产品
编 号：F753670
分子式：C17H19ClFN5O3
分子量：395.82
分子式：C17H19ClFN5O3
分子量：395.82
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CAS No: 2550400-52-5
产品详情
生物活性：
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases.
体内研究：
Adenosine receptor inhibitor 1 (20, 30, 40 mg/kg; i.p.) shows antinociceptive activity at a concentration-dependent mannner.Adenosine receptor inhibitor 1 (20 mg/kg; i.p.) shows anti-inflammatory effect in carrageenan-induced edema model.Adenosine receptor inhibitor 1 (5, 10, 20 mg/kg; i.p.) shows analgesic effect in mouse.Animal Model:18-26 g male albino Swiss mice (chronic pain induced by the administration of 5% formalin)
Dosage:20, 30, 40 mg/kg
Administration:I.p.
Result:Showed antinociceptive activity with decreasesed the licking/biting time of the right hind paw of mice in response to the irritating chemical stimulus.
Animal Model:150-180 g male rats Wistar(carrageenan-induced edema model)
Dosage:20 mg/kg
Administration:I.p.
Result:Showed anti-inflammatory effect with the inhibition of 23.3%, 54.2%, 66.0% at 1h, 2h, 3h, respectively.
Animal Model:Mouse (induce pain of peripheral origin by injection of an irritant like phenylbenzoquinone or acetic acid in mice)
Dosage:5, 10, 20 mg/kg
Administration:I.p.
Result:Showed peripheral analgesic effect with the significant decrease in the number of writhings by 32.9%, 54.9%, 82.0% at doses of 5, 10, 20 mg/kg, respectively.
体外研究：
Adenosine receptor inhibitor 1 (compound 12d) (120 min) shows metabolic stability incubated with with 96.56 and 97.97% of the parent compound remained in the reaction mixtures after incubation with mouse (MLMs) and rat liver microsomes (RLMs), respectively.
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases.
体内研究：
Adenosine receptor inhibitor 1 (20, 30, 40 mg/kg; i.p.) shows antinociceptive activity at a concentration-dependent mannner.Adenosine receptor inhibitor 1 (20 mg/kg; i.p.) shows anti-inflammatory effect in carrageenan-induced edema model.Adenosine receptor inhibitor 1 (5, 10, 20 mg/kg; i.p.) shows analgesic effect in mouse.Animal Model:18-26 g male albino Swiss mice (chronic pain induced by the administration of 5% formalin)
Dosage:20, 30, 40 mg/kg
Administration:I.p.
Result:Showed antinociceptive activity with decreasesed the licking/biting time of the right hind paw of mice in response to the irritating chemical stimulus.
Animal Model:150-180 g male rats Wistar(carrageenan-induced edema model)
Dosage:20 mg/kg
Administration:I.p.
Result:Showed anti-inflammatory effect with the inhibition of 23.3%, 54.2%, 66.0% at 1h, 2h, 3h, respectively.
Animal Model:Mouse (induce pain of peripheral origin by injection of an irritant like phenylbenzoquinone or acetic acid in mice)
Dosage:5, 10, 20 mg/kg
Administration:I.p.
Result:Showed peripheral analgesic effect with the significant decrease in the number of writhings by 32.9%, 54.9%, 82.0% at doses of 5, 10, 20 mg/kg, respectively.
体外研究：
Adenosine receptor inhibitor 1 (compound 12d) (120 min) shows metabolic stability incubated with with 96.56 and 97.97% of the parent compound remained in the reaction mixtures after incubation with mouse (MLMs) and rat liver microsomes (RLMs), respectively.
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