Search Results - "Brelière, Jean Claude"

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…”
Get full text

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…”
Get more information

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…”
Get more information

Blockade of cannabinoid (CB1) receptors by SR 141716 selectively antagonizes drug-induced reinstatement of exploratory behaviour in gerbils by PONCELET, M, BARNOUIN, M.-C, BRELIERE, J.-C, LE FUR, G, SOUBRIE, P

“…Rationale: A cannabinoid hypothesis of schi- zophrenia has been proposed according to which cognitive dysfunction could be associated with dysregulation of an…”
Get full text

Characterization and distribution of binding sites for [ 3H]-SR 141716A, a selective brain (CB1) cannabinoid receptor antagonist, in rodent brain by Rinaldi-Carmona, Murielle, Pialot, Françoise, Congy, Christian, Redon, Elsa, Barth, Francis, Bachy, André, Brelière, Jean-Claude, Soubrié, Philippe, Le Fur, Gérard

“…SR 141716A belongs to a new class of compounds (diarylpyrazole) that inhibits brain carmabinoid receptors (CB1) in vitro and in vivo . The present study showed…”
Get full text

Effect of substance P on cytokine production by human astrocytic cells and blood mononuclear cells: characterization of novel tachykinin receptor antagonists by Derocq, Jean-Marie, Ségui, Michel, Blazy, Chantal, Emonds-Alt, Xavier, Le Fur, Gérard, Brelière, Jean-Claude, Casellas, Pierre

“…Substance P (SP) has been reported to induce inflammatory cytokine production in human neuroglial cells and peripheral lymphoid cells as well. In order to…”
Get full text

A new series of imidazolones: highly specific and potent nonpeptide AT1 angiotensin II receptor antagonists by Bernhart, Claude A, Perreaut, Pierre M, Ferrari, Bernard P, Muneaux, Yvette A, Assens, Jean Louis A, Clement, Jacques, Haudricourt, Frederique, Muneaux, Claude F, Taillades, Joelle E, Vignal, Marie-Aimee, Gougat, Jean, Guiraudou, Pierre R, Lacour, Colette A, Roccon, Alain, Cazaubon, Catherine F, Breliere, Jean-Claude, Le Fur, Gerard, Nisato, Dino

“…Starting from the structure of the novel nonpeptide AT1 receptor antagonist DuP 753 (losartan), a new series of potent antagonists was designed. In these…”
Get full text

Immunopharmacological profile of SR 31747: in vitro and in vivo studies on humoral and cellular responses by Casellas, P, Bourrié, B, Canat, X, Carayon, P, Buisson, I, Paul, R, Brelière, J C, Le Fur, G

“…In our preceding paper, we demonstrated that both human and rat lymphocytes possess saturable high-affinity binding sites for the new sigma ligand SR 31747…”
Get more information

Allosteric modulation of peripheral sigma binding sites by a new selective ligand: SR 31747 by Paul, R, Lavastre, S, Floutard, D, Floutard, R, Canat, X, Casellas, P, Le Fur, G, Brelière, J C

“…The interactions of a new compound SR 31747 with sigma sites were examined in rat spleen membranes and in human peripheral blood leukocytes (PBL). Nanomolar…”
Get more information

Turning behavior induced in mice by a neurokinin A receptor agonist: stereoselective blockade by SR 48968, a non-peptide receptor antagonist by Poncelet, M, Gueudet, C, Emonds-Alt, X, Brelière, J C, Le Fur, G, Soubrié, P

“…The intrastriatal injection of [Nle10]-NKA(4-10), a neurokinin A agonist, (0.05-5 ng/mouse) elicited vigorous contralateral rotations. This behavior was…”
Get more information

The NK2 receptor antagonist SR48968 inhibits thalamic responses evoked by thermal but not mechanical nociception by Santucci, V, Gueudet, C, Edmonds-Alt, X, Brelière, J C, Soubrié, P, Le Fur, G

