In Search of Novel AMPA Potentiators

Author(s): Pierre Francotte, Pascal de Tullio, Pierre Fraikin, Stephane Counerotte, Eric Goffin, Bernard Pirotte

Journal Name: Recent Patents on CNS Drug Discovery (Discontinued)

Volume 1 , Issue 3 , 2006


Glutamate is the major excitatory neurotransmitter in the brain. Amongst ionotropic receptors responding to glutamate, the AMPA subtype has been considered as essential for the fast excitatory neurotransmission in the central nervous system and the expression and maintenance of long-term potentiation. As glutamate is known to be involved in many neurological and psychiatric disorders, AMPA receptors seem to represent interesting targets to develop therapeutic drugs. Hence, the enhancement of AMPA signals is an approach currently investigated for the management of Alzheimers disease, schizophrenia or mood disorders. In particular, many efforts are being conducted in the development of AMPA positive allosteric modulators (“potentiators”), which alter the rate of receptor desensitization. The major chemical families developed as AMPA potentiators are aniracetam derivatives, cyclothiazide derivatives and biarylpropylsulfonamides derivatives.

Keywords: Glutamate receptors, AMPA potentiator, AMPA positive allosteric modulator, cognitive enhancers, mood disorders treatment

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Article Details

Year: 2006
Published on: 01 March, 2012
Page: [239 - 246]
Pages: 8
DOI: 10.2174/157488906778773661
Price: $65

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