UNC9994 hydrochloride

Names

[ Name ]:
UNC9994 hydrochloride

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

D2 Receptor:79 nM (Ki)

D1 Receptor:4000 nM (Ki)

D3 Receptor:17 nM (Ki)

D4 Receptor:138 nM (Ki)

5-HT2A Receptor:140 nM (Ki)

5-HT2B Receptor:25 nM (Ki)

5-HT2C Receptor:512 nM (Ki)

5-HT1A Receptor:26 nM (Ki)

[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[1]. UNC9994 hydrochloride is an antagonist at 5HT2A and 5HT2B and an agonist at 5HT2C and 5HT1A[1].

[In Vivo]

UNC9994 (2.0 mg/kg; i.p.; once) hydrochloride shows antipsychotic activity that is attenuated in β-arrestin-2 knockout mice[1]. Animal Model: C57BL/6J wild-type and β-arrestin-2 knockout mice[1] Dosage: 2.0 mg/kg, followed 30 min later with 6 mg/kg phencyclidine (PCP, i.p.) Administration: IP, once Result: Markedly inhibited PCP-induced hyperlocomotion in wild-type mice and the activity was completely abolished in β-arrestin-2 knockout mice.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₂₃Cl₃N₂OS

[ Molecular Weight ]:
457.84

Related Compounds

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