1354030-51-5
1354030-51-5 structure
- Name: UNC9994
- Chemical Name: UNC9994
- CAS Number: 1354030-51-5
- Molecular Formula: C21H22Cl2N2OS
- Molecular Weight: 421.38
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2021-09-11 08:52:13
- Modify Date: 2024-01-09 06:54:35
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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].
| Name | UNC9994 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
D2 Receptor:79 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-HT1F Receptor:26 nM (Ki) H1-histamine receptor:2.4 nM (Ki) H1-histamine receptor:79 (pA2) |
| In Vitro | 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: C57BL/6J wild-type and β-arrestin-2 knockout mice (phencyclidine-induced hyperlocomotion)[1] 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. |
| References |
| Molecular Formula | C21H22Cl2N2OS |
|---|---|
| Molecular Weight | 421.38 |