Subtype-Selective, Positive and Negative Allosteric Modulators of NMDA Receptors
University of Nebraska System: University of Nebraska Medical Center
posted on 01/03/2011
This new subtype-selective library of NMDA modulating compounds provides the basis for the generation of therapeutics to treat a variety of neurological conditions with decreased side effects compared to current NMDA receptor-based therapeutics.
Advantages
Subtype selective compounds should yield therapeutics with fewer side effects
Library consists of both antagonist and potentiating compounds
Useful for treating a variety of neurological and psychiatric conditions
Detailed Description
N-methyl-D-aspartate (NMDA) receptors are glutamate gated ion channel receptors that play critical roles in synaptic transmission, synaptic plasticity, learning, and memory. NMDA receptors are also involved in various pathological conditions such as epilepsy, schizophrenia, neuropathic pain, and neurodegenerative disorders. Due to their role in these diseases, a variety of NMDA receptor-based therapeutics have been developed and tested in both pre-clinical and clinical studies. However, the majority of these drugs have had very disappointing results due to adverse side effects and limited efficacy. To overcome this problem researchers at the University of Nebraska Medical Center and the University of Bristol have created a library of subtype selective NMDA receptor compounds that have a novel allosteric modulator mechanism of action. This library consists of both NMDA receptor antagonists and NMDA receptor potentiators. Antagonists could be useful for blocking epilepsy, neuropathic pain and preventing death of neurons in neurodegenerative diseases while the potentiators could have use in cognitive enhancement and the treatment of schizophrenia, post-traumatic stress syndrome, and drug addiction.
File Number: 231
Web site: http://www.unemed.com
Disease: Central Nervous System
This innovation currently is not available for online licensing. Please contact Steve Schreiner at University of Nebraska System: University of Nebraska Medical Center for more information.
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