GAT228 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
GAT228 is an allosteric agonist of cannabinoid receptor 1 (CB
1), the R-(+)-enantiomer of the CB
1 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 CB
1 (hCB
1-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 hCB
1 when used at concentrations up to 1 μM. It inhibits excitatory postsynaptic currents (EPSCs) in a subset of CB
1-expressing murine autaptic hippocampal neurons when used at a concentration of 1 μM.
GAT228 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte