DMPX

DMPX (3,7-Dimethyl-1-propargylxanthine) is a selective A_2A adenosine receptor (A_2A AR) antagonist that crosses the blood-brain barrier, with a K_i of 11 μM for rat A₂ adenosine receptor and a K_i of 45 μM for rat A₁ adenosine receptor. By blocking A2A receptors in specific brain regions, DMPX protects dopaminergic and GABAergic neurons from mitochondrial dysfunction. DMPX is applicable to research related to depression, Parkinson's disease and Huntington's disease^[1][2][3]. In Vivo:Co-administration of DMPX (3 mg/kg; i.p.; single dose) with Agomelatine (HY-17038) or Tianeptine (HY-90003) produces synergistic antidepressant-like effects in mouse behavioral despair tests. These effects correlate with increased brain concentrations of the co-administered antidepressants, without altering spontaneous locomotor activity^[1].
DMPX (0.032-10 mg/kg; 9.9 μmol/kg; i.p.; single administration) is a potent and selective in vivo A₂ adenosine receptor antagonist. It is 57 times more potent at blocking NECA-induced hypothermia than CHA (HY-18939)-induced hypothermia, and 11 times more potent at blocking NECA (HY-103173)-induced motor inhibition than CHA-induced motor inhibition. In addition, its intrinsic motor stimulant potency (ED₅₀ = 9.9 μmoL/kg) is slightly higher than that of caffeine^[2].
DMPX (5 mg/kg; i.p.; single administration) significantly attenuates the malonate-induced depletion of striatal dopamine and tyrosine hydroxylase (TH). In rats, DMPX also completely blocks malonate-induced striatal GABA loss^[3].