2,4-Dicarboxy-pyrroles as selective non-Competitive mGluR1 antagonists: further characterization of 3,5-Dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-Trimethyl-propyl) ester and structure–Activity relationships

Following the disclosure of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester [3,5-dimethyl PPP] as a potent and selective mGluR1 non-competitive antagonist, we report here further in vivo characterization of this important tool and disclose the investigation...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-07, Vol.13 (13), p.2113-2118
Main Authors: Micheli, Fabrizio, Di Fabio, Romano, Bordi, Fabio, Cavallini, Palmina, Cavanni, Paolo, Donati, Daniele, Faedo, Stefania, Maffeis, Micaela, Sabbatini, Fabio Maria, Tarzia, Giorgio, Tranquillini, Maria Elvira
Format: Article
Language:English
Subjects:
Animals
Binding, Competitive - drug effects
Dose-Response Relationship, Drug
Electrophysiology
Esters - chemical synthesis
Esters - pharmacology
Excitatory Amino Acid Antagonists - chemical synthesis
Excitatory Amino Acid Antagonists - pharmacology
Indicators and Reagents
Morphine - pharmacology
Neurons - drug effects
Neurons - metabolism
Nociceptors - drug effects
Pyrroles - chemical synthesis
Pyrroles - pharmacology
Rats
Receptors, Metabotropic Glutamate - antagonists & inhibitors
Spinal Cord - drug effects
Spinal Cord - metabolism
Structure-Activity Relationship
Synaptic Transmission - drug effects
Thalamus - drug effects
Thalamus - metabolism
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Summary:Following the disclosure of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester [3,5-dimethyl PPP] as a potent and selective mGluR1 non-competitive antagonist, we report here further in vivo characterization of this important tool and disclose the investigation of the C-5 position, which led to very potent compounds. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00396-2