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

Autor:	William A. Million, Pauline Carnell, Gareth W. Harbottle, Russell Monhemius, Simon A. Osborne, Cedric Poinsard, Maw Graham Nigel, Ben S. Greener, Karl Richard Gibson, Rebecca L. Prime, Steven England, Peter G. Dodd, Simon John Mantell, Alison Betts, Huw Rees
Rok vydání:	2009
Předmět:	Stereochemistry Clinical Biochemistry Analgesic Pharmaceutical Science Pharmacology Receptors Metabotropic Glutamate Biochemistry Cns penetration Structure-Activity Relationship In vivo Drug Discovery Animals Structure–activity relationship Molecular Biology Pain Measurement Bicyclic molecule Electromyography Chemistry Organic Chemistry Antagonist In vitro Rats body regions Molecular Medicine Metabotropic glutamate receptor 1 Excitatory Amino Acid Antagonists
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:2190-2194
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dedc2e644ebe905bda97f0d735bbb991 https://doi.org/10.1016/j.bmcl.2009.02.106 Zobrazit plný text záznamu Full Text from ScienceDirect