ST-1535是腺苷A(2A)受体拮抗剂,具有神经保护和抗炎作用。
产品描述
ST-1535 is a neuroprotective and anti-inflammatory effects of the adenosine A(2A) receptor antagonist.
体外活性
ST-1535 competitively antagonizes the effects of the A2A adenosine agonist NECA on cAMP in cells cloned with the human A2A adenosine receptor (IC50=353+/-30 nM), and the effects of the A1 adenosine agonist CHA on cAMP in cells cloned with the human A1 adenosine receptor (IC50=510+/-38 nM). [1]
体内活性
ST 1535, at oral doses of 5 and 10 mg/kg, antagonizes catalepsy induced by intracerebroventricular administration of the A2A adenosine agonist CGS 21680 (10 microg/5 microl) in mice. At oral doses ranging between 5 and 20 mg/kg, ST 1535 induces hypermotility and antagonizes haloperidol-induced catalepsy in mice up to 7 h. Oral ST 1535, at 1.25 and 2.5 mg/kg, potentiates L-dopa effects in reducing haloperidol-induced catalepsy. [1]
Cas No.
496955-42-1
分子式
C12H16N8
分子量
272.31
储存和溶解度
DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years