Cariprazine impurity 1 is a dopamine D2 receptor ( D2R ) agonist. Cariprazine impurity 1 modulates D2R -mediated G i/o signaling pathway to inhibit cAMP production, and regulates D2R -mediated β-arrestin2 recruitment pathway [1].
In Vitro, Cariprazine impurity 1 (Compound 11) acts as a balanced partial agonist of human D2R, mediates Gi/o-dependent cAMP inhibition (with an EC50 of 0.7 nM) and β-arrestin2 recruitment (with an EC50 of 2 nM), and exhibits a mild bias toward the Gi/o signaling pathway[1].
References:
[1]. Shen Y, et al. D 2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine. J Med Chem. 2019;62(9):4755-4771.
In Vitro, Cariprazine impurity 1 (Compound 11) acts as a balanced partial agonist of human D2R, mediates Gi/o-dependent cAMP inhibition (with an EC50 of 0.7 nM) and β-arrestin2 recruitment (with an EC50 of 2 nM), and exhibits a mild bias toward the Gi/o signaling pathway[1].
References:
[1]. Shen Y, et al. D 2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine. J Med Chem. 2019;62(9):4755-4771.