Neuroprotective steroids

Synthesis of positive and negative modulators of NMDA receptor

N-Methyl-D-aspartate (NMDA) receptors are glutamate-gated ion channels ubiquitously distributed throughout the brain, fundamental to excitatory neurotransmission and critical for normal CNS function. Its role relates to memory functions, learning processes and mental performance. NMDA receptors are modulated by a variety of endogenous and exogenous ligands among which sulfates of some steroids represent an important group. However, their low bioavailability and poor metabolic stability limit their in vivo application. Finding a derivative that would show better pharmacological properties while keeping the activity, could greatly influence the impact on many degenerative and other neurological and psychiatric disorders that form a significant problem of the society today.