For research use only. Not for therapeutic Use.
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats[1].
RTICBM-189 (10 mg/kg; i.p.) rapidly absorbs into systemic circulation, with peak plasma concentration (Cmax,plasma=288.4 ng/mL) observed at tmax,plasma of 0.4 h post-dose. Peak brain levels are also reached at tmax,brain of 0.4 h with a significantly higher Cmax,brain value of 594.6 ng/mL in the brain[1].
| Catalog Number | I045161 |
| CAS Number | 551909-15-0 |
| Synonyms | 1-(4-chlorophenyl)-3-[2-(3-chlorophenyl)ethyl]urea |
| Molecular Formula | C15H14Cl2N2O |
| Purity | ≥95% |
| InChI | InChI=1S/C15H14Cl2N2O/c16-12-4-6-14(7-5-12)19-15(20)18-9-8-11-2-1-3-13(17)10-11/h1-7,10H,8-9H2,(H2,18,19,20) |
| InChIKey | PPKIPROVSKBYAT-UHFFFAOYSA-N |
| SMILES | C1=CC(=CC(=C1)Cl)CCNC(=O)NC2=CC=C(C=C2)Cl |
| Reference | [1]. Nguyen T, et al. Development of 3-(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type-1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior [published online ahead of print, 2021 Dec 20]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01432. |
