Novel Potent Anticonvulsant Agent Containing a Tetrahydroisoquinoline Skeleton.
From: Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy. rgitto@pharma.unime.it
Journal of medicinal chemistry
- Publish Date: Sep 2006
- ISSN: 0022-2623
- Volume: 49
- Issue: 18
- Pages: 5618-22
- Medium: Print
- Language: English
- Citation (JAMA): Gitto Rosaria, Caruso Roberta, Pagano Benedetta, et al. Novel Potent Anticonvulsant Agent Containing a Tetrahydroisoquinoline Skeleton.. J. Med. Chem. Sep 2006;49:5618-22
Abstract
In our studies on the development of new anticonvulsants, we planned the synthesis of N-substituted 1,2,3,4-tetrahydroisoquinolines to explore the structure-activity relationships. All derivatives were evaluated against audiogenic seizures in DBA/2 mice, and the 1-(4’-bromophenyl)-6,7-dimethoxy-2-(piperidin-1-ylacetyl) derivative (26) showed the highest activity with a potency comparable to that of talampanel, the only noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonist in clinical trials as an anticonvulsant agent. Electrophysiological experiments indicated that 26 acts as noncompetitive AMPA receptor modulator.
Mesh Headings (Keywords): Acoustic Stimulation, Animals, Anticonvulsants, Isoquinolines, Male, Mice, Mice, Inbred DBA, Olfactory Pathways, Piperidines, Rats, Rats, Wistar, Receptors, AMPA, Seizures, Structure-Activity Relationship, Tetrahydroisoquinolines
Check for Full Text / PubMed Unique Identifier (PMID): 16942035
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