In Search of Novel Ampa PotentiatorsFrancotte, Pierre ; De Tullio, Pascal ; Fraikin, Pierre et alin Recent Patents on CNS Drug Discovery (2006), 1(3), 239-46 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 ... [more ▼] 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 Alzheimer's 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. [less ▲] Detailed reference viewed: 41 (21 ULg) Fluorinated benzothiadiazine derivatives and their use as AMPA receptor modulatorsFrancotte, Pierre ; ; De Tullio, Pascal et alPatent (2005) Detailed reference viewed: 15 (9 ULg) Preparation of fluorinated benzothiadiazine derivatives and their use as AMPA receptor modulatorsFrancotte, Pierre ; Fraikin, Pierre ; De Tullio, Pascal et alPatent (2005) Detailed reference viewed: 11 (5 ULg) Modulateurs allostériques positifs des récepteurs AMPA de la classe des 1,2,4-benzothiadiazine 1,1-dioxydes : conception, synthèse et évaluation pharmacologiqueFrancotte, Pierre ; Fraikin, Pierre ; De Tullio, Pascal et alPoster (2005, May) Detailed reference viewed: 13 (1 ULg) 3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers : effect of 6,7-distribution on potency and tissue selectivityDe Tullio, Pascal ; ; et alin Journal of Medicinal Chemistry (2005), 48 Detailed reference viewed: 10 (4 ULg) Novel thiadiazine derivatives useful as AMPA receptor modulators, preparation method, and pharmaceutical compositions containing them; Francotte, Pierre ; et alPatent (2004) Detailed reference viewed: 8 (1 ULg) Synthesis and biological evaluation of novel 2,3-dihydro-4H-1,2,4-benzothiadiazine 1,1-dioxides acting as AMPA potentiatorsFrancotte, Pierre ; Fraikin, Pierre ; De Tullio, Pascal et alPoster (2004, August) Detailed reference viewed: 2 (0 ULg) Prodrogues de modulateurs allostériques positifs des récepteurs AMPA apparentés à l’IDRA-21 : design, synthèse, étude de la stabilité et évaluation pharmacologiqueFrancotte, Pierre ; ; Fraikin, Pierre et alPoster (2004, June) Detailed reference viewed: 14 (0 ULg) Prodrugs of AMPA potentiators structurally related to IDRA-21: design, preparation, hydrolysis study and pharmacological evaluationFrancotte, Pierre ; ; Fraikin, Pierre et alConference (2004, May) Detailed reference viewed: 12 (1 ULg) New trends in the development of positive allosteric modulators of AMPA receptors; Francotte, Pierre ; et alin Current Medicinal Chemistry - Central Nervous System Agents (2004), 4 Detailed reference viewed: 2 (0 ULg) Produgs of AMPA potentiators structurally related to IDRA21 : design, preparation, hydrolysis study and pharmacological evaluationFrancotte, Pierre ; ; Fraikin, Pierre et alin Fundamental & Clinical Pharmacology (2004) Detailed reference viewed: 15 (2 ULg) New trends in the design of drugs against Alzheimer's diseaseFrancotte, Pierre ; ; et alin Current Medicinal Chemistry (2004), 11(13), 1757-1778 First described by Alois Alzheimer in 1907, Alzheimer's disease (AD) is the most common dementia type, affecting approximately 20 million people worldwide. As the population is getting older, AD is a ... [more ▼] First described by Alois Alzheimer in 1907, Alzheimer's disease (AD) is the most common dementia type, affecting approximately 20 million people worldwide. As the population is getting older, AD is a growing health problem. AD is currently treated by symptomatic drugs, the acetylcholinesterase inhibitors. based on the cholinergic hypothesis (1976). During the past decade, advances in neurobiology have conducted to the identification of new targets. Although some of these innovative approaches tend to delay onset of AD, others are still symptomatic. In this review, we present an overview of the several strategies and new classes of compounds against AD. [less ▲] Detailed reference viewed: 32 (11 ULg) Préparation et évaluation pharmacologique de modulateurs allostériques positifs des récepteurs AMPA : les 2,3-dihydro-4H-1,2,4-pyridothiadiazine 1,1-dioxydesFrancotte, Pierre ; ; et alPoster (2003, January 31) Detailed reference viewed: 3 (0 ULg) Nouveaux composés agissant en tant que modulateurs allostériques positifs des récepteurs glutamatergiques de sous-type AMPA : les 2,3-dihydro-4H-1,2,4-benzothiadiazine 1,1-dioxydes; Francotte, Pierre ; et alPoster (2003, January 31) Detailed reference viewed: 5 (0 ULg) Synthèse et évaluation biologique de 2,3-dihydro-4H-1,2,4-pyridothiadiazine 1,1-dioxydes en tant que modulateurs allostériques positifs des récepteurs AMPAFrancotte, Pierre ; ; et alPoster (2002, May) Detailed reference viewed: 3 (0 ULg) Les 2,3-dihydro-4H-1,2,4-benzothiadiazine 1,1-dioxydes en tant que modulateurs allostériques positifs des récepteurs glutamatergiques de sous-type AMPA; Francotte, Pierre ; et alPoster (2002, May) Detailed reference viewed: 4 (0 ULg) |
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