MS1768
MS1768 is a G protein-biased, partial, and selective D2R agonist. MS1768 selectively activates the Gi/o signaling pathway rather than recruiting β-arrestin2. MS1768 inhibits hyperkinesia. MS1768 can be used in studies of hyperkinesia.
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- CAS No.: 2349365-88-2
- Formule: C20H30ClN3O
- Masse moléculaire:363.93
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
D2 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
11 nM
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D2R Gᵢ/ₒ-mediated cAMP inhibition activity in D2R transfected HEK293T cells co-expressing the GloSensor-22F cAMP biosensor with 15 min pre-incubation followed by 15 min incubation with isoproterenol measured by luminescence assay.
D2R Gᵢ/ₒ-mediated cAMP inhibition activity in D2R transfected HEK293T cells co-expressing the GloSensor-22F cAMP biosensor with 15 min pre-incubation followed by 15 min incubation with isoproterenol measured by luminescence assay.
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30964661 |
| HTLA | EC50 |
40 nM
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D2R-mediated β-arrestin2 recruitment activity in HTLA cells stably expressing β-arrestin-TEV protease and a tTA-driven luciferase transfected with the human D2V2-TCS-tTA construct after 20-22 h incubation measured by Tango assay with BrightGlo reagent.
D2R-mediated β-arrestin2 recruitment activity in HTLA cells stably expressing β-arrestin-TEV protease and a tTA-driven luciferase transfected with the human D2V2-TCS-tTA construct after 20-22 h incubation measured by Tango assay with BrightGlo reagent.
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30964661 |
| HEK-293T | EC50 |
0.40 nM
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D2R-mediated Gαi1-γ2 dissociation activity in HEK293T cells co-expressing Gαi1-RLuc, Gβ1, GFP2-Gγ2, and human D2long after 15 min incubation measured by BRET assay using coelenterazine 400a substrate.
D2R-mediated Gαi1-γ2 dissociation activity in HEK293T cells co-expressing Gαi1-RLuc, Gβ1, GFP2-Gγ2, and human D2long after 15 min incubation measured by BRET assay using coelenterazine 400a substrate.
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30964661 |
In Vitro
MS1768 (15 min) is a potent partial agonist of Gαi1-γ2 protein dissociation. In an in vitro BRET assay using HEK293T cells co-expressing Gαi1-RLuc, Gβ1, GFP2-Gγ2, and D2long, it exhibits an EC50 of 0.40 nM and an Emax of 47% relative to Quinpirole[1].
MS1768 (15 min) exhibits no detectable agonist activity on the D3R Gi/o-mediated cAMP inhibition pathway in HEK293T cells transfected with D3R[1].
MS1768 (20-22 h) exhibits no detectable D3R-mediated β-arrestin2 recruitment agonist activity in D3R-expressing HTLA Tango assay cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MS1768 (1-3.5 mg/kg; i.p.) almost completely inhibits phencyclidine-induced hyperlocomotion at a dose of 3.5 mg/kg, indicating its potent in vivo efficacy in a psychosis-mimetic mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57 mice[1]
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Dosage:0.32 mg/kg (s.c.); 1 mg/kg (s.c.); 3.2 mg/kg (s.c.); 10 mg/kg (s.c.); 32 mg/kg (s.c./i.v.)
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Administration:s.c.; i.v.
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Result:Exhibited dose-dependent D2R binding in mouse striatum and cerebellum.
Achieved full D2R receptor occupancy at the 32 mg/kg dose.
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Animal Model:Adult male and female C57BL/6 mice[1]
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Dosage:1 mg/kg (i.p.); 3.5 mg/kg (i.p.)
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Administration:i.p.
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Result:Significantly reduced PCP-induced hyperlocomotion at 1 mg/kg.
Almost completely suppressed the PCP-elicited hyperlocomotor response at 3.5 mg/kg.
Chemical Information
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CAS No. 2349365-88-2
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Masse moléculaire 363.93
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Formule C20H30ClN3O
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SMILES
ClC1=C2C(CCN(CC[C@H]3CC[C@H](NC(N(C)C)=O)CC3)C2)=CC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS1768 Related Classifications
HY-187696 Related Classifications
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