GAT228 Chemical Properties

Boiling point:

585.8±50.0 °C(Predicted)

Density 

1.237±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 20 mg/ml

form 

A solid

pka

7.77±0.18(Predicted)

color 

white to beige

optical activity

[α]/D 80 to 94°, c =1 in methanol

GAT228 Usage And Synthesis

Description

GAT228 is an allosteric agonist of cannabinoid receptor 1 (CB₁), the R-(+)-enantiomer of the CB₁ positive allosteric modulator (PAM) GAT229 , and a component of the racemic mixture GAT211, which acts as both an agonist and PAM. GAT228 increases β-arrestin recruitment, cAMP inhibition, and ERK1/2 and PLCβ3 phosphorylation in HEK293A cells expressing GFP-tagged human CB₁ (hCB₁-GFP) in a concentration-dependent manner. Unlike GAT229, GAT228 has no effect on the binding of the CB receptor agonist CP 55,940 to membranes from CHO cells expressing hCB₁ when used at concentrations up to 1 μM. It inhibits excitatory postsynaptic currents (EPSCs) in a subset of CB₁-expressing murine autaptic hippocampal neurons when used at a concentration of 1 μM.

Uses

GAT228, the enantiomer of GAT211, is an allosteric cannabinoid receptor 1 (CB1) ligand[1].

in vivo

References

[1] Dinesh Thapa, et al. Allosteric Cannabinoid Receptor 1 (CB1) Ligands Reduce Ocular Pain and Inflammation. Molecules. 2020 Jan 20;25(2):417. DOI:10.3390/molecules25020417