RTICBM-74
RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder.
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- CAS No.: 2130881-32-0
- Formule: C19H14ClFN2O
- Masse moléculaire:340.78
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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
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CB1 23 nM (IC50) |
CB1 153 nM (IC50) |
RTICBM-74 (1 μM; 15-240 min) exhibits excellent metabolic stability in hepatocytes of male Sprague-Dawley rats, with a half-life of 461 min and an intrinsic clearance rate of 14.5 mL/min/kg[1].
RTICBM-74 (1 μM; 6 h) binds highly to rat plasma proteins, with a binding rate of 99.9% under equilibrium conditions[1].
RTICBM-74 exhibits excellent metabolic stability in rat liver microsomes, with a half-life exceeding 300 min and an intrinsic clearance of less than 4.6 mL/min/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax (Plasma) | CL/F | AUCinf | Cmax (Brain) | Tmax (Brain) |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 70.2 (Plasma) ng/mL | 6.0 (Plasma) h | 119.4 (Plasma) mL/min/kg | 1476.2 (Plasma) ng·h/mL | 272.0 ng/mL | 4.5 (Brain) h |
RTICBM-74 (i.p.; single administration, dose 7.5-10 mg/kg) specifically reduces voluntary alcohol intake behavior in male Wistar rats without inducing motor impairment[1].
RTICBM-74 (i.p.; single administration, dose 7.5-10 mg/kg) has no effect on sucrose self-administration or spontaneous activity in male Wistar rats, confirming the specificity of its alcohol intake-reducing effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long-Evans (female, adult, alcohol self-administration trained via sucrose fading on fixed ratio 2 schedule for ~4 months)[1]
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Dosage:5 mg/kg; 7.5 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Significantly reduced alcohol lever responses (F(3, 30) = 7.90; P < 0.0001).
Reduced alcohol intake from vehicle 0.53 g/kg to 0.40 g/kg (5 mg/kg), 0.42 g/kg (7.5 mg/kg), and 0.17 g/kg (10 mg/kg) (F(3,30) = 9.18; P<0.001).
Reduced alcohol lever responses in the first 5 minutes of the session at 7.5 and 10 mg/kg doses.
Reduced alcohol lever responses from the second 5-minute bin onward at all three doses.
Reduced locomotor rate and sucrose lever responses from vehicle 7.90 mL/kg to 5.38 mL/kg (10 mg/kg) (F(3,30) = 5.52; P<0.01).
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Animal Model:Wistar (male, adult, alcohol self-administration trained via sucrose fading on fixed ratio 2 schedule for ~4 months)[1]
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Dosage:7.5 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Significantly reduced alcohol lever responses (F(2, 20) = 4.79; P < 0.05).
Reduced alcohol intake from vehicle 0.65 g/kg to 0.43 g/kg (7.5 mg/kg) and 0.44 g/kg (10 mg/kg) (F(2,20) = 4.07; P<0.01).
Reduced alcohol lever responses at the 15-minute time bin at 7.5 mg/kg dose.
Reduced alcohol lever responses at the 20, 25, and 30-minute time bins at 10 mg/kg dose.
Caused no changes to locomotor rate or inactive lever presses.
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Animal Model:Wistar (male, adult, sucrose self-administration trained on fixed ratio 2 schedule)[1]
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Dosage:7.5 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Caused no significant effects on sucrose lever responses.
Caused no significant effects on sucrose intake (vehicle: 12.28 mL/kg; 7.5 mg/kg: 10.88 mL/kg; 10 mg/kg: 8.37 mL/kg; F(2,20) = 1.96; P<0.05).
Caused no changes to locomotor rate or inactive lever presses.
Chemical Information
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CAS No. 2130881-32-0
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Masse moléculaire 340.78
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Formule C19H14ClFN2O
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SMILES
O=C(NC1=CC(C2=CC=C(F)C=C2)=CC=C1)NC3=CC=C(C=C3)Cl
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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)
RTICBM-74 Related Classifications
HY-182697 Related Classifications
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