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Your search keyword '"Lingenhoehl K"' showing total 3 results
Start Over Author "Lingenhoehl K" Publisher elsevier science ltd
3 results on '"Lingenhoehl K"'

1. 6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.

Author

Orain D, Ofner S, Koller M, Carcache DA, Froestl W, Allgeier H, Rasetti V, Nozulak J, Mattes H, Soldermann N, Floersheim P, Desrayaud S, Kallen J, Lingenhoehl K, and Urwyler S

Subjects
Administration, Oral, Animals, Anticonvulsants administration & dosage, Anticonvulsants chemistry, Crystallography, X-Ray, Disease Models, Animal, Dose-Response Relationship, Drug, Mice, Mice, Inbred DBA, Models, Molecular, Molecular Structure, Quinazolinones administration & dosage, Quinazolinones chemistry, Seizures drug therapy, Stereoisomerism, Structure-Activity Relationship, Sulfonamides administration & dosage, Sulfonamides chemistry, Anticonvulsants pharmacology, Quinazolinones pharmacology, Receptors, AMPA antagonists & inhibitors, Sulfonamides pharmacology
Abstract

A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified with a low ED(50) of 5.5mg/kg in an animal model of anticonvulsant activity after oral dosage., (Copyright © 2011. Published by Elsevier Ltd.)

Published
2012
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2. Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity.

Author

Koller M, Lingenhoehl K, Schmutz M, Vranesic IT, Kallen J, Auberson YP, Carcache DA, Mattes H, Ofner S, Orain D, and Urwyler S

Subjects
Administration, Oral, Animals, Anticonvulsants pharmacology, Binding, Competitive drug effects, Crystallography, X-Ray, Mice, Molecular Structure, Quinazolinones chemistry, Quinazolinones pharmacology, Rats, Structure-Activity Relationship, Sulfonamides chemistry, Sulfonamides pharmacology, Quinazolinones chemical synthesis, Receptors, AMPA antagonists & inhibitors, Sulfonamides chemical synthesis
Abstract

Quinazoline-2,4-diones with a sulfonamide group attached to the N(3) ring atom constitute a novel class of competitive AMPA receptor antagonists. One of the synthesized compounds, 28, shows nanomolar receptor affinity, whereas other examples of the series display oral anticonvulsant activity in animal models., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
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3. 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition.

Author

Auberson YP, Allgeier H, Bischoff S, Lingenhoehl K, Moretti R, and Schmutz M

Subjects
Animals, Binding, Competitive, Electric Stimulation, Humans, Mice, Molecular Structure, Quinoxalines chemical synthesis, Anticonvulsants pharmacology, Quinoxalines chemistry, Quinoxalines pharmacology, Receptors, N-Methyl-D-Aspartate antagonists & inhibitors
Abstract

NMDA antagonists derived from 5-phosphonomethyl-1,4-dihydroquinoxaline-2,3-dione (3a) are potent anticonvulsant agents, and display strong protective effects in the electroshock-induced convulsion assay in mice. Their preference for the human NMDAR 1A/2A over 1A/2B subunit composition was optimized, leading to (1RS,1'S)-PEAQX (9r), which shows a >100-fold selectivity.

Published
2002
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