| Identification | Back Directory | [Name]
Benzothiazole, 5-[3-[4-(2,3-dichlorophenyl)-1-piperidinyl]propoxy]-, hydrochloride (1:1) | [CAS]
2108826-33-9 | [Synonyms]
Benzothiazole, 5-[3-[4-(2,3-dichlorophenyl)-1-piperidinyl]propoxy]-, hydrochloride (1:1) | [Molecular Formula]
C21H23Cl3N2OS | [MOL File]
2108826-33-9.mol | [Molecular Weight]
457.84 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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]. | [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. |
| [IC 50]
D3 Receptor: 17 nM (Ki); D2 Receptor: 79 nM (Ki); D4 Receptor: 138 nM (Ki); D1 Receptor: 4000 nM (Ki); 5-HT2B Receptor: 25 nM (Ki); 5-HT1A Receptor: 26 nM (Ki); 5-HT2A Receptor: 140 nM (Ki); 5-HT2C Receptor: 512 nM (Ki) | [storage]
4°C, away from moisture | [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. |
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