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.
For research use only. We do not sell to patients.
- CAS No.: 2130881-32-0
- Formula: C19H14ClFN2O
- Molecular Weight:340.78
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CB1 23 nM (IC50) |
CB1 153 nM (IC50) |
In Vitro
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. Further protocols information, click here.
Parmacokinetics
| 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 |
In Vivo
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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Molecular Weight 340.78
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Formula 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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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RTICBM-74 Related Classifications
HY-182697 Related Classifications
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