R-185
R-185 is an orally active and brain-penetrant GPR52 agonist. R-185 activates GPR52 to increase intracellular cAMP levels. R-185 can be used for the research of schizophrenia.
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- No. CAS: 3066783-67-0
- Fòrmula: C22H19F4N5O2
- Peso molecular:461.41
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Almacenamiento:
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Actividad biológica
| Species | Dose | Route | AUC0-∞ | T1/2 | Cmax | CL | Vd | F |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | p.o. | 3232 ng·h/mL | 1.76 h | 1173 ng/mL | / | / | 130 % |
| Mice[1] | 1 mg/kg | i.v. | 496 ng·h/mL | 1.40 h | 1283 ng/mL | 33.8 mL/min/kg | 1.74 L/kg | / |
| Rat[1] | 5 mg/kg | p.o. | 2284 ng·h/mL | 3.53 h | 318 ng/mL | / | 4.40 L/kg | 67 % |
| Rat[1] | 1 mg/kg | i.v. | 680 ng·h/mL | 2.05 h | 760 ng/mL | 24.8 mL/min/kg | / | / |
R-185 (1-5 mg/kg; p.o. or i.v.; single dose) exhibits favorable pharmacokinetic characteristics in mice, crosses the blood-brain barrier, and has an oral bioavailability of 130%[1].
R-185 (1-5 mg/kg; p.o. or i.v.; single dose) exhibits favorable pharmacokinetic characteristics in rats, crosses the blood-brain barrier, and has an oral bioavailability of 67%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD mice (male, 30 g)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:p.o. or i.v.; single dose
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Result:Exihibited favorable pharmacokinetic characteristics and could cross the blood-brain barrier.
Showed F of 130%, Cmax of 1173 ng/mL, Tmax of 1.76 h and AUC0-∞ of 3232 ng·h/mL (p.o.).
Showed T1/2 of 1.40 h, CL of 33.8 mL/min/kg, Vd of 1.74 L/kg and AUC0-∞ of 496 ng·h/mL (i.v.).
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Animal Model:SD rats (male, 200-250 g)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:p.o. or i.v.; single dose
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Result:Exihibited favorable pharmacokinetic characteristics and could cross the blood-brain barrier.
Exhibited F of 67%, Cmax of 318 ng/mL, Tmax of 3.53 h and AUC0-∞ of 2284 ng·h/mL (p.o.).
Exhibited T1/2 of 2.05 h, CL of 24.8 mL/min/kg, Vd of 4.4 L/kg and AUC0-∞ of 680 ng·h/mL (i.v.).
Chemical Information
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No. CAS 3066783-67-0
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Peso molecular 461.41
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Fòrmula C22H19F4N5O2
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SMILES
FC1=CC(OC2CCN(CC2)C3=C(N=CC=N3)C(NC4=CC=NC=C4)=O)=CC(C(F)(F)F)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
R-185 Related Classifications
HY-184192 Related Classifications
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