Adenosine receptor inhibitor 1 是一种有效的选择性腺苷受体 (adenosine receptor (AR)) 抑制剂，A1AR、A2AAR、A2BAR、A3AR 的Ki值 分别为 >1000, 68.5, >1000, >1000 nM。Adenosine receptor inhibitor 1 显示出镇痛活性、抗炎作用和外周镇痛作用。Adenosine receptor inhibitor 1具有研究癌症或神经退行性疾病的潜力。
| 生物活性 | Adenosine receptorinhibitor 1 is a potent and selectiveadenosine receptor(AR)inhibitor withKivalues of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively.Adenosine receptorinhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect.Adenosine receptorinhibitor 1 has the potential for the research ofcanceror neurodegenerative diseases[1]. |
| IC50& Target[1] | A1AR >1000 nM (Ki) | A2AR 68.5 nM (Ki) | hA2B >1000 nM (Ki) | Adenosine A3receptor >1000 nM (Ki) |
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体外研究
(In Vitro) | 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[1].
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体内研究
(In Vivo) | Adenosine receptor inhibitor 1 (20, 30, 40 mg/kg; i.p.) shows antinociceptive activity at a concentration-dependent mannner[1].
Adenosine receptor inhibitor 1 (20 mg/kg; i.p.) shows anti-inflammatory effect in carrageenan-induced edema model[1].
Adenosine receptor inhibitor 1 (5, 10, 20 mg/kg; i.p.) shows analgesic effect in mouse[1].
| Animal Model: | 18-26 g male albino Swiss mice (chronic pain induced by the administration of 5% formalin)[1] | | 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)[1] | | 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)[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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