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Novel NMDA receptor antagonists, potent CNS therapeutics

INTRODUCTION: 
Searching for novel drugs potentially useful for therapy of CNS damage belongs to the most investigated topics in contemporary pharmacology and neurosciences. A number of studies demonstrated a neuroprotective ability of NMDA receptor antagonists. Nonetheless, their therapeutic potential is rather limited due to severe negative side effects.

TECHNOLOGY (INVENTION) DESCRIPTION: 
New, innovative neurosteroids, derivatives of pregnanolone and androstane, were synthesized and tested. In vitro, they reveal use-dependent inhibition of NMDA receptor, a promising attribute of neuroprotective properties. In vivo, they reveal antidepressant, anti-convulsive, anxiolytic and pro-cognitive properties without typical negative side effects of NMDA receptor antagonists. They penetrate the blood brain barrier very fast and are bio-available after per-oral administration.

ADVANTAGES OVER EXISTING SOLUTIONS: 
Our compounds show absence of side effects in animal models compared to commercially available drugs. Low toxicity in vitro and in vivo has been observed

DEVELOPMENT STATUS (STAGE): 
Early preclinical stage, in vitro and in vivo testing, lead structure optimization, pharmacokinetics, behavioral tests

PUBLICATIONS: 
Rambousek L., et al. Neuropharmacology. 2011; 61(1-2): 61-8 Vales K., et al. Behav Brain Res. 2012; 235(1):82-8

IP PROTECTION STATUS: 
PCT/CZ2009/000091, PCT/CZ10/000065, PCT/CZ12/000016

TECHNOLOGY / IP OWNERS : 
Institute of Organic Chemistry and Biochemistry AS CR, v.v.i. Institute of PhysiologyAS CR, v.v.i.