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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-JNJ-40255293
JNJ-40255293

Chemical Structure : JNJ-40255293

CAS No.: 1147271-25-7

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JNJ-40255293 (JNJ40255293)

货号: PC-20100Not For Human Use, Lab Use Only.

JNJ-40255293 (JNJ 40255293) is a potent, dual adenosine A2A/A1 receptor antagonist with Ki of 6.8/42 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    JNJ-40255293 (JNJ 40255293) is a potent, dual adenosine A2A/A1 receptor antagonist with Ki of 6.8/42 nM, respectively.
    JNJ-40255293 shows weaker affinity for A2B/A3 receptors with binding Ki of 230/9200 nM, respectively.
    JNJ-40255293 shows similar A2A:A1 selectivity (7-fold) in vivo (ED50s of 0.21 and 2.1 mg/kg p.o. for occupancy of rat brain A2A and A1 receptors, respectively).
    JNJ-40255293 dose-dependently enhanced a consolidated waking associated with a subsequent delayed compensatory sleep (EC50= 0.63 mg/kg p.o.) in sleep–wake encephalographic (EEG) studies.
    JNJ-40255293 did not affect dopamine and noradrenaline release in the prefrontal cortex and the striatum.
    JNJ-40255293 potentiated the agitation induced by the dopamine agonist apomorphine.
    JNJ-40255293 also reversed hypolocomotion produced by the dopamine-depleting agent reserpine and potentiated the effects of l-dihydroxyphenylalanine (L-DOPA) in rats.

    物理化学性质&存储条件

    分子量 402.45
    分子式 C23H22N4O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    2-amino-8-[2-(4-morpholinyl)ethoxy]-4-phenyl-5H-indeno[1,2-d]pyrimidin-5-one

    参考文献

    1. John R Atack, et al. ACS Chem Neurosci. 2014 Oct 15;5(10):1005-19.

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