Compounds active at a novel site on receptor-operated...

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/137 (2006.01) A61K 31/14 (2006.01) A61K 31/165 (2006.01) A61K 31/4045 (2006.01) A61P 25/00 (2006.01) G01N 33/53 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2182680

Method for identifying a compound useful for the therapeutic treatment of a neurological disease or disorder such as stroke, head trauma, spinal cord injury, epilepsy, anxiety, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease or Parkinson's Disease, or useful as a muscle relaxant, analgesic, or adjuvant to general anesthetics. The compounds is active on a receptor- operated calcium channel, including but not limited to, that present as part of an NMDA receptor-ionophore complex, a calcium-permeable AMPA receptor, or a nicotinic cholinergic receptor, as a noncompetitive antagonist. The method includes identifying a compound which binds to the receptor-operated calcium channel at the site bound by the arylalkylamines Compound 1, Compound 2 or Compound 3.

L'invention se raporte à un procédé d'identification d'un composé utilisé dans le traitement d'une maladie ou d'un trouble neurologique, tel qu'une attaque, un traumatisme crânien, une lésion de la moelle épinière, l'épilepsie, l'anxiété ou des maladies neurodégénératives, telles que la maladie d'Alzheimer, la maladie d'Huntington ou la maladie de Parkinson, ou apte à être utilisé comme un relaxant musculaire, un analgésique, ou un adjuvant à un anesthésique général. Le composé agit sur un canal calcique activé par des récepteurs, comprenant notamment, mais non exclusivement, les canaux calciques faisant partie d'un complexe ionophore/récepteurs NMDA, un récepteur AMPA perméable au calcium, ou un récepteur cholinergique nicotinique, en tant qu'antagoniste non compétitif. Le procédé consiste à identifier un composé qui se lie au canal calcique activé par des récepteurs sur le site lié par les composés 1, 2 ou 3 d'arylalkylamines.

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