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Synthesis and pharmacological properties of 5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, a new competitive AMPA/KA receptor antagonist
Drug development research, 1999-11, Vol.48 (3), p.121-129
Mignani, Serge
Aloup, Jean-Claude
Barreau, Michel
Blanchard, Jean Charles
Böhme, Georg Andrees
Boireau, Alain
Damour, Dominique
Debono, Marc-Williams
Dubroeucq, Marie-Christine
Genevois-Borella, Arielle
Imperato, Assunta
Jimonet, Patrick
Pratt, Jeremy
Randle, John C.R.
Reibaud, Michel
Ribeill, Yves
Stutzmann, Jean-Marie
1999
Details
Autor(en) / Beteiligte
Mignani, Serge
Aloup, Jean-Claude
Barreau, Michel
Blanchard, Jean Charles
Böhme, Georg Andrees
Boireau, Alain
Damour, Dominique
Debono, Marc-Williams
Dubroeucq, Marie-Christine
Genevois-Borella, Arielle
Imperato, Assunta
Jimonet, Patrick
Pratt, Jeremy
Randle, John C.R.
Reibaud, Michel
Ribeill, Yves
Stutzmann, Jean-Marie
Titel
Synthesis and pharmacological properties of 5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, a new competitive AMPA/KA receptor antagonist
Ist Teil von
Drug development research, 1999-11, Vol.48 (3), p.121-129
Ort / Verlag
New York: John Wiley & Sons, Inc
Erscheinungsjahr
1999
Link zum Volltext
Quelle
Wiley Online Library - AutoHoldings Journals
Beschreibungen/Notizen
The excessive release of glutamate, a potent excitatory neurotransmitter, is thought to play an important role in a variety of acute and chronic neurological disorders. Consequently, excitatory amino acid antagonists may have an important therapeutic potential in the treatment of these diseases. Glutamate interacts with at least three types of receptor: 1) NMDA (N‐methyl‐D‐aspartic acid) receptors; 2) AMPA [2‐amino‐3‐(3‐hydroxy‐5‐methylisoxazol‐4‐yl)propionic acid]/kainic acid (KA) receptors; and 3) metabotropic receptors. Blockade of ionotropic AMPA/KA receptors has been shown to prevent cerebral ischemia insult in experimental models. This article describes the synthesis, pharmacological activity, and neuroprotective properties of 5H,10H‐imidazo[1,2‐a]indeno[1,2‐e]pyrazine‐4‐one (1), a novel AMPA/KA antagonist which showed micromolar affinity at AMPA/KA receptors and competitively inhibited functional responses mediated by these receptors. In mice, 1 had significant anticonvulsive properties and conferred protection against hypobaric hypoxia and KCN intoxication. In rats and gerbils, 1 possesses significant activity in models of global or focal cerebral ischemia, as well as in a model of neurotrauma. Compound 1 was prepared from 2‐bromo‐indanone using two synthetic pathways in two or three steps with moderate (30%) or good (70%) yields, respectively. Drug Dev. Res. 48:121–129, 1999. © 1999 Wiley‐Liss, Inc.
Sprache
Englisch
Identifikatoren
ISSN: 0272-4391
eISSN: 1098-2299
DOI: 10.1002/(SICI)1098-2299(199911)48:3<121::AID-DDR4>3.0.CO;2-E
Titel-ID: cdi_crossref_primary_10_1002__SICI_1098_2299_199911_48_3_121__AID_DDR4_3_0_CO_2_E
Format
–
Schlagworte
AMPA/KA antagonists
,
anticonvulsant agent
,
Anticonvulsants. Antiepileptics. Antiparkinson agents
,
Biological and medical sciences
,
Medical sciences
,
Neuropharmacology
,
Neuroprotective agent
,
Pharmacology. Drug treatments
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