Dopamine D3 receptor antagonist-3

Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R) -selective positive allosteric modulator (PAM) -antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC50 and a Kd of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder[1].

Product Specifications

CAS Number

[2894793-37-2]

UNSPSC

12352005

Target

Dopamine Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

ClC(C=C1NS(C(C(C(N(C2)CCC2(F)F)=O)=C3C)=C(N3)C)(=O)=O)=C(C=C1)C(F)(F)F

Molecular Formula

C18H17ClF5N3O3S

Molecular Weight

485.86

References & Citations

[1]Moritz AE, et al. Discovery, Characterization, and Optimization of a Novel Positive Allosteric Modulator-Antagonist of the D3 Dopamine Receptor. J Med Chem. 2025 Aug 14;68 (15) :16691-16749.