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编 号:F740941
分子式:C15H14Cl2N2O
分子量:309.19
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
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.

体内研究:
RTICBM-189 (10 mg/kg;腹腔注射)迅速吸收进入体循环,在给药后 0.4 小时的 tmax,plasma 观察到峰值血浆浓度 (Cmax,plasma=288.4 ng/mL)。大脑峰值水平也在 0.4 小时 (tmax,brain) 时达到,Cmax,brain 为 594.6 ng/mL。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: Cmax (288.4 ng/mL), tmax (0.4 hours), CL_F (240.6 mL/min/kg), AUCinf (715.2 ng/mL × h), half-life t1/2 (9.9 hours).Brain: Cmax (594.6 ng/mL), tmax (0.4 hours), CL_F (120.7 mL/min/kg), AUCinf (1438.2 ng/mL × h).
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