An antisense oligodeoxynucleotide to μ-opioid receptors inhibits μ-opioid receptor agonist-induced analgesia in rats

1995 ◽  
Vol 275 (1) ◽  
pp. 105-108 ◽  
Author(s):  
Xiao-Hong Chen ◽  
Jill U. Adams ◽  
Ellen B. Geller ◽  
J.Kim DeRiel ◽  
Martin W. Adler ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Opioid Receptors ◽  
Receptor Agonist ◽  
Antisense Oligodeoxynucleotide ◽  
Opioid Receptor Agonist ◽  
Μ Opioid Receptor ◽  
Μ Opioid Receptors

scholarly journals Tonic GABAA receptor conductance in medial subnucleus of the tractus solitarius neurons is inhibited by activation of μ-opioid receptors

2012 ◽  
Vol 107 (3) ◽  
pp. 1022-1031 ◽  
Author(s):  
Melissa A. Herman ◽  
Richard A. Gillis ◽  
Stefano Vicini ◽  
Kenneth L. Dretchen ◽  
Niaz Sahibzada
Keyword(s):  
Opioid Receptor ◽  
Opioid Receptors ◽  
Receptor Activation ◽  
Membrane Excitability ◽  
Selective Blockade ◽  
Medial Nucleus ◽  
Opioid Receptor Agonist ◽  
Gaba Signaling ◽  
Μ Opioid Receptor ◽  
Μ Opioid Receptors

Our laboratory previously reported that gastric activity is controlled by a robust GABAA receptor-mediated inhibition in the medial nucleus of the tractus solitarius (mNTS) ( Herman et al. 2009 ), and that μ-opioid receptor activation inhibits gastric tone by suppression of this GABA signaling ( Herman et al. 2010 ). These data raised two questions: 1) whether any of this inhibition was due to tonic GABAA receptor-mediated conductance in the mNTS; and 2) whether μ-opioid receptor activation suppressed both tonic and phasic GABA signaling. In whole cell recordings from rat mNTS neurons, application of three GABAA receptor antagonists (gabazine, bicuculline, and picrotoxin) produced a persistent reduction in holding current and decrease in population variance or root mean square (RMS) noise, suggesting a blockade of tonic GABA signaling. Application of gabazine at a lower concentration abolished phasic currents, but had no effect on tonic currents or RMS noise. Application of the δ-subunit preferring agonist gaboxadol (THIP) produced a dose-dependent persistent increase in holding current and RMS noise. Pretreatment with tetrodotoxin prevented the action of gabazine, but had no effect on the THIP-induced current. Membrane excitability was unaffected by the selective blockade of phasic inhibition, but was increased by blockade of both phasic and tonic currents. In contrast, activation of tonic currents decreased membrane excitability. Application of the μ-opioid receptor agonist DAMGO produced a persistent reduction in holding current that was not observed following pretreatment with a GABAA receptor antagonist and was not evident in mice lacking the δ-subunit. These data suggest that mNTS neurons possess a robust tonic inhibition that is mediated by GABAA receptors containing the δ-subunit, that determines membrane excitability, and that is partially regulated by μ-opioid receptors.

Properties of TAN-67, a nonpeptide δ-opioid receptor agonist, at cloned human δ-and μ-opioid receptors

1995 ◽  
Vol 291 (2) ◽  
pp. 129-134 ◽  
Author(s):  
Richard J. Knapp ◽  
Robert Landsman ◽  
Sue Waite ◽  
Ewa Malatynska ◽  
Eva Varga ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Opioid Receptors ◽  
Receptor Agonist ◽  
Opioid Receptor Agonist ◽  
Δ Opioid Receptor ◽  
Μ Opioid Receptors

scholarly journals The μ-opioid receptor agonist morphine, but not agonists at δ- or κ-opioid receptors, induces peripheral antinociception mediated by cannabinoid receptors

2008 ◽  
Vol 154 (5) ◽  
pp. 1143-1149 ◽  
Author(s):  
D Da Fonseca Pacheco ◽  
A Klein ◽  
A De Castro Perez ◽  
C M Da Fonseca Pacheco ◽  
J N De Francischi ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Opioid Receptors ◽  
Receptor Agonist ◽  
Cannabinoid Receptors ◽  
Opioid Receptor Agonist ◽  
Μ Opioid Receptor

scholarly journals Four stereoisomers of the novel μ-opioid receptor agonist tapentadol hydrochloride

2011 ◽  
Vol 67 (2) ◽  
pp. o71-o76 ◽  
Author(s):  
Krishnan Ravikumar ◽  
Balasubramanian Sridhar ◽  
Nitin Pradhan ◽  
Mayur Khunt
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
The Novel ◽  
Opioid Receptor Agonist ◽  
Μ Opioid Receptor

scholarly journals Analgesic effects of a novel pH-dependent μ-opioid receptor agonist in models of neuropathic and abdominal pain

Pain ◽  
2018 ◽  
Vol 159 (11) ◽  
pp. 2277-2284 ◽  
Author(s):  
Antonio Rodriguez-Gaztelumendi ◽  
Viola Spahn ◽  
Dominika Labuz ◽  
Halina Machelska ◽  
Christoph Stein
Keyword(s):  
Abdominal Pain ◽  
Opioid Receptor ◽  
Receptor Agonist ◽  
Analgesic Effects ◽  
Opioid Receptor Agonist ◽  
Μ Opioid Receptor ◽  
Ph Dependent

Effects of an opioid receptor agonist and antagonist on cytokine-stimulated canine articular chondrocytes in three-dimensional culture

2002 ◽  
Vol 15 (02) ◽  
pp. 72-77
Author(s):  
J. L. Cook ◽  
J. R. Dodam ◽  
J. M. Kreeger ◽  
J. L. Tomlinson ◽  
K. Kuroki ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
Articular Chondrocytes ◽  
Interleukin 1 ◽  
Three Dimensional ◽  
Culture Liquid ◽  
Pge2 Production ◽  
Opioid Receptor Agonist ◽  
Agonist And Antagonist ◽  
Μ Opioid Receptor

SummaryThe objective of this study was to evaluate the effects of [D-Ala2, Nme-Phe4, Gly5-ol] enkephalin (DAMGO), a μ-opioid receptor agonist, and β-funaltrexamine (β-FNA), a μ-opioid receptor antagonist, on the biosynthetic capabilities of canine chondrocytes cultured in the presence of interleukin-1 β (IL-1 β). Articular chondrocytes were harvested from the humeral heads of three adult dogs and cultured in a three-dimensional (3-D) gel medium made from low-melting agarose and cell culture medium. Chondrocytes in 3-D culture were exposed to IL-1 β (0 or 20 ng/ml), DAMGO (0,0.1,1.0, or 10 μM), and β-FNA (0 or 10 μM) by addition to the liquid media in all possible combinations. On days five and 15 of 3-D culture, liquid medium samples were harvested for subsequent analysis of glycosaminogly- can (GAG), prostaglandin E2 (PGE2) and matrix metalloprotease-3 (MMP-3) content. On the same days, gel plugs were also harvested and evaluated for GAG content.Incubation with IL-1 β decreased the amount of GAG in the gel plugs and caused an increase in PGE2 production on days five and 15 of 3-D culture. Treatment with DAMGO or β-FNA did not significantly modulate PGE2 production, MMP-3 production, GAG loss to the medium or GAG content of the gel plugs on either day five or 15 of 3-D culture in the presence or absence of IL-1 β. We concluded that DAMGO and β-FNA had neither protective nor detrimental effects on the biosynthetic capabilities of chondrocytes in the presence or absence of IL-1 β.

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