A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity.
Bioorg Med Chem
; 18(16): 6089-98, 2010 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-20638290
ABSTRACT
As part of the vital search towards improved therapeutic agents for the treatment of neuropathic pain, the central nervous system glutamate receptors have become a major focus of research. Outlined herein are the syntheses of two new biologically active 3'-cycloalkyl-substituted carboxycyclopropylglycines, utilizing novel synthetic chemistry. The reaction between substituted 1,2-dioxines and an aminophosphonate furnished the cyclopropane core in a single step with all required stereochemistry of pendant groups. In vitro binding assays at metabotropic glutamate receptors revealed selective activity. In vivo testing in a rodent model of neuropathic pain indicated one amino acid significantly and dose-dependently decreased mechanical allodynia.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Receptores de Glutamato Metabotrópico
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Ciclopropanos
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Glicina
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Hiperalgesia
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Analgésicos
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Neuralgia
Limite:
Animals
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article