Search Results - "Héaulme, Michel"

SR141716A, a potent and selective antagonist of the brain cannabinoid receptor by Rinaldi-Carmona, Murielle, Barth, Francis, Héaulme, Michel, Shire, David, Calandra, Bernard, Congy, Christian, Martinez, Serge, Maruani, Jeanne, Néliat, Gervais, Caput, Daniel, Ferrara, Pascual, Soubrié, Philippe, Brelière, Jean Claude, Le Fur, Gérard

“…SR141716A is the first selective and orally active antagonist of the brain cannabinoid receptor. This compound displays nanomolar affinity for the central…”
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Neurochemical, Electrophysiological and Pharmacological Profiles of the Selective Inhibitor of the Glycine Transporter-1 SSR504734, a Potential New Type of Antipsychotic by Depoortère, Ronan, Dargazanli, Gihad, Estenne-Bouhtou, Genevieve, Coste, Annick, Lanneau, Christophe, Desvignes, Christophe, Poncelet, Martine, Heaulme, Michel, Santucci, Vincent, Decobert, Michel, Cudennec, Annie, Voltz, Carolle, Boulay, Denis, Terranova, Jean Paul, Stemmelin, Jeanne, Roger, Pierre, Marabout, Benoit, Sevrin, Mireille, Vigé, Xavier, Biton, Bruno, Steinberg, Régis, Françon, Dominique, Alonso, Richard, Avenet, Patrick, Oury-Donat, Florence, Perrault, Ghislaine, Griebel, Guy, George, Pascal, Soubrié, Philippe, Scatton, Bernard

“…Noncompetitive N-methyl-D-aspartate (NMDA) blockers induce schizophrenic-like symptoms in humans, presumably by impairing glutamatergic transmission…”
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SR 57227A: a potent and selective agonist at central and peripheral 5-HT3 receptors in vitro and in vivo by Bachy, A, Héaulme, M, Giudice, A, Michaud, J C, Lefevre, I A, Souilhac, J, Manara, L, Emerit, M B, Gozlan, H, Hamon, M

“…SR 57227A (4-amino-(6-chloro-2-pyridyl)-1 piperidine hydrochloride) is a novel compound with high affinity and selectivity for the 5-HT3 receptor. The compound…”
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In vitro and in vivo biological activities of SR140333, a novel potent non-peptide tachykinin NK1 receptor antagonist by Emonds-Alt, X, Doutremepuich, J D, Heaulme, M, Neliat, G, Santucci, V, Steinberg, R, Vilain, P, Bichon, D, Ducoux, J P, Proietto, V

“…(S)1-(2-[3-(3,4-dichlorophenyl)-1-(3-isopropoxyphenylacetyl)pip eridin-3- yl]ethyl)-4-phenyl-1-azoniabicyclo[2.2.2]octane chloride (SR140333) is a new…”
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Biochemical and pharmacological characterisation of SR141716A, the first potent and selective brain cannabinoid receptor antagonist by Rinaldi-Carmona, M, Barth, F, Héaulme, M, Alonso, R, Shire, D, Congy, C, Soubrié, P, Brelière, J C, Le Fur, G

“…SR141716A is a selective, potent and orally active antagonist of the brain cannabinoid receptor with a long duration of action. This compound shows high…”
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Neurochemical, electrophysiological and pharmacological profiles of the selective inhibitor of the glycine transporter-I SSR504734, a potential new type of antipsychotic by DEPOORTERE, Ronan, DARGAZANLI, Gihad, CUDENNEC, Annie, VOLTZ, Carolle, BOULAY, Denis, TERRANOVA, Jean Paul, STEMMELIN, Jeanne, ROGER, Pierre, MARABOUT, Benoit, SEVRIN, Mireille, VIGE, Xavier, BITON, Bruno, ESTENNE-BOUHTOU, Genevieve, STEINBERG, Régis, FRANCON, Dominique, ALONSO, Richard, AVENET, Patrick, OURY-DONAT, Florence, PERRAULT, Ghislaine, GRIEBEL, Guy, GEORGE, Pascal, SOUBRIE, Philippe, SCATTON, Bernard, COSTE, Annick, LANNEAU, Christophe, DESVIGNES, Christophe, PONCELET, Martine, HEAULME, Michel, SANTUCCI, Vincent, DECOBERT, Michel

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Characterization of the binding of [3H]SR 95531, a GABAA antagonist, to rat brain membranes by Heaulme, M, Chambon, J P, Leyris, R, Wermuth, C G, Biziere, K

“…A synthetic derivative of gamma-aminobutyric acid (GABA), SR 95531 [2-(3'-carboxy-2'-propyl)-3-amino-6-p-methoxyphenylpyridazinium bromide], has recently been…”
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Noradrenaline and prostaglandin E2 stimulate LH-RH release from rat median eminence through distinct 1-alpha-adrenergic and PGE2 receptors by Heaulme, M, Dray, F

