UNC9994 hydrochloride

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CAS NO:

2108826-33-9

UNC9994 hydrochloride 是一种功能选择性的 β-arrestin 偏向的多巴胺 D₂受体 (D₂R) 激动剂，可选择性激活 β- arresttin 招募和信号转导。对D₂R的K_i值为 79 nM。UNC9994 hydrochloride 也是 G_i调节 cAMP 产生的拮抗剂和 D2R/β-arrestin-2 相互作用的部分激动剂。UNC9994 hydrochloride 具有稳定精神效果。

生物活性

UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamineD₂receptor(D₂R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with aK_iof 79 nM forD₂R. 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^[1].

IC₅₀& Target

D₂Receptor

79 nM (Ki)

D₁Receptor

4000 nM (Ki)

D₃Receptor

17 nM (Ki)

D₄Receptor

138 nM (Ki)

5-HT_2AReceptor

140 nM (Ki)

5-HT_2BReceptor

25 nM (Ki)

5-HT_2CReceptor

512 nM (Ki)

5-HT_1AReceptor

26 nM (Ki)

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^[1].
UNC9994 hydrochloride is an antagonist at 5HT_2Aand 5HT_2Band an agonist at 5HT_2Cand 5HT_1A^[1].

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^[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.

分子量

457.84

性状

Solid

Formula

C₂₁H₂₃Cl₃N₂OS

CAS 号

2108826-33-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)