Dopamine D3 receptor antagonist-3
Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC50 and a Kd of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder.
For research use only. We do not sell to patients.
- CAS No.: 2894793-37-2
- Formula: C18H17ClF5N3O3S
- Molecular Weight:485.86
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Dopamine Receptor Isoforms
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Biological Activity
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Dopamine D3 receptor 0.49 μM (Kd) |
Dopamine D3 receptor antagonist-3 (Compound 6a) exhibits good microsomal stability microsome stability (human/mouse/rat) and lacks activity at the hERG channel with estimated IC50 values >10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUClast | AUCinf |
|---|---|---|---|---|---|---|---|
| Mice[1] | 40 mg/kg | i.p. | 1.0 h | 28 μM | 3.97 h | 72681 ng·h/mL | 97638 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2894793-37-2
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Molecular Weight 485.86
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Formula C18H17ClF5N3O3S
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SMILES
ClC(C=C1NS(C(C(C(N(C2)CCC2(F)F)=O)=C3C)=C(N3)C)(=O)=O)=C(C=C1)C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)