“…Noradrenaline (NA) and prostaglandin (PG) E2 produced a dose-related stimulation of luteinizing hormone releasing hormone (LH-RH) release from incubated median…”
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SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. II. In vivo pharmacological characterization by Bignon, E, Alonso, R, Arnone, M, Boigegrain, R, Brodin, R, Gueudet, C, Héaulme, M, Keane, P, Landi, M, Molimard, J C, Olliero, D, Poncelet, M, Seban, E, Simiand, J, Soubrié, P, Pascal, M, Maffrand, J P, Le Fur, G

“…SR146131 is a potent and selective agonist at cholecystokinin subtype 1 (CCK1) receptors in vitro. The present study evaluates the activity of the compound in…”
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Biochemical and Pharmacological Profile of a Potent and Selective Nonpeptide Antagonist of the Neurotensin Receptor by Gully, Danielle, Canton, Maryse, Boigegrain, Robert, Jeanjean, Francis, Molimard, Jean-Charles, Poncelet, Martine, Gueudet, Christiane, Heaulme, Michel, Leyris, Roger, Brouard, Aline, Pelaprat, Didier, Labbe-Jullie, Catherine, Mazella, Jean, Soubrie, Philippe, Maffrand, Jean-Pierre, Rostene, William, Kitabgi, Patrick, Le Fur, Gerard

“…We describe the characteristics of SR 48692, a selective, nonpeptide antagonist of the neurotensin receptor. In vitro, this compound competitively…”
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Involvement of potentially distinct neurotensin receptors in neurotensin-induced stimulation of striatal [ 3H]dopamine release evoked by KC1 versus electrical depolarization by Heaulme, Michel, Leyris, Roger, Le Fur, Gérard, Soubrie, Philippe

“…We intended to determine whether the effect of neurotensin (NT) on K + and electrically evoked [ 3H]dopamine (DA) release from rat and guinea-pig striatal…”
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Involvement of potentially distinct neurotensin receptors in neurotensin-induced stimulation of striatal [3H]dopamine release evoked by KCl versus electrical depolarization by HEAULME, M, LEYRIS, R, LE FUR, G, SOUBRIE, P

“…We intended to determine whether the effect of neurotensin (NT) on K+ and electrically evoked [3H]dopamine (DA) release from rat and guinea-pig striatal slices…”
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SR 48692 inhibits neurotensin-induced [3H]dopamine release in rat striatal slices and mesencephalic cultures by Brouard, A, Heaulme, M, Leyris, R, Pelaprat, D, Gully, D, Kitabgi, P, Le Fur, G, Rostene, W

“…In rat striatal slices, the increase (114 +/- 11%) in K(+)-evoked [3H]dopamine release induced by neurotensin (10 nM) was antagonized by…”
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Synthesis and biochemical evaluation of baclofen analogs locked in the baclofen solid-state conformation by Mann, Andre, Boulanger, Thierry, Brandau, Barbara, Durant, Francois, Evrard, Guy, Heaulme, Michel, Desaulles, Eric, Wermuth, Camille Georges

“…The synthesis of six close analogues of baclofen [3-(4-chlorophenyl)-4-aminobutyric acid] (BAC), a potent GABAB agonist, are reported. The compounds were…”
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Neurotensin receptor interaction with dopaminergic systems in the guinea-pig brain shown by neurotensin receptor antagonists by Azzi, M, Gully, D, Heaulme, M, Bérod, A, Pélaprat, D, Kitabgi, P, Boigegrain, R, Maffrand, J P, LeFur, G, Rostène, W

“…Neurotensin has been suggested to be involved in neurological and mental disorders associated with altered dopaminergic transmission. The lack of a potent…”
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Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site by Heaulme, M, Chambon, J P, Leyris, R, Molimard, J C, Wermuth, C G, Biziere, K

“…An arylaminopyridazine derivative of gamma-aminobutyric acid (GABA), SR 95103, has been shown to be a selective antagonist of GABA at the GABAA receptor site…”
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Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of .gamma.-aminobutyric acid acting as selective GABA-A antagonists by Wermuth, Camille Georges, Bourguignon, Jean Jacques, Schlewer, Gilbert, Gies, Jean Pierre, Schoenfelder, Angele, Melikian, Anita, Bouchet, Marie Jeanne, Chantreux, Dominique, Molimard, Jean Charles

“…We have recently shown that an arylaminopyridazine derivative of GABA, SR 95103 [2-(3-carboxypropyl)-3-amino-4-methyl-6-phenylpyridazinium chloride], is a…”
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Absence of modifications in gamma-aminobutyric acid metabolism after repeated generalized seizures in amygdala-kindled rats by Lerner-Natoli, M, Heaulme, M, Leyris, R, Biziere, K, Rondouin, G

“…Alterations in gamma-aminobutyric acid (GABA) metabolism have been investigated in the kindling model of epilepsy. Numerous generalized seizures were induced…”
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An Arylaminopyridazine Derivative of γ -aminobutyric Acid (GABA) is a Selective and Competitive Antagonist at the GABAAReceptor Site by Chambon, Jean-Pierre, Feltz, Paul, Heaulme, Michel, Restle, Serge, Schlichter, Remy, Biziere, Kathleen, Wermuth, Camille G.

“…In view of finding a new γ -aminobutyric acid (GABA) receptor ligand we synthesized an arylaminopyridazine derivative of GABA, SR 95103…”
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