RWJ-51204

Research use only, not for human use.

RWJ-51204 is a selective adenosine A2A receptor antagonist and a partial agonist of GABA(A) receptor (IC50: 0.2-2 nM).

RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

RWJ-51204 binds to receptors in the cerebral cortex, cerebellum, or medulla-spinal cord with Ki ranging from 0.2 to 0.6 nM.

RWJ-51204 is orally active in anxiolytic efficacy tests. WJ 51204 dose-relatedly antagonizes PTZ-induced clonic convulsions when administered orally (ED50 = 0.04 mg/kg). RWJ-51204 is effective in the conflict test in monkeys (ED50 of approximately 0.5 mg/kg p.o.). RWJ-51204 potently impairs rotarod performance in rats (ED50 = 0.12 mg/kg), and all rats given RWJ-51204 orally at 30 mg/kg exhibit sedation, reduced skeletal muscle tone, and impairment of rotarod performance.

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Others

Other Targets

GABA Receptor

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205701-85-5

399.39

C21H19F2N3O3

>98% (HPLC)

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C(OCC)N1C=2N(C=3C1=CC(F)=CC3)CCC(=O)C2C(NC4=C(F)C=CC=C4)=O

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(-20℃)

With Ice Pack

≥ 2 years