SCH58261 是一种强选择性的竞争性腺苷 A2A 受体拮抗剂，IC50值为 15 nM，对 A2A 受体的选择性分别是 A1、A2B 和 A3 受体的 323 倍、53 倍、100 倍。

SCH 58261 is a potent and selective A2a adenosine receptor antagonist.The Ki =2.3 nM for rat A2a and 2 nM is for bovine A2a.

SCH 58261 causes the inhibition of rabbit platelet aggregation and porcine coronary artery relaxation by antagonizing competitively the effects induced by CGS 21680. [1]

In mice with Spinal cord injury, SCH58261 (0.01 mg/kg, i.p.) reduces demyelination and levels of TNF-α, Fas-L, PAR, Bax expression and activation of JNK MAPK. Chronic SCH58261 administration improves the neurological deficit up. [2] In rats with 6-OHDA-induced Parkinson's disease, SCH58261 (2 mg/kg, i.p.) improves the 6-OHDA-induced bradykinesia and motor disturbance. [3]

160098-96-4

C18H15N7O

345.36

SCH58261

DMSO:34.5 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years