Inverse agonism and constitutive activity as functional correlates of serotonin h5-HT(1B) receptor/G-protein stoichiometryA Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, Croissy sur Seine Paris, France
Mol Pharmacol 58:1042-9. 2000
....
- [(35)S]-GTPgammaS autoradiography reveals alpha(2) adrenoceptor-mediated G-protein activation in amygdala and lateral septum
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
Neuropharmacology 39:1111-3. 2000
..Conversely, in caudate nucleus, which expresses few alpha(2) receptors, noradrenaline-induced stimulation was not inhibited by atipamezole, suggesting that it is not mediated by alpha(2)-adrenoceptors...
- The 5HT(1A) receptor ligand, S15535, antagonises G-protein activation: a [35S]GTPgammaS and [3H]S15535 autoradiography study
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, F 78290 Croissy sur Seine, Paris, France
Eur J Pharmacol 384:111-21. 1999
....
Differential modulation by GTPgammaS of agonist and inverse agonist binding to h5-HT(1A) receptors revealed by [3H]-WAY100,635A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, 125, Chemin de Ronde, 78290, Croissy sur Seine, France
Br J Pharmacol 132:518-24. 2001
....
- Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors
A Newman-Tancredi
Psychopharmacology Department, Institut de Recherches Servier, Croissy sur Seine Paris, France
Naunyn Schmiedebergs Arch Pharmacol 359:447-53. 1999
..7%). The present data suggest that roxindole activates mainly D3 vs. D2 or D4 receptors and 5-HT1A vs. 5-HT1B or 5-HT1D receptors. Activation of D3 and/or 5-HT1A receptors may thus contribute to its potential antidepressant properties...
- G protein activation by human dopamine D3 receptors in high-expressing Chinese hamster ovary cells: A guanosine-5'-O-(3-[35S]thio)- triphosphate binding and antibody study
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, Croissy sur Seine Paris, France
Mol Pharmacol 55:564-74. 1999
....
- Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, Paris, France
Eur J Pharmacol 355:245-56. 1998
..It is suggested that agonist activity at 5-HT1A receptors may be of utility for certain antipsychotic agents...
- Efficacy of antipsychotic agents at human 5-HT(1A) receptors determined by [3H]WAY100,635 binding affinity ratios: relationship to efficacy for G-protein activation
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
Eur J Pharmacol 428:177-84. 2001
..In conclusion, modulation of [3H]-WAY100,635 binding by GTPgammaS differentiated agonist vs. inverse agonist properties of antipsychotics at 5-HT(1A) receptors. These may contribute to differing profiles of antipsychotic activity...
- Dopamine D2 receptor-mediated G-protein activation in rat striatum: functional autoradiography and influence of unilateral 6-hydroxydopamine lesions of the substantia nigra
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
Brain Res 920:41-54. 2001
....
- Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, Croissy sur Seine, France
Naunyn Schmiedebergs Arch Pharmacol 355:682-8. 1997
....
- Simultaneous quantification of serotonin, dopamine and noradrenaline levels in single frontal cortex dialysates of freely-moving rats reveals a complex pattern of reciprocal auto- and heteroreceptor-mediated control of release
A Gobert
Institut de Recherches Servier, Psychopharmacology Department, Croissy sur Seine, France
Neuroscience 84:413-29. 1998
..Control of serotonin release is expressed phasically and that of noradrenaline and dopamine release tonically...
- Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization
M J Millan
Department of Psychopharmacology, Institut de Recherches Servier, Centre de Recherches de Croissy, Paris, France
J Pharmacol Exp Ther 297:876-87. 2001
..6). In conclusion, piribedil displays essentially antagonist properties at cloned, human and cerebral, rat alpha(2)-ARs. Blockade of alpha(2)-ARs may, thus, contribute to its clinical antiparkinsonian profile...
- Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic tr
M J Millan
Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, 125, Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
Synapse 35:79-95. 2000
..However, in contrast to the selective alpha(2)-AR antagonist, fluparoxan, the 5-HT(1A) agonist actions of yohimbine suppress 5-HT levels alone and underlie its inability to augment the influence of fluoxetine upon 5-HT levels...
- Comparison of hippocampal G protein activation by 5-HT(1A) receptor agonists and the atypical antipsychotics clozapine and S16924
A Newman-Tancredi
Dept. of Psychopharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290, Croissy-sur-Seine, France
Naunyn Schmiedebergs Arch Pharmacol 368:188-99. 2003
..These data support a role of postsynaptic 5-HT(1A) receptors in the functional profiles of certain antipsychotic agents...
- S18327 (1-[2-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)piperid-1-yl]ethyl]3-phenyl imidazolin-2-one), a novel, potential antipsychotic displaying marked antagonist properties at alpha(1)- and alpha(2)-adrenergic receptors: II. Functional profile and a multipara
M J Millan
Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, Paris, Croissy sur Seine, France
J Pharmacol Exp Ther 292:54-66. 2000
..In this respect, S18327 closely resembles clozapine, but it is chemically distinct and displays weak affinity for histaminic and muscarinic receptors...
