UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D 2 receptor (D 2 R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a K i of 79 nM for D 2 R. UNC9994 hydrochloride is also an antagonist of G i -regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.
性状
Solid
IC50 & Target[1][2]
D3 Receptor 17 nM (Ki) D2 Receptor
体外研究(In Vitro)
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.UNC9994 hydrochloride is an antagonist at 5HT2A and 5HT2B and an agonist at 5HT2C and 5HT1A. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
UNC9994 (2.0 mg/kg; i.p.; once) hydrochloride shows antipsychotic activity that is attenuated in β-arrestin-2 knockout mice. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: C57BL/6J w
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[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.