RG-15 is a potent oral antagonist of the dopamine receptors, specifically targeting the human D2 and D3 receptors with pKi values of 8.23 and 10.49, respectively. It effectively inhibits dopamine-stimulated [35S]GTPγS binding, demonstrating an IC50 of 21.2 nM in rat striatal membranes, 36.7 nM in mouse A9 cells expressing human D2L receptors, and 7.2 nM in CHO cells expressing human D3 receptors. RG-15 also enhances dopamine turnover and biosynthesis in the mouse striatum and olfactory bulb, indicating potential antipsychotic properties. This compound is valuable for research into dopamine-related disorders and therapeutics.
RG-15 is a potent oral antagonist of the dopamine receptors, specifically targeting the human D2 and D3 receptors with pKi values of 8.23 and 10.49, respectively. It effectively inhibits dopamine-stimulated [35S]GTPγS binding, demonstrating an IC50 of 21.2 nM in rat striatal membranes, 36.7 nM in mouse A9 cells expressing human D2L receptors, and 7.2 nM in CHO cells expressing human D3 receptors. RG-15 also enhances dopamine turnover and biosynthesis in the mouse striatum and olfactory bulb, indicating potential antipsychotic properties. This compound is valuable for research into dopamine-related disorders and therapeutics.
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