RTICBM-303
RTICBM-303 is a blood-brain barrier-penetrant cannabinoid receptor type 1 (CB1) inhibitor. RTICBM-303 concentration-dependently decreases the Emax of the agonist CP55,940, increases the binding of [3H]CP55,940, and inhibits CB1 receptor signaling. RTICBM-303 selectively reduces cue-induced and drug-priming-induced drug-seeking relapse behaviors in rats. RTICBM-303 can be used in studies related to addictive behaviors.
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- Formel: C19H15FN2O3S
- Molecular Weight:370.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
hCB1 5.91 (pIC50) |
mCB1 6.24 (pIC50) |
In Vitro
RTICBM-303 (60 min) inhibits CP55,940-induced G protein activation in human CB1-expressing HEK293 cell membranes and mouse cerebellar membranes, with pIC50 values of 5.91 and 6.24, respectively[1].
RTICBM-303 positively regulates the binding of [3H]CP55,940 to cell membranes of HEK293 cells expressing human CB1, increasing the binding rate to 218% of the baseline level, with a pEC50 of 6.33[1].
RTICBM-303 exhibits low apparent permeability in MDCK-MDR1 cells, with Papp values of < 0.1 × 10-6 cm/s in both transport directions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 (Plasma) | T1/2 (Brain) | Tmax (Plasma) | Tmax (Brain) | Cmax (Brain) | Cmax |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 3.01 h | 2.36 h | 1.00 h | 1.00 h | 535 ng/g | 403 ng/mL |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 6-8 weeks old, 220-280 g, surgically implanted with jugular catheters, trained to self-administer via fixed ratio schedule, followed by 5 days of extinction training)[1]
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Dosage:10 mg/kg (cue- or drug-primed reinstatement tests)
5.6 mg/kg, 10 mg/kg (food-maintained operant responding tests) -
Administration:i.p.; single dose; 15 minutes prior (cue- or drug-primed reinstatement tests)
i.p.; single dose; 10 minutes prior (food-maintained operant responding tests) -
Result:Significantly reduced lever-pressing responses in both cue-induced and drug-primed psychostimulant reinstatement tests at 10 mg/kg.
Failed to alter food-reinforced operant response rates at 5.6 mg/kg or 10 mg/kg.
Chemical Information
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Molecular Weight 370.40
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Formel C19H15FN2O3S
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SMILES
O=S(C1=CC=C(NC(NC2=CC(C3=CC=CC=C3)=CC=C2)=O)C=C1)(F)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
RTICBM-303 Related Classifications
HY-187995 Related Classifications
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