General description

A blood-brain barrier-permeant indenopyrimidinone compound that acts as a dual A₁/A_2A antagonist (K_i = 48.2 and 6.5 nM, respectively, against agonist-induced cAMP response in A₁- or A_2A-expressing CHO-K1 cells) and effectively reverses neuroleptic D₂ receptor antagonist haloperidol- (1 mg/kg; s.c.) induced catalepsy in both mice (by 85% and 100%, respectively, with 0.1 mg/kg or 1 mg/kg oral dosage 30 min after haloperidol) and rats (by 88% and 97%, respectively, with 1 mg/kg or 10 mg/kg oral dosage) in vivo by simultaneously reversing A₁-mediated inhibition of DA (Dopamine) release and A_2A-dependent inhibition of D₂ receptor response to DA.

The Adenosine A_2A/A₁ Receptor Antagonist controls the biological activity of Adenosine A_2A/A₁ Receptor. This small molecule/inhibitor is primarily used for Biochemicals applications.

A blood-brain barrier-permeant indenopyrimidinone that acts as a dual A₁/A_2A antagonist (K_i = 48.2 and 6.5 nM, respectively, against agonist-induced cAMP response in A₁- or A_2A-expressing CHO-K1 cells) and effectively reverses D₂ antagonist haloperidol- (1 mg/kg; s.c.) induced catalepsy in both rats and mice (ED₅₀ = 0.3 and ﹤0.1 mg/kg, respectively) in vivo by simultaneously reversing A₁-mediated inhibition of DA (Dopamine) release and A_2A-dependent inhibition of D₂ receptor response to DA.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Shook, B.C., et al. 2012. J. Med. Chem.55, 1402.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)