Since beta-endorphins can bind both mu opioid and kappa-opioid receptors we investigated the effect of a mu specific receptor agonist, D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin (DAMGO) and a mu specific antagonist, D-Phe-Cys-Trp-Arg-Thr-Pen-Thr-NH2 (CTAP) on cardiovascular responses in conscious control and obese rats. (nih.gov)
The μ-opioid receptor (MOP-R) agonist [D-Ala 2 ,N-Me-Phe 4 ,Gly 5 -ol]-enkephalin (DAMGO) also produced dose-dependent flexor response in same dose ranges. (illinois.edu)
Intrathecal (i.t.) administration of peptidic MOR agonist [D-Ala 2 , N-Me-Phe 4 ,Gly 5 -ol]-enkephalin (DAMGO, 0.00032-0.01 mg) evoked scratching, but i.v, DAMGO (0.01-1 mg/kg) did not increase scratching. (ewha.ac.kr)
Neither the δ-opioid agonist, DPDPE ([D-Pen 2,5 ]-enkephalin) nor the μ-opioid agonist, DAMGO (Tyr-D-Ala-Gly-N-Me-Phe-Gly-ol enkephalin) elevated [Ca 2+ ](i) when applied alone. (edu.au)
4. The δ-receptor antagonist, naltrindole (30 nM), blocked the elevations of [Ca 2+ ](i) by DPDPE (100 nM) without affecting those caused by DAMGO while the μ-receptor antagonist, CTAP (D-Phe-Cys-Tyr-D-Trp-Arg-Pen-Thr-NH 2 ) (100 nM-1 μM) blocked the elevations of [Ca 2+ ](i) caused by DAMGO (1 μM) without affecting those caused by DPDPE. (edu.au)
Our results show a rise in basal intracellular calcium ([Ca(2+)]i) in response to application of [D-Ala(2)-N-Me-Phe(4),Gly5-ol]-Enkephalin (DAMGO), a MOR agonist, that is blocked by D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP), a MOR antagonist. (umassmed.edu)
Rats2
In slices from morphine-dependent rats maintained in morphine (5 μ m ) in vitro , action potential frequencies of opioid-sensitive neurons did not differ from untreated control neurons but were greater than in control neurons maintained in morphine in vitro , indicating development of tolerance. (jneurosci.org)
Substance P (SP) levels in the spinal cords of very old rats are less than the levels in younger rats (Bergman et al. (omeka.net)
Opioid2
In contrast, the amplitude of evoked IPSCs was not altered either by Met-enkephalin or by any of the opioid receptor-selective agonists. (psu.edu)
opioid receptor in the brain determined by the [tylosil-3,5-(3)H(N)]-[d-Ala(2),N-MePhe(4),Gly-ol(5)]enkephalin binding assay was not significantly changed by a deletion of the dopamine D(3) receptor gene. (opioids.wiki)
Receptors2
furthermore, oxytocin-induced synaptic plasticity requires activation of nucleus accumbens 5-ht1b receptors, the blockade of which prevents social reward. (cognitive-liberty.online)
5. Block of carbachol activation of muscarinic receptors with atropine (10 μM) abolished the elevation of [Ca 2+ ](i) by the opioids. (edu.au)
Morphine1
Prior incubation with capsaicin, a depletor of SP from polymodal C fibers and [(+)-(2S,3S)-(2-methoxybenzylamino)-2-phenylpiperidine] (CP-99994), a tachykinin 1 receptor antagonist, also blocked the morphine-induced flexor responses. (illinois.edu)
Receptor1
These results demonstrate that the modulatory effects of opioids on 5-HT release are receptor-specific and state-dependent, indicating the complex nature of the roles of different opioids in regulating hibernation. (elsevierpure.com)
Vitro1
The responses of canine middle cerebral arteries to changes in pCO 2 and pO 2 were tested in vitro. (cambridge.org)
British Journal of P1
British Journal of Pharmacology , 117 (2), 333-340. (edu.au)
Amino1
The central theme of this methodology is the formation of alpha -aminoalkyl radicals from existing amino acid and alpha -amino alcohol derivatives by 1,5-hydrogen atom transfer and the subsequent trapping of these radicals with appropriate radicalphiles, thus generating quaternary centres with high efficiency and excellent stereocontrol. (exeter.ac.uk)
Slices4
