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编 号：F683051
分子式：C21H22Cl2N2OS
分子量：421.38
分子式：C21H22Cl2N2OS
分子量：421.38
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CAS No: 1354030-51-5
产品详情
生物活性：
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.
体内研究：
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.Animal Model:C57BL/6J wild-type and β-arrestin-2 knockout mice (phencyclidine-induced hyperlocomotion)
Dosage:2 mg/kg
Administration:I.p. followed 30 min later with 6 mg/kg phencyclidine
Result:Markedly inhibited PCP-induced hyperlocomotion in wild-type mice. This significant antipsychotic-like activity of UNC9994 was completely abolished in β-arrestin-2 knockout mice.
体外研究：
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.
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.
体内研究：
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.Animal Model:C57BL/6J wild-type and β-arrestin-2 knockout mice (phencyclidine-induced hyperlocomotion)
Dosage:2 mg/kg
Administration:I.p. followed 30 min later with 6 mg/kg phencyclidine
Result:Markedly inhibited PCP-induced hyperlocomotion in wild-type mice. This significant antipsychotic-like activity of UNC9994 was completely abolished in β-arrestin-2 knockout mice.
体外研究：
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.
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