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• W2108443815 abstract "The CB₁ cannabinoid receptor antagonist <i>N</i>-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1<i>H</i>-pyrazole-3-carboxamide hydrochloride (SR141716) has been shown by many investigators to inhibit basal G-protein activity, i.e., to display inverse agonism at high concentrations. However, it is not clear whether this effect is cannabinoid CB₁ receptor-mediated. Using the ligand-stimulated [³⁵S]guanosine 5′-3-<i>O</i>-(thio)triphosphate (GTPγS) assay, we have found that 10 μM SR141716 slightly but significantly decreases the basal [³⁵S]GTPγS binding in membranes of the wild-type and CB₁ receptor knockout mouse cortex, parental Chinese hamster ovary (CHO) cells, and CHO cells stably transfected with μ-opioid receptors, MOR-CHO. Accordingly, we conclude that the inverse agonism of SR141716 is CB₁ receptor-independent. Although the specific MOR agonist Tyr-d-Ala-Gly-(NMe)Phe-Gly-ol (DAMGO) saturably and concentration-dependently stimulated [³⁵S]GTPγS binding, SR141716 (10 μM) inhibited the basal by 25% and competitively inhibited DAMGO stimulation in the mouse cortex. In MOR-CHO membranes, DAMGO caused a 501 ± 29% stimulation of the basal activity, which was inhibited to 456 ± 22% by 10 μM SR141716. The inverse agonism of SR141716 was abolished, and DAMGO alone displayed weak, naloxone-insensitive stimulation, whereas the combination of DAMGO and SR141716 (10 μM each) resulted in a 169 ± 22% stimulation of the basal activity (that was completely inhibited by the prototypic opioid antagonist naloxone) because of pertussis toxin (PTX) treatment to uncouple MORs from G_i/G_o proteins. SR141716 proved to bind directly to MORs with low affinity (IC₅₀ = 5.7 μM). These results suggest the emergence of novel, PTX-insensitive G-protein signaling that is blocked by naloxone when MORs are activated by the combination of DAMGO and SR141716." @default.
• W2108443815 created "2016-06-24" @default.
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• W2108443815 date "2009-05-15" @default.
• W2108443815 modified "2023-10-17" @default.
• W2108443815 title "CB₁ Receptor-Independent Actions of SR141716 on G-Protein Signaling: Coapplication with the μ-Opioid Agonist Tyr-d-Ala-Gly-(NMe)Phe-Gly-ol Unmasks Novel, Pertussis Toxin-Insensitive Opioid Signaling in μ-Opioid Receptor-Chinese Hamster Ovary Cells" @default.
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• W2108443815 doi "https://doi.org/10.1124/jpet.109.152710" @default.
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