concentrations of 10(-7)-10(-11) M increased interleukin-1beta (IL-1beta) production in unfractionated leukocyte suspensions both in the presence of 0.1 microg/ml lipopolysaccharide (LPS) and in cultures not stimulated with LPS. Interleukin-8 (IL-8) production by

Delta opioid receptor-mediated analgesia is not altered in preprotachykinin A knockout mice.

Dave Dubois et al.

The European journal of neuroscience, 32(11), 1921-1929 (2010-11-04)

We have shown that delta opioid receptor (DOPR)-mediated analgesia was enhanced in the complete Freund's adjuvant (CFA) model of inflammation. This effect is thought to originate from translocation of DOPR in the plasma membrane of dorsal root ganglia and spinal

Membrane partitioning of various delta-opioid receptor forms before and after agonist activations: the effect of cholesterol.

Aurore André et al.

Biochimica et biophysica acta, 1778(6), 1483-1492 (2008-04-22)

Lipid rafts depicted as densely packed and thicker membrane microdomains, based on the dynamic clustering of cholesterol and sphingolipids, may help as platforms involved in a wide variety of cellular processes. The reasons why proteins segregate into rafts are yet

Effect of potent endomorphin degradation blockers on analgesic and antidepressant-like responses in mice.

Aurore Cravezic et al.

Neuropharmacology, 61(8), 1229-1238 (2011-08-02)

The biological effects of endomorphins (EMs) are short-lasting due to their rapid degradation by endogenous enzymes. Competing enzymatic degradation is an approach to prolong EM bioavailability. In the present study, a series of tetra- and tripeptides of similar to EMs

[Effect of opioid peptides on oxygen-dependent microbicidity of peripheral blood neutrophils].

S V Geĭn et al.

Fiziologiia cheloveka, 38(3), 100-106 (2012-07-27)

Investigation ofopioid peptide effect on the production of reactive oxygen species by neutrophils in non-fractionated leukocyte suspension and in purified fraction of peripheral blood neutrophils is disclosed in this work. It was determined that selective delta- and micro-agonists of peptide

Differential noxious and motor tolerance of chronic delta opioid receptor agonists in rodents.

H Beaudry et al.

Neuroscience, 161(2), 381-391 (2009-03-31)

In the present study, we asked whether multiple intrathecal injections of deltorphin II, a selective delta opioid receptor (DOPR) agonist, induced DOPR tolerance in three behavioral assays. Unilateral inflammation caused by complete Freund's adjuvant (CFA) injection into the rat or

Distinct inhibition of voltage-activated Ca2+ channels by delta-opioid agonists in dorsal root ganglion neurons devoid of functional T-type Ca2+ currents.

Z-Z Wu et al.

Neuroscience, 153(4), 1256-1267 (2008-04-25)

Both mu- and delta-opioid agonists selectively inhibit nociception but have little effect on other sensory modalities. Voltage-activated Ca(2+) channels in the primary sensory neurons are important for the regulation of nociceptive transmission. In this study, we determined the effect of

Transport of hepcidin, an iron-regulatory peptide hormone, into retinal pigment epithelial cells via oligopeptide transporters and its relevance to iron homeostasis.

Paresh P Chothe et al.

Biochemical and biophysical research communications, 405(2), 244-249 (2011-01-12)

Retinal pigment epithelial cells (RPE) express two transport systems (SOPT1 and SOPT2) for oligopeptides. Hepcidin is an iron-regulatory peptide hormone consisting of 25 amino acids. This hormone binds to ferroportin, an iron exporter expressed on the cell surface, and facilitates

Design, data analysis, and simulation of in vitro drug transport kinetic experiments using a mechanistic in vitro model.

Agnès Poirier et al.

Drug metabolism and disposition: the biological fate of chemicals, 36(12), 2434-2444 (2008-09-24)

The use of in vitro data for quantitative predictions of transporter-mediated elimination in vivo requires an accurate estimation of the transporter Michaelis-Menten parameters, V(max) and K(m), as a first step. Therefore, the experimental conditions of in vitro studies used to

[Analysis of central mechanisms involved in gastric mucosal integrity].

Klára Gyires et al.

Neuropsychopharmacologia Hungarica : a Magyar Pszichofarmakologiai Egyesulet lapja = official journal of the Hungarian Association of Psychopharmacology, 10(3), 121-125 (2008-10-30)

Beta-endorphin, deltorphin II, [D-Ala2, Phe4, Gly5-ol-enkephalin (DAGO) as well as endomorphin-1 and endomorphin-2 injected intracerebroventricularly (i.c.v.) induced gastroprotective action. It has been raised that endogenous opioids may have a central role in maintaining gastric mucosal integrity. Therefore we aimed to

Functional identification of a novel transport system for endogenous and synthetic opioid peptides in the rabbit conjunctival epithelial cell line CJVE.

Sudha Ananth et al.