“…Extracellular recordings were made in the thalamic posterior nuclear group of anesthetized rats to study the effects of SR48968, a non-peptide NK2 receptor…”
Get more information

Identification of binding sites for SR 46349B, a 5-hydroxytryptamine2 receptor antagonist, in rodent brain by Rinaldi-Carmona, M, Congy, C, Pointeau, P, Vidal, H, Brelière, J C, Le Fur, G

“…SR 46349B belongs to a new class of compounds (propenone oxime ether derivative) that inhibit 5-hydroxytryptamine (HT)2 receptors in vitro and in vivo. (3H) SR…”
Get more information

SR 48968, a neurokinin A (NK2) receptor antagonist by Emonds-Alt, X, Advenier, C, Croci, T, Manara, L, Neliat, G, Poncelet, M, Proietto, V, Santucci, V, Soubrié, P, Van Broeck, D

Get more information

SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor by Rinaldi-Carmona, M, Barth, F, Millan, J, Derocq, J M, Casellas, P, Congy, C, Oustric, D, Sarran, M, Bouaboula, M, Calandra, B, Portier, M, Shire, D, Brelière, J C, Le Fur, G L

“…Based on both binding and functional data, this study introduces SR 144528 as the first, highly potent, selective and orally active antagonist for the CB2…”
Get more information

Effects of 1-hydroxyethylidene-1,1 bisphosphonate and (chloro-4 phenyl) thiomethylene bisphosphonic acid (SR 41319) on the mononuclear cell factor-mediated release of neutral proteinases by articular chondrocytes and synovial cells by Emonds-Alt, X, Brelière, J C, Roncucci, R

“…Articular chondrocytes and synovial cells were stimulated to produce collagenase, neutral casein and proteoglycan-degrading proteinases by conditioned medium…”
Get more information

Tachykinin-induced contractions of the guinea pig ileum longitudinal smooth muscle: tonic and phasic muscular activities by Vilain, P, Emonds-Alt, X, Le Fur, G, Brelière, J C

“…In vitro tachykinin-induced contractions of guinea pig ileum longitudinal smooth muscle were investigated under isometric conditions by using selective…”
Get more information

Two nonpeptide tachykinin antagonists act through epitopes on corresponding segments of the NK1 and NK2 receptors by U Gether, Y Yokota, X Emonds-Alt, J C Brelière, J A Lowe, 3rd, R M Snider, S Nakanishi, T W Schwartz

“…The molecular mechanism of action for two chemically distinct and highly selective, nonpeptide antagonists, CP-96,345 and SR-48,968, was studied by development…”
Get full text

Evidence for a common molecular mode of action for chemically distinct nonpeptide antagonists at the neurokinin-1 (substance P) receptor by Gether, U, Emonds-Alt, X, Brelière, J C, Fujii, T, Hagiwara, D, Pradier, L, Garret, C, Johansen, T E, Schwartz, T W

“…The molecular mechanism of action of three chemically distinct nonpeptide antagonists, SR 140,333, FK 888, and RP 67,580, was compared with that of the…”
Get more information

Effects on the isolated human bronchus of SR 48968, a potent and selective nonpeptide antagonist of the neurokinin A (NK2) receptors by Advenier, C, Naline, E, Toty, L, Bakdach, H, Emonds-Alt, X, Vilain, P, Brelière, J C, Le Fur, G

“…Tachykinins produce concentration-dependent contraction of the human isolated bronchus by stimulation of receptors that belong to the NK2 type. The aim of this…”
Get more information

Two Nonpeptide Tachykinin Antagonists Act Through Epitopes on Corresponding Segments of the NK1and NK2Receptors by Gether, Ulrik, Yokota, Yoshifumi, Emonds-Alt, Xavier, Breliere, Jean-Claude, Lowe, John A., Snider, R. Michael, Nakanishi, Shigetada, Schwartz, Thue W.

“…The molecular mechanism of action for two chemically distinct and highly selective, nonpeptide antagonists, CP-96,345 and SR-48,968, was studied by development…”
Get full text