Dopamine D3 receptor antagonist-3 is a selective positive allosteric modulator-antagonist targeting the D3 dopamine receptor (D3R) that effectively penetrates the blood-brain barrier. It demonstrates robust antagonist activity in D3R-mediated β-arrestin recruitment assays, exhibiting an IC50 of 2.5 μM and a Kd of 0.49 μM, and in D3R-mediated Go-BRET assays, with an IC50 of 0.34 μM. This reagent is suitable for investigating neuropsychiatric disorders, including substance use disorder, providing valuable insights into D3R's role in these conditions.
Dopamine D3 receptor antagonist-3 is a selective positive allosteric modulator-antagonist targeting the D3 dopamine receptor (D3R) that effectively penetrates the blood-brain barrier. It demonstrates robust antagonist activity in D3R-mediated β-arrestin recruitment assays, exhibiting an IC50 of 2.5 μM and a Kd of 0.49 μM, and in D3R-mediated Go-BRET assays, with an IC50 of 0.34 μM. This reagent is suitable for investigating neuropsychiatric disorders, including substance use disorder, providing valuable insights into D3R's role in these conditions.
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