In vitro and in vivo SAR of pyrido[3,4- d]pyramid-4-ylamine based mGluR1 antagonists

SAR and CNS penetration of a series of novel mgluR1 antagonists is described. The multiple of the unbound K i in cerebrospinal fluid necessary to give morphine like analgesic effects in an electromyograph pinch model in rodents is given. The SAR of a series of novel pyrido[3,4- d]pyramid-4-ylamine m...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2009-04, Vol.19 (8), p.2190-2194
Hauptverfasser: Mantell, Simon J., Gibson, Karl R., Osborne, Simon A., Maw, Graham N., Rees, Huw, Dodd, Peter G., Greener, Ben, Harbottle, Gareth W., Million, William A., Poinsard, Cedric, England, Steven, Carnell, Pauline, Betts, Alison M., Monhemius, Russell, Prime, Rebecca L.
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Sprache:eng
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