ST4206 |
رقم الكتالوجGC31256 |
ST4206 هو أحد مضادات مستقبلات الأدينوزين A2A القوية والفعالة عن طريق الفم ، مع Kis من 12 نانومتر و 197 نانومتر لمستقبل الأدينوزين A2A ومستقبل الأدينوزين A1 ، على التوالي
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Cas No.: 1246018-36-9
Sample solution is provided at 25 µL, 10mM.
ST4206 is a potent adenosine A2A antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively.
ST4206 inhibits agonist-induced cAMP accumulation with an IC50 of 990 nM[1].
ST4206 (10, 20, and 40 mg/kg, p.o.) antagonizes haloperidol-induced catalepsy, and increases motor activity in a dose dependent manner in mice. ST4206 (20 and 40 mg/kg) significantly increases the number of contralateral turns induced by l-DOPA in rats[1]. ST4206 is orally active at concentrations of 10, 20, and 40 mg/kg in haloperidol-induced catalepsy in mice[2].
[1]. Stasi MA, et al. Animal models of Parkinson?s disease: Effects of two adenosine A2A receptor antagonists ST4206 and ST3932, metabolites of 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535). [2]. de Lera Ruiz M, et al. Adenosine A2A receptor as a drug discovery target. J Med Chem. 2014 May 8;57(9):3623-50.
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