FMJ-01-054
FMJ-01-054 is a selective dopamine D4 Receptor (D4R) antagonist with a Ki od 77.7 nM. FMJ-01-054 shows subtype selectivity over D2R and D3R. FMJ-01-054 inhibits D4R-mediated β-arrestin recruitment and cAMP production with IC50 values of 3800 nM and 134 nM, respectively. FMJ-01-054 has desirable plasma half-life and brain exposure in rats. FMJ-01-054 can be used for the research of neurological disorders.
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- Formule: C19H21ClN6
- Masse moléculaire:368.86
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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
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Human D4 Receptor 77.7 nM (Ki) |
Human D2 Receptor >100,000 nM (Ki) |
Human D3 Receptor >100,000 nM (Ki) |
In Vitro
FMJ-01-054 (compound 17) (0.3 nM-100 μM; 1 h) binds to the human dopamine D4 receptor with high affinity (Ki = 77.7 nM) and >1287-fold selectivity over D2 and D3 receptors[1].
FMJ-01-054 acts as an antagonist at the human dopamine D4 receptor with an IC50 of 3800 nM and has no agonist activity[1].
FMJ-01-054 (30 min) inhibits dopamine D4 receptor-mediated cAMP production as an antagonist with an IC50 of 134 nM[1].
FMJ-01-054 exhibits metabolic stability in rat and human liver microsomes with half-lives of 64.77 min and 46.84 min, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Tmax | Brain-to-Plasma Ratio |
|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.p. | 0.25 h | 0.3 |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 368.86
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Formule C19H21ClN6
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SMILES
CC1=CC(N2N=NC(CN3CCN(C4=NC=C(Cl)C=C4)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)
FMJ-01-054 Related Classifications
HY-181049 Related Classifications
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Keywords
- FMJ-01-054
- Dopamine Receptor
- rats
- substance use disorders
- D3R
- amide analogs
- human dopamine D? receptor
- blood-brain barrier
- D4R
- schizophrenia
- Sprague?Dawley rats
- l-dopa-induced dyskinesias
- Dopamine D4 Receptor
- D2R
- attention-deficit/hyperactivity disorder
- cAMP
- β-arrestin recruitment
- human liver microsomes
- rat liver microsomes
- Inhibitor
- inhibitor
- inhibit