RTICBM-189

RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB 1 ) receptor with a pIC 50 of 7.54 in Ca 2+ mobilization assay. RTICBM-189 has pIC 50 s of 5.29 and 6.25 for hCB 1 and mCB 1 , respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats In Vivo RTICBM-189 (10 mg/kg; i.p.) rapidly absorbs into systemic circulation, with peak plasma concentration (C max,plasma =288.4 ng/mL) observed at t max,plasma of 0.4 h post-dose. Peak brain levels are also reached at t max,brain of 0.4 h with a significantly higher C max,brain value of 594.6 ng/mL in the brain . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult male Sprague-Dawley rats weighing 280-300 g Dosage: 10 mg/kg Administration: IP Result: Significantly attenuated drug-induced reinstatement of the cocaine-seeking behavior. Animal Model: Male Sprague-Dawley rats weighing 258-277 g Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: IP Result: Plasma: C max (288.4 ng/mL), t max (0.4 hours), CL_F (240.6 mL/min/kg), AUC inf (715.2 ng/mL × h), half-life t 1/2 (9.9 hours). Brain: C max (594.6 ng/mL), t max (0.4 hours), CL_F (120.7 mL/min/kg), AUC inf (1438.2 ng/mL × h). Form:Solid IC50& Target:CB1 7.54 (pIC 50 ) hCB 1 5.29 (pIC 50 ) mCB 1 6.25 (pIC 50 )

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet