GP 1a
Chemical Name: N-(Piperidin-1-yl)-1-(2,4-dichlorophenyl)-1,4-dihydro-6-methylindeno[1,2-c]pyrazole-3-carboxamide
Purity: ≥99%
Biological Activity
GP 1a is a CB2 receptor inverse agonist (pEC50 = 7.1), shown in cAMP, GTPγS and β-arrestin recruitment assays. Demonstrates approximately 30-fold selectivity for CB2 receptors over CB1 receptors. Increases P-ERK1/2 expression in HL-60 cells in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Background References
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Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.
Soethoudt et al.
Nat.Commun., 2017;8:13958 -
The cannabinoid receptor 2 is critical for the host response to sepsis.
Tschop et al.
J.Immunol., 2009;183:499 -
Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxam
Murineddu et al.
J.Med.Chem., 2006;49:7502
Product Datasheets
Citations for GP 1a
The citations listed below are publications that use Tocris products. Selected citations for GP 1a include:
6 Citations: Showing 1 - 6
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Antiallodynic Effects of Cannabinoid Receptor 2 (CB2R) Agonists on Retrovirus Infection-Induced Neuropathic Pain.
Authors: Sheng Et al.
Pain Res Manag 2019;2019:1260353
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Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.
Authors: Soethoudt Et al.
Nat.Commun. 2017;
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CB2R orchestrates fibrogenesis through regulation of inflammatory response during the repair of skeletal muscle contusion.
Authors: Zhang Et al.
Am J Physiol Regul Integr Comp Physiol 2015;8:3491
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Activation of cannabinoid receptor 2 inhibits experimental cystitis.
Authors: Wang Et al.
J Neuroimmune Pharmacol 2013;304:R846
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The anti-apoptotic Bcl-B protein inhibits BECN1-dependent autophagic cell death.
Authors: Robert Et al.
Int J Clin Exp Pathol 2012;8:637
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Cannabinoid 2 (CB2) receptor involvement in the down-regulation but not up-regulation of serum IgE levels in immunized mice.
Authors: Newton and Klein
PLoS One 2012;7:591
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