RG-15

RG-15 is the orally active antagonist for dopamine receptor that exhibits goof affinity to human D2 receptor and human D3 receptor with pKi of 8.23 and 10.49. RG-15 inhibits dopamine-stimulated [35S]GTPγS binding with IC50 of 21.2 nM (rat striatal membranes), 36.7 nM (mouse A9 cells expressing human D2L receptors) and 7.2 nM (CHO cells expressing human D3 receptors) . RG-15 increases the turnover and biosynthesis of dopamine in mouse striatum and olfactory bulb, exhibiting antipsychotic activity[1].

Product Specifications

CAS Number

[1076189-55-3]

UNSPSC

12352005

Target

Dopamine Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

Purity

95.18

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

FC(F)(C1=CC(C#N)=CC(N2CCN(CC2)CC[C@H]3CC[C@@H](CC3)NS(=O)(C4=CN=CC=C4)=O)=C1)F.Cl.Cl

Molecular Formula

C25H32Cl2F3N5O2S

Molecular Weight

594.52

References & Citations

[1]Kiss B, et al., Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: I. neurochemical characterisation of RG-15. Naunyn Schmiedebergs Arch Pharmacol. 2008 Nov;378 (5) :515-28.