hu-308 and lysophosphatidylinositol

hu-308 has been researched along with lysophosphatidylinositol* in 1 studies

Other Studies

1 other study(ies) available for hu-308 and lysophosphatidylinositol

Article	Year
Modulation of l-α-lysophosphatidylinositol/GPR55 MAP kinase signalling by CB2 receptor agonists: identifying novel GPR55 inhibitors. Journal of basic and clinical physiology and pharmacology, 2016, May-01, Volume: 27, Issue:3 GPR55 is a lipid-sensing G protein-coupled receptor that is activated by the endogenous lipid l-α-lysophosphatidylinositol (LPI) and can be modulated by certain cannabinoid ligands.. In this study we investigated the GPR55 activity of four synthetic CB2 receptor agonists using the AlphaScreen® SureFire® assay.. Here we show that the CB2 receptor-selective agonists HU-308, HU-433 and HU-910 do not promote GPR55-mediated ERK1/2 phosphorylation up to a concentration of 3 μM. However, LPI-induced ERK1/2 phosphorylation is inhibited by the (-)-enantiomer of HU-308, designated HU-433, whereas HU-308 has no effect on LPI activity. The carboxylic analogue of HU-910, designated HU-914, potently inhibits LPI-induced ERK1/2 phosphorylation; however, HU-914 was less effective, with potential biphasic effects.. This structure-activity-relationship study has identified novel ligands which act both as CB2 receptor agonists and GPR55 modulators and related compounds that lack GPR55 activity. Topics: Bridged Bicyclo Compounds; Cannabinoid Receptor Agonists; Cannabinoid Receptor Antagonists; Cannabinoids; Cell Line; HEK293 Cells; Humans; Ligands; Lysophospholipids; MAP Kinase Signaling System; Phosphorylation; Receptor, Cannabinoid, CB2; Receptors, Cannabinoid; Receptors, G-Protein-Coupled; Signal Transduction	2016

Article

Year

Modulation of l-α-lysophosphatidylinositol/GPR55 MAP kinase signalling by CB2 receptor agonists: identifying novel GPR55 inhibitors.

Journal of basic and clinical physiology and pharmacology, 2016, May-01, Volume: 27, Issue:3

GPR55 is a lipid-sensing G protein-coupled receptor that is activated by the endogenous lipid l-α-lysophosphatidylinositol (LPI) and can be modulated by certain cannabinoid ligands.. In this study we investigated the GPR55 activity of four synthetic CB2 receptor agonists using the AlphaScreen® SureFire® assay.. Here we show that the CB2 receptor-selective agonists HU-308, HU-433 and HU-910 do not promote GPR55-mediated ERK1/2 phosphorylation up to a concentration of 3 μM. However, LPI-induced ERK1/2 phosphorylation is inhibited by the (-)-enantiomer of HU-308, designated HU-433, whereas HU-308 has no effect on LPI activity. The carboxylic analogue of HU-910, designated HU-914, potently inhibits LPI-induced ERK1/2 phosphorylation; however, HU-914 was less effective, with potential biphasic effects.. This structure-activity-relationship study has identified novel ligands which act both as CB2 receptor agonists and GPR55 modulators and related compounds that lack GPR55 activity.

Topics: Bridged Bicyclo Compounds; Cannabinoid Receptor Agonists; Cannabinoid Receptor Antagonists; Cannabinoids; Cell Line; HEK293 Cells; Humans; Ligands; Lysophospholipids; MAP Kinase Signaling System; Phosphorylation; Receptor, Cannabinoid, CB2; Receptors, Cannabinoid; Receptors, G-Protein-Coupled; Signal Transduction

2016