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
Schlagworte:	Analgesics Animals Biological and medical sciences Central nervous system Electromyography - methods Excitatory Amino Acid Antagonists - chemical synthesis Excitatory Amino Acid Antagonists - chemistry Excitatory Amino Acid Antagonists - pharmacology Glutamatergic system (aspartate and other excitatory aminoacids) Medical sciences mgluR1 Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Nociceptive pain Pain Measurement - drug effects Pain Measurement - methods Pharmacology. Drug treatments Rats Receptors, Metabotropic Glutamate - antagonists & inhibitors Receptors, Metabotropic Glutamate - physiology Structure-Activity Relationship
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container_title	Bioorganic & medicinal chemistry letters
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creator	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.
description	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 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 determined and the effect of structure on CNS penetration examined.
doi_str_mv	10.1016/j.bmcl.2009.02.106
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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 determined and the effect of structure on CNS penetration examined.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2009.02.106</identifier><identifier>PMID: 19289283</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Analgesics ; Animals ; Biological and medical sciences ; Central nervous system ; Electromyography - methods ; Excitatory Amino Acid Antagonists - chemical synthesis ; Excitatory Amino Acid Antagonists - chemistry ; Excitatory Amino Acid Antagonists - pharmacology ; Glutamatergic system (aspartate and other excitatory aminoacids) ; Medical sciences ; mgluR1 ; Neuropharmacology ; Neurotransmitters. Neurotransmission. 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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 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 determined and the effect of structure on CNS penetration examined.</description><subject>Analgesics</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Central nervous system</subject><subject>Electromyography - methods</subject><subject>Excitatory Amino Acid Antagonists - chemical synthesis</subject><subject>Excitatory Amino Acid Antagonists - chemistry</subject><subject>Excitatory Amino Acid Antagonists - pharmacology</subject><subject>Glutamatergic system (aspartate and other excitatory aminoacids)</subject><subject>Medical sciences</subject><subject>mgluR1</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Nociceptive pain</subject><subject>Pain Measurement - drug effects</subject><subject>Pain Measurement - methods</subject><subject>Pharmacology. 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Neurotransmission. Receptors</topic><topic>Nociceptive pain</topic><topic>Pain Measurement - drug effects</topic><topic>Pain Measurement - methods</topic><topic>Pharmacology. 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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 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 determined and the effect of structure on CNS penetration examined.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>19289283</pmid><doi>10.1016/j.bmcl.2009.02.106</doi><tpages>5</tpages></addata></record>
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subjects	Analgesics Animals Biological and medical sciences Central nervous system Electromyography - methods Excitatory Amino Acid Antagonists - chemical synthesis Excitatory Amino Acid Antagonists - chemistry Excitatory Amino Acid Antagonists - pharmacology Glutamatergic system (aspartate and other excitatory aminoacids) Medical sciences mgluR1 Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Nociceptive pain Pain Measurement - drug effects Pain Measurement - methods Pharmacology. Drug treatments Rats Receptors, Metabotropic Glutamate - antagonists & inhibitors Receptors, Metabotropic Glutamate - physiology Structure-Activity Relationship
title	In vitro and in vivo SAR of pyrido[3,4- d]pyramid-4-ylamine based mGluR1 antagonists
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