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In vitro and in vivo SAR of pyrido[3,4-d]pyramid-4-ylamine based mGluR1 antagonists |
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| Authors: | Simon J. Mantell Karl R. Gibson Simon A. Osborne Graham N. Maw Huw Rees Peter G. Dodd Ben Greener Gareth W. Harbottle William A. Million Cedric Poinsard Steven England Pauline Carnell Alison M. Betts Russell Monhemius Rebecca L. Prime |
| Affiliation: | 1. Drug Discovery Group, Medical Research Council Technology, Mill Hill, London NW7 1AA, United Kingdom;2. Galderma, Sophia Antipolis, 2400 Route des Colles, 06902 BIOT, France;3. Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Kent, CT13 9NJ, United Kingdom |
| Abstract: | The SAR of a series of novel pyrido[3,4-d]pyramid-4-ylamine mGluR1 antagonists is described. The multiple of the unbound Ki in cerebrospinal fluid necessary to give morphine like analgesic effects in an electromyograph pinch model in rodents is determined and the effect of structure on CNS penetration examined. |
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