A CB1 receptor agonist and PAM; a racemic mixture of GAT228 and GAT229; increases β-arrestin recruitment and cAMP inhibition in HEK293A cells expressing hCB1-GFP in a concentration-dependent manner; enhances the binding of the CB1 full agonist CP 55

GAT211 – 1 mg

Brand:
Cayman
CAS:
102704-40-5
Storage:
-20
UN-No:
Non-Hazardous - /

GAT211 is an agonist and positive allosteric modulator (PAM) of cannabinoid receptor 1 (CB1) and a racemic mixture of GAT228 (Item No. 24485) and GAT229 (Item No. 24486), which have enantiomer-specific activities.{35179} GAT211 increases β-arrestin recruitment and cAMP inhibition in HEK293A cells expressing GFP-tagged human CB1 (hCB1-GFP) in a concentration-dependent manner. It also enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing hCB1, as well as the activity of 2-arachidonoyl glycerol (2-AG; Item No. 62160), arachidonoyl ethanolamide (AEA; Item No. 90050), and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. It inhibits excitatory postsynaptic currents (EPSCs) in a subset of CB1-expressing murine autaptic hippocampal neurons when used at a concentration of 1 µM.{48089} GAT211 also decreases mechanical hypersensitivity in wild-type (EC50 = 9.75 mg/kg), but not CB1 knockout, mice in a model of inflammatory pain induced by complete Freund’s adjuvant (CFA), and decreases mechanical and cold allodynia in a mouse model of paclitaxel-induced neuropathic pain when used at doses of 10 and 20 mg/kg per day.{47206}  

 

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Description

A CB1 receptor agonist and PAM; a racemic mixture of GAT228 and GAT229; increases β-arrestin recruitment and cAMP inhibition in HEK293A cells expressing hCB1-GFP in a concentration-dependent manner; enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing hCB1; inhibits EPSCs in a subset of CB1-expressing murine autaptic hippocampal neurons at 1 µM; decreases mechanical hypersensitivity in wild-type (EC50 = 9.75 mg/kg), but not CB1 knockout, mice in a model of CFA-induced inflammatory pain; decreases mechanical and cold allodynia in a mouse model of paclitaxel-induced neuropathic pain at 10 and 20 mg/kg per day

Formal name: 3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole

Synonyms: 

Molecular weight: 342.4

CAS: 102704-40-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors||Research Area|Neuroscience|Pain Research

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