Diminution of contractile response by κ-opioid receptor agonists in isolated rat ventricular cardiomyocytes is mediated via a pertussis toxin-sensitive G protein

1998 ◽  
Vol 358 (3) ◽  
pp. 360-366 ◽  
Author(s):  
H. Wenzlaff ◽  
Birgitt Stein ◽  
Hansjörg Teschemacher
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Pertussis Toxin ◽  
Contractile Response ◽  
Receptor Agonists ◽  
Ventricular Cardiomyocytes ◽  
Opioid Receptor Agonists ◽  
Isolated Rat

Some effects of putative G-protein biased mu-opioid receptor agonists in male rhesus monkeys

2021 ◽  
Vol Publish Ahead of Print ◽  
Author(s):  
Jeremy C. Cornelissen ◽  
Bruce E. Blough ◽  
Laura M. Bohn ◽  
S. Stevens Negus ◽  
Matthew L. Banks
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Rhesus Monkeys ◽  
Mu Opioid Receptor ◽  
Mu Opioid ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists ◽  
Male Rhesus

scholarly journals Absence of G-protein activation by μ-opioid receptor agonists in the spinal cord of μ-opioid receptor knockout mice

1999 ◽  
Vol 126 (2) ◽  
pp. 451-456 ◽  
Author(s):  
Minoru Narita ◽  
Hirokazu Mizoguchi ◽  
Michiko Narita ◽  
Ichiro Sora ◽  
George R Uhl ◽  
...  
Keyword(s):  
Spinal Cord ◽  
G Protein ◽  
Opioid Receptor ◽  
Knockout Mice ◽  
Protein Activation ◽  
Receptor Agonists ◽  
G Protein Activation ◽  
Μ Opioid Receptor ◽  
Opioid Receptor Agonists

scholarly journals Cholinoceptor Activation Subserving the Effects of Interferon Gamma on the Contractility of Rat Ileum

1994 ◽  
Vol 3 (6) ◽  
pp. 453-458 ◽  
Author(s):  
Enri S. Borda ◽  
Leonor Sterin-Borda ◽  
Martin Rodriguez ◽  
Maria M. E. de Bracco
Keyword(s):  
G Protein ◽  
Interferon Gamma ◽  
Pertussis Toxin ◽  
Contractile Response ◽  
Interferon Γ ◽  
Maximum Effect ◽  
Rat Ileum ◽  
Muscarinic Cholinoceptors ◽  
Cytochalasine B ◽  
Isolated Rat

Recombinant rat interferon γ stimulated the contractility of isolated rat ileum at doses of 4–12 units/ml. Muscarinic cholinoceptors were involved, as treatment of the tissue with atropine prevented the contractile response of the ileum. Furthermore, interferon γ increased the affinity of carbachol for the cholinoceptors and did not change its maximum effect. Neurogenic pathways were also involved since pretreatment of ileum with hexamethonium, hemicholinium or tetrodotoxin impaired the contractile effect of interferon γ. In contrast to the action of exogenous carbachol, the effects of interferon γ are indirect. They appear to involve a G protein regulating phosphoinositide turnover and cytoskeletal structures since they could not be induced in ileum strips that were pretreated with pertussis toxin, phospholipase C inhibitors (2-nitro-carboxyphenyl,NN-diphenyl carbamate and neomycin), cytochalasine B or colchicine.

scholarly journals In Vitro Analyses of Spinach-Derived Opioid Peptides, Rubiscolins: Receptor Selectivity and Intracellular Activities through G Protein- and β-Arrestin-Mediated Pathways

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 6079
Author(s):  
Yusuke Karasawa ◽  
Kanako Miyano ◽  
Hideaki Fujii ◽  
Takaaki Mizuguchi ◽  
Yui Kuroda ◽  
...  
Keyword(s):  
Side Effects ◽  
G Protein ◽  
Opioid Receptor ◽  
Opioid Receptors ◽  
Opioid Peptides ◽  
Opioid Analgesics ◽  
Receptor Agonists ◽  
Δ Opioid Receptor ◽  
Opioid Receptor Agonists

Activated opioid receptors transmit internal signals through two major pathways: the G-protein-mediated pathway, which exerts analgesia, and the β-arrestin-mediated pathway, which leads to unfavorable side effects. Hence, G-protein-biased opioid agonists are preferable as opioid analgesics. Rubiscolins, the spinach-derived naturally occurring opioid peptides, are selective δ opioid receptor agonists, and their p.o. administration exhibits antinociceptive effects. Although the potency and effect of rubiscolins as G-protein-biased molecules are partially confirmed, their in vitro profiles remain unclear. We, therefore, evaluated the properties of rubiscolins, in detail, through several analyses, including the CellKeyTM assay, cADDis® cAMP assay, and PathHunter® β-arrestin recruitment assay, using cells stably expressing µ, δ, κ, or µ/δ heteromer opioid receptors. In the CellKeyTM assay, rubiscolins showed selective agonistic effects for δ opioid receptor and little agonistic or antagonistic effects for µ and κ opioid receptors. Furthermore, rubiscolins were found to be G-protein-biased δ opioid receptor agonists based on the results obtained in cADDis® cAMP and PathHunter® β-arrestin recruitment assays. Finally, we found, for the first time, that they are also partially agonistic for the µ/δ dimers. In conclusion, rubiscolins could serve as attractive seeds, as δ opioid receptor-specific agonists, for the development of novel opioid analgesics with reduced side effects.

Region-dependent G-protein activation by μ-, δ1- and δ2-opioid receptor agonists in the brain: Comparison between the midbrain and forebrain

Life Sciences ◽  
1999 ◽  
Vol 65 (16) ◽  
pp. PL233-PL239 ◽  
Author(s):  
Minoru Tsuji ◽  
Minoru Narita ◽  
Hirokazu Mizoguchi ◽  
Michiko Narita ◽  
Masahiro Ohsawa ◽  
...  
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Protein Activation ◽  
Receptor Agonists ◽  
G Protein Activation ◽  
Opioid Receptor Agonists ◽  
The Brain
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