Pharmaceutical research, 26(5), 1226-1235 (2008-09-11)

To investigate whether conjunctival epithelial cells express transport processes for opioid peptides. We monitored the uptake of [(3)H]deltorphin II and [(3)H]DADLE, two hydrolysis-resistant synthetic opioid peptides, in the rabbit conjunctival epithelial cell line CJVE and elucidated the characteristics of the

Agonist-induced phosphorylation bar code and differential post-activation signaling of the delta opioid receptor revealed by phosphosite-specific antibodies.

Anika Mann et al.

Scientific reports, 10(1), 8585-8585 (2020-05-24)

The δ-opioid receptor (DOP) is an attractive pharmacological target due to its potent analgesic, anxiolytic and anti-depressant activity in chronic pain models. However, some but not all selective DOP agonists also produce severe adverse effects such as seizures. Thus, the

Transport of the synthetic opioid peptide DADLE ([D-Ala2,D-Leu5]-enkephalin) in neuronal cells.

Sudha Ananth et al.

Journal of pharmaceutical sciences, 101(1), 154-163 (2011-09-10)

The sodium-coupled oligopeptide transporters 1 and 2 (SOPT1 and SOPT2) transport peptides consisting of at least five amino acids and show potential for the delivery of therapeutically relevant peptides/peptidomimetics. Here, we examined the expression of these two transporters in the

Activation of spinal mu- and delta-opioid receptors potently inhibits substance P release induced by peripheral noxious stimuli.

Hélène Beaudry et al.

The Journal of neuroscience : the official journal of the Society for Neuroscience, 31(37), 13068-13077 (2011-09-16)

Over the past few years, δ-opioid receptors (DOPRs) and μ-opioid receptors (MOPRs) have been shown to interact with each other. We have previously seen that expression of MOPR is essential for morphine and inflammation to potentiate the analgesic properties of

Removing TRPV1-expressing primary afferent neurons potentiates the spinal analgesic effect of delta-opioid agonists on mechano-nociception.

Shao-Rui Chen et al.

Neuropharmacology, 55(2), 215-222 (2008-06-27)

Most delta-opioid receptors are located on the presynaptic terminals of primary afferent neurons in the spinal cord. However, their presence in different phenotypes of primary afferent neurons and their contribution to the analgesic effect of delta-opioid agonists are not fully

Spinal activation of delta opioid receptors alleviates cancer-related bone pain.

V Otis et al.

Neuroscience, 183, 221-229 (2011-04-05)

Over the past few years, significant progress has been made in cancer therapy. Indeed, the lifespan of cancer patients has significantly increased. Although patients live longer, cancer-related pain remains a daily problem affecting their quality of life, especially when metastases

Opioid δ(1) and δ(2) receptor agonist attenuate myocardial injury via mPTP in rats with acute hemorrhagic shock.

Xiaoli Zeng et al.

The Journal of surgical research, 169(2), 267-276 (2010-05-07)

Studies have documented the beneficial roles of δ opioid receptor (OR) agonist for hemorrhagic shock. However, the myocardial protection roles and the mechanisms of hemodynamic stability during resuscitation of δ-OR agonist have not been explored. This study was designed to

Stimulation of Na+/Cl--coupled opioid peptide transport system in SK-N-SH cells by L-kyotorphin, an endogenous substrate for H+-coupled peptide transporter PEPT2.

Santoshanand V Thakkar et al.

Drug metabolism and pharmacokinetics, 23(4), 254-262 (2008-09-03)

We have recently identified a Na+/Cl--coupled transport system in mammalian cells for endogenous and synthetic opioid peptides. This transport system does not transport dipeptides/tripeptides, but is stimulated by these small peptides. Here we investigated the influence of L-kyotorphin (L-Tyr-L-Arg), an

[Regulation of IL-1beta and IL-8 production by mu-, delta-opiate receptors agonists in vitro].

S V Geĭn et al.

Rossiiskii fiziologicheskii zhurnal imeni I.M. Sechenova, 94(7), 814-821 (2008-09-05)

The beta-endorphin 10(-7-)-10(-11) M in LPS (lypopolisaccharide) presence and in spontaneous cultures promoted the IL-1beta production in mixed leukocyte fraction. LPS-induced IL-8 production in leukocyte fraction was inhibited by beta-endorphin 10(-7), 10(-11) M. The enchasing effect of beta-endorphin on IL-1beta

Evidence for two different broad-specificity oligopeptide transporters in intestinal cell line Caco-2 and colonic cell line CCD841.

Paresh Chothe et al.

American journal of physiology. Cell physiology, 300(6), C1260-C1269 (2011-02-11)

Recently the existence of two different Na(+)-coupled oligopeptide transport systems has been described in mammalian cells. These transport systems are distinct from the previously known H(+)/peptide cotransporters PEPT1 and PEPT2, which transport only dipeptides and tripeptides. To date, the only

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