Jean-Claude Aloup
Rhône-Poulenc
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Featured researches published by Jean-Claude Aloup.
Drug Development Research | 1999
Serge Mignani; Jean-Claude Aloup; Michel Barreau; Jean Charles Blanchard; Georg Andrees Böhme; Alain Boireau; Dominique Damour; Marc-Williams Debono; Marie-Christine Dubroeucq; Arielle Genevois-Borella; Assunta Imperato; Patrick Jimonet; Jeremy Pratt; John Randle; Michel Reibaud; Yves Ribeill; Jean-Marie Stutzmann
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.
Archive | 1994
Jean-Claude Aloup; Francois Audiau; Dominique Damour; Arielle Genevois-Borella; Patrick Jimonet; Serge Mignani
Journal of Medicinal Chemistry | 1987
Jean-Claude Aloup; Jean Bouchaudon; Daniel Farge; Claude James; Jean Deregnaucourt; Monique Hardy-Houis
Archive | 1993
Jean-Claude Aloup; Francois Audiau; Dominique Damour; Patrick Jimonet; Serge Mignani
Archive | 1994
Jean-Claude Aloup; Francois Audiau; Dominique Damour; Arielle Genevois-Borella; Patrick Jimonet; Serge Mignani; Yves Ribeill
Archive | 1994
Jean-Claude Aloup; Serge Mignani
Archive | 1995
Jean-Claude Aloup; Francois Audiau; Michel Barreau; Dominique Damour; Arielle Genevois-Borella; Patrick Jimonet; Serge Magnani; Yves Ribeill
Archive | 1995
Jean-Claude Aloup; Fran Cedilla Ois Audiau; Michel Barreau; Dominique Damour; Arielle Genevois-Borella; Patrick Jimonet; Serge Mignani; Yves Ribeill
Archive | 1993
Jean-Claude Aloup; Fran Cedilla Ois Audiau; Dominique Damour; Arielle Genevois-Borella; Patrick Jimonet; Serge Mignani
Archive | 1995
Jean-Claude Aloup; Francois Audiau; Michel Barreau; Dominique Damour; Arielle Genevois-Borella; Patrick Jimonet; Serge Mignani; Yves Ribeill