MLS6357, a D3 dopamine receptor (D3R)-selective positive allosteric modulator and antagonist, demonstrates significant antagonist activity in D3R-mediated assays, including BRET-based β-arrestin recruitment and Go-BRET assays, with IC50 values of 13 μM, 14 μM, and 17 μM respectively. It shows selectivity for D3R, with no notable activity on other dopamine receptor subtypes (D1R, D2R, D4R, D5R) at concentrations above 100 μM. MLS6357 serves as a valuable tool for investigating neuropsychiatric disorders, particularly in the context of substance use disorders.
MLS6357, a D3 dopamine receptor (D3R)-selective positive allosteric modulator and antagonist, demonstrates significant antagonist activity in D3R-mediated assays, including BRET-based β-arrestin recruitment and Go-BRET assays, with IC50 values of 13 μM, 14 μM, and 17 μM respectively. It shows selectivity for D3R, with no notable activity on other dopamine receptor subtypes (D1R, D2R, D4R, D5R) at concentrations above 100 μM. MLS6357 serves as a valuable tool for investigating neuropsychiatric disorders, particularly in the context of substance use disorders.
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