To elucidate the role of opioids in regulating hibernation, the modulatory effects of different opioids on 35 mM K + -stimulated [ 3 H]-5-HT release from brain slices were examined in the Richardson's ground squirrels. (elsevierpure.com)
DAGO ([D-Ala 2 ,N-Me-Phe 4 ,Gly-ol 5 ]-enkephalin), a specific μ agonist, evoked a significant dose-dependent (10 -7 -10 -5 M) inhibition of K + -stimulated 5-HT release from hippocampal slices of the non-hibernating squirrels. (elsevierpure.com)
In contrast, κ agonist U50488 (10 -5 M) exerted a significant enhancement of K + -stimulated 5-HT release from hippocampal slices of the non-hibernating squirrels. (elsevierpure.com)
DAGO and U50488 had no modulatory effects on K + -stimulated 5-HT release from the hypothalamic slices of either the non-hibernating or hibernating squirrels. (elsevierpure.com)
Specific1
This enhancement was blocked by either the specific κ antagonist nor-binaltorphimine (10 -6 M) or TTX (10 -6 M). However, in the hibernating squirrels, the stimulatory effect of U50488 (10 -5 M) on 5-HT release was absent. (elsevierpure.com)
Cells1
2. The Ca 2+ -sensitive dye, fura-2, was used to measure [Ca 2+ ](i) in confluent monolayers of SH-SY5Y cells. (edu.au)
Research1
This ongoing area of research has led to further investigations into the 1,5-hydrogen atom transfer process and in particular, studies into the effectiveness of deuterium as a protecting group for C-H bonds in radical and carbene chemistry. (exeter.ac.uk)
Issue1
Metabolic syndrome (MS) has been an important health issue in the world, and insulin resistance (IR) is one of the characteristics of MS, increasing the risk for the onset and poor prognosis of type 2 diabetes mellitus (T2D). (bvsalud.org)
Opioid receptor3
SB-612111 had no intrinsic agonistic activity and did not affect the GIRK current induced by [D-Ala 2 , N-Me-Phe 4 , Gly 5 -ol]-enkephalin, a mu-opioid receptor agonist, when tested at concentrations of up to 1 μM. (sri.com)
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR . (nih.gov)
The mouse mu opioid receptor (OPRM1) gene undergoes extensive alternative splicing at both the 3'- and 5'-ends of the gene. (biomedcentral.com)
Antinociceptive3
The aims, with this study, were to use nerve-injured animals to determine: (1) whether the antinociceptive potency and efficacy of intrathecal clonidine was altered, and (2) whether the combination of intrathecal morphine and clonidine would act synergistically to produce antinociception. (nih.gov)
2. Competitive and non-competitive NMDA antagonists block the development of antinociceptive tolerance to morphine, but not to selective mu or delta opioid agonists in mice. (nih.gov)
18. Effect of MK-801 on the antinociceptive effect of [D-Ala(2),N-MePhe(4), Gly-ol(5)]enkephalin in diabetic mice. (nih.gov)
Mice1
In both mice and humans 5' splicing generates a number of exon 11-containing variants. (biomedcentral.com)
Ligand1
The goal of this study was to investigate the crosstalk between the mu OR, transient receptor potential vanilloid 1 (TRPV1) receptor and C-C motif ligand 2 (CCL2) chemokine and the involvement of spinal microglia in the modulation of opioid analgesia. (cas.cz)
Analgesics1
[ 5 , 6 ] These guidelines recommend against using opioid analgesics for CNCP as a first-line medication because the harms frequently outweigh the benefits. (medscape.com)
Two countries at the epicenter of the opioid crisis, Canada and the United States, [ 1-4 ] recently released clinical practice guidelines for opioid prescribing for chronic noncancer pain (CNCP). (medscape.com)
Spinal1
8. Dynorphinergic mechanism mediating endomorphin-2-induced antianalgesia in the mouse spinal cord. (nih.gov)
Effects1
Thus, we investigated opioid effects on intracellular Ca 2+ in cultured rat hippocampal neurons by using fura-2-based microscopic Ca 2+ imaging. (jneurosci.org)