RTICBM-189 is a potent, selective, brain-penetrant CB1 negative allosteric modulator (NAM) with pIC50 of 7.54 in Ca2+ assay, 5.29 in GTPγS assay.
RTICBM-189 shows no activity at >50 protein targets and excellent brain permeation but relatively low metabolic stability in rat liver microsomes.
RTICBM-189 (10 mg/kg, i.p.) significantly and selectively attenuated the reinstatement of the cocaine-seeking behavior in rats without affecting locomotion.
Physicochemical Properties
M.Wt
309.19
Formula
C15H14Cl2N2O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
1-(3-chlorophenethyl)-3-(4-chlorophenyl)urea
References
1. Nguyen T, et al. J Med Chem. 2022 Jan 13;65(1):257-270.
