UNC9994_product_DataBase

Bioactivity	UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity[1].
Invitro	UNC9994 displays a lower binding affinity (Ki=79 nM) to D2R than UNC9975, UNC0006, and aripiprazole. At serotonin (as known as 5-HT) receptors, UNC9994 displays moderate to high binding affinities (Ki=25-512 nM) for 5HT2A, 5HT2B, 5HT2C, and 5HT1A, but is significantly less potent in functional assays (Ca2+ mobilization FLIPR or cAMP biosensor). UNC9994 is an antagonist at 5HT2A and 5HT2B and agonists at 5HT2C and 5HT1A. UNC9994 has relatively high affinities to H1-histamine receptor (Ki=2.4 nM) but is less potent antagonists in H1 functional assays[1].
In Vivo	The antipsychotic-like activity displayed by UNC9994 (2 mg/kg; i.p.) in wild-type mice is completely abolished in β-arrestin-2 knockout mice[1]. Animal Model:
Name	UNC9994
CAS	1354030-51-5
Formula	C21H22Cl2N2OS
Molar Mass	421.38
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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;108(45):18488-18493.

PeptideDB

UNC9994

CAS: 1354030-51-5 F: C21H22Cl2N2OS W: 421.38