Abstract::
N-Methyl-D-aspartate (NMDA) receptors together with AMPA and kainite receptors belongs to the family of
ionotropic glutamate receptors. NMDA receptors plays a crucial role in neuronal plasticity and cognitive functions.
Overactivation of those receptors leads to glutamate induced excitotoxicity, which could be suppressed by NMDA
antagonists. Dizocilpine was firstly reported in 1982 as a NMDA receptor antagonist with anticonvulsive properties, but due
to serious side effects like neuronal vacuolization, its use in human medicine is restricted. However, dizocilpine is still used
as validated tool to induce the symptoms of schizophrenia in animal models and also as a standart for comparative purposes
to newly developed NMDA receptor antagonists. For this reason, synthesis of dizocilpine and specially its more active
enantiomer (+)-dizocilpine is still relevant. In this review we bring a collection of various synthetic approaches leading to
dizocilpine and its analogues.