ZM 241385

ZM 241385 is a potent, selective adenosine A_2A receptor inverse agonist (K_i values are <1, 50, 255 nM and >10 µM at A_2A, A_2B, A₁ and A₃ receptors respectively).

The crystal structure of the human A_2A receptor was determined in complex with ZM 241385.

Activation of the A_2A receptor enhances the release of glutamate, dopamine and acetylcholine and also inhibits GABA release.

The A_2AR has been shown to interact with various receptors including the mGlu₅, D2R, A1R and CB1 receptors.

A_2A receptor activation modulates synaptic plasticity and neuronal excitability.

ZM 241385 is active in vivo.