Dopamine D3 receptor agonist-3
Dopamine D3 receptor agonist-3 is a selective, partial, blood-brain barrier-penetrant dopamine D3 receptor (D3R) agonist with a Ki of 2.7 nM for hD3R. Dopamine D3 receptor agonist-3 can be used for research on central nervous system-related diseases.
For research use only. We do not sell to patients.
- Formula: C28H33Cl2N5O3
- Molecular Weight:558.50
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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
Description
IC50 & Target
[1]|
Human D3 Receptor 2.7 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
1.3 nM
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Agonist activity at human D3R expressed in CHO cells assessed as cAMP accumulation by HTRF after 30 min at 37°C.
Agonist activity at human D3R expressed in CHO cells assessed as cAMP accumulation by HTRF after 30 min at 37°C.
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42664598 |
| CHO | IC50 |
0.7 nM
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Antagonist activity at human D3R expressed in CHO cells assessed as inhibition of dopamine-induced cAMP accumulation by HTRF after 5 min preincubation at room temperature followed by 30 min at 37°C.
Antagonist activity at human D3R expressed in CHO cells assessed as inhibition of dopamine-induced cAMP accumulation by HTRF after 5 min preincubation at room temperature followed by 30 min at 37°C.
|
42664598 |
In Vitro
Dopamine D3 receptor agonist-3 (30 min) is a partial agonist of hD3R expressed in CHO cells, with an EC50 of 1.3 nM, an Emax of 56% relative to dopamine, and inhibits dopamine-induced signaling with an IC50 of 0.7 nM[1].
Dopamine D3 receptor agonist-3 (50-250 μM; 1 h) showed high BBB permeability in PAMPA, with a log10 Papp of -4.30 cm/s[1].
Dopamine D3 receptor agonist-3 (1 μM; 120 min) is highly stable in rat plasma, with 86% remaining after 2 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 558.50
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Formula C28H33Cl2N5O3
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SMILES
CC1=C(N(C)C(NC1=O)=O)C2=CC=C(C(NCCCCN3CCN(C4=C(Cl)C(Cl)=CC=C4)CC3)=O)C=C2C
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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)