Abstract
The effect of nociceptin/orphanin FQ (N/OFQ) on protein kinase C (PKC) was investigated in Chinese hamster ovary cells stably expressing opioid receptor-like (ORL1) receptor (CHO-ORL1 cells). N/OFQ significantly activated PKC in CHO-ORL1 cells with EC50 of 0.2 nM. This response was blocked by PKC inhibitors chelerythrine and Gö 6976, and by pretreatment of cells with pertussis toxin (PTX). The inhibition of PKC activation by N/OFQ was also achieved by use of Ca(2+)-chelators and phospholipase C (PLC) inhibitor U-73122. These results indicate that N/OFQ can effectively activate PKC via ORL1 receptor, and suggest the activation involve the PLC/Ca2+ system.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkaloids
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Animals
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Benzophenanthridines
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CHO Cells
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Calcium / metabolism*
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Carbazoles / pharmacology
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Chelating Agents / pharmacology
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Cricetinae
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Egtazic Acid / analogs & derivatives
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Egtazic Acid / pharmacology
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Enzyme Activation
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Enzyme Inhibitors / pharmacology
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Estrenes / pharmacology
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Indoles / pharmacology
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Nociceptin
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Nociceptin Receptor
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Opioid Peptides / pharmacology*
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Pertussis Toxin
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Phenanthridines / pharmacology
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Protein Kinase C / metabolism*
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Pyrrolidinones / pharmacology
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Receptors, Opioid / agonists
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Receptors, Opioid / biosynthesis
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Receptors, Opioid / physiology*
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Recombinant Proteins / metabolism
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Signal Transduction
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Transfection
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Type C Phospholipases / metabolism*
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Virulence Factors, Bordetella / pharmacology
Substances
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Alkaloids
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Benzophenanthridines
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Carbazoles
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Chelating Agents
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Enzyme Inhibitors
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Estrenes
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Indoles
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Opioid Peptides
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Phenanthridines
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Pyrrolidinones
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Receptors, Opioid
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Recombinant Proteins
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Virulence Factors, Bordetella
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1-(6-((3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione
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Go 6976
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1,2-bis(2-aminophenoxy)ethane N,N,N',N'-tetraacetic acid acetoxymethyl ester
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Egtazic Acid
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chelerythrine
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Pertussis Toxin
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Protein Kinase C
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Type C Phospholipases
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Calcium
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Nociceptin Receptor