RG-15 is an orally active dopamine receptor antagonist with high affinity for the human D2 receptor (pKi of 8.23) and human D3 receptor (pKi of 10.49). It inhibits dopamine-stimulated [35S]GTPgammaS binding with IC50 values 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 enhances dopamine turnover and synthesis in the striatum and olfactory bulb of mice, exhibiting antipsychotic activity.
Molecular Weight:
594.52
CAS Number:
[1076189-55-3]
Formula:
C25H32Cl2F3N5O2S
Target:
Dopamine Receptor
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