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Chemical Structure : JNJ-40255293
Catalog No.: 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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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.
| M.Wt | 402.45 | |
| Formula | C23H22N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. John R Atack, et al. ACS Chem Neurosci. 2014 Oct 15;5(10):1005-19.
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