2108826-33-9

UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity[1].

UNC9994 hydrochloride is a functionally selective, β-arrestin-biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity[1]. UNC9994 hydrochloride induces D2-mediated β-arrestin-2 translocation with an EC50s of 6.1 nM and 448 nM in Tango assay and DiscoveRx assay, respectively[1].UNC9994 hydrochloride is an antagonist at 5HT2A and 5HT2B and an agonist at 5HT2C and 5HT1A[1]. UNC9994 (2.0 mg/kg; i.p.; once) hydrochloride shows antipsychotic activity that is attenuated in β-arrestin-2 knockout mice[1].

D₃ Receptor: 17 nM (Ki); D₂ Receptor: 79 nM (Ki); D₄ Receptor: 138 nM (Ki); D₁ Receptor: 4000 nM (Ki); 5-HT_2B Receptor: 25 nM (Ki); 5-HT_1A Receptor: 26 nM (Ki); 5-HT_2A Receptor: 140 nM (Ki); 5-HT_2C Receptor: 512 nM (Ki)

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[1]. Allen JA, et al. Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy. Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18488-93.