- [35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, Croissy sur Seine, France
J Pharmacol Exp Ther 282:181-91. 1997
..4 receptors might be associated with a lesser incidence of side effects. Furthermore, antagonist activity at D4.4 receptors is a common property of many typical and atypical antipsychotic agents...
- Noradrenaline and adrenaline are high affinity agonists at dopamine D4 receptors
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, Croissy sur Seine, Paris, France
Eur J Pharmacol 319:379-83. 1997
..These results indicate that dopamine D4 receptors are activated by noradrenaline and adrenaline, although at 50-100-fold higher concentrations than dopamine...
- Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization
M J Millan
Psychopharmacology Department, Centre de Recherches de Croissy, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy Seine, Paris, France
Pharmacol Biochem Behav 71:589-98. 2002
..In conclusion, [3H]GR125,743 is an appropriate tool for the radiolabelling of native, rat 5-HT(1B) receptors and permitted determination of the affinities of an extensive series of ligands at these sites...
- The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways
M J Millan
Department of Psychopharmacology, Institut de Recherches Servier, Croissy Seine, France
J Pharmacol Exp Ther 306:954-64. 2003
..In conclusion, in contrast to melatonin, agomelatine behaves as an antagonist at 5-HT2B and 5-HT2C receptors: blockade of the latter reinforces frontocortical adrenergic and dopaminergic transmission...
- S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine
M J Millan
Psychopharmacology Department, Institut de Recherches Servier, Centre de Recherches de Croissy, Paris, France
J Pharmacol Exp Ther 298:565-80. 2001
..It enhances extracellular levels of 5-HT and NE throughout corticolimbic structures and selectively elevates dialysis levels of DA in frontal cortex versus subcortical regions...
- Agonist and inverse agonist efficacy at human recombinant serotonin 5-HT1A receptors as a function of receptor:G-protein stoichiometry
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, Croissysur Seine, Paris, France
Neuropharmacology 36:451-9. 1997
..Furthermore, these data suggest that spiperone induces, or stabilises, a G-protein-coupled, but inactive conformation of the receptor...
- Potential antidepressants displayed combined alpha(2)-adrenoceptor antagonist and monoamine uptake inhibitor properties
A A Cordi
Institut de Recherches Servier, 11, rue des Moulineaux, F 92150 Suresnes, France
J Med Chem 44:787-805. 2001
..Structure-activity relationships permitted the selection of 14c (4(5)-[(5-fluoroindan-2-yl)methyl]-4,5-dihydroimidazole) as a development candidate...
- Inverse agonist properties of antipsychotic agents at cloned, human (h) serotonin (5-HT)(1B) and h5-HT(1D) receptors
V Audinot
Dept. of Molecular and Cellular Pharmacology, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy-sur-Seine, Paris, France
Neuropsychopharmacology 25:410-22. 2001
..In conclusion, with the exception of ziprasidone, all antipsychotics were inverse agonists at h5-HT(1B) and h5-HT(1D) receptors, although they differed markedly in their potency at these sites as compared to hD(2) receptors...
- Agonist properties of pindolol at h5-HT1A receptors coupled to mitogen-activated protein kinase
M J Millan
Psychopharmacology Department, Centre de Recherches de Croissy, Institut de Recherches Servier, 125 Chemin de Ronde, 78290 Croissy sur Seine, Paris, France
Eur J Pharmacol 424:13-7. 2001
..Thus, stimulation of MAPK provides an intracellular marker and signal for expression of the agonist actions of (-)-pindolol at h5-HT1A receptors...
- [3H]S33084: a novel, selective and potent radioligand at cloned, human dopamine D3 receptors
D Cussac
Psychopharmacology Department, Institut de Recherches Servier, Croissy sur Seine Paris, France
Naunyn Schmiedebergs Arch Pharmacol 361:569-72. 2000
..99) with that of [3H]spiperone. In conclusion, [3H]S33084 is a highly potent and selective radioligand at dopamine D3 receptors, which should be of considerable use for their characterisation...
- Pindolol antagonises G-protein activation at both pre- and postsynaptic serotonin 5-HT1A receptors: a
A Newman-Tancredi
Department of Psychopharmacology, Institut de Recherches Servier, Croissy-sur-Seine Paris, France
Naunyn Schmiedebergs Arch Pharmacol 363:391-8. 2001
..In conclusion, these data suggest that, as characterised by [35S]GTPgammaS autoradiography, and compared with 5-HT and 8-OH-DPAT, pindolol possesses low efficacy at both pre- and postsynaptic 5-HT1A receptors...
- The "selective" dopamine D1 receptor antagonist, SCH23390, is a potent and high efficacy agonist at cloned human serotonin2C receptors
M J Millan
Institut de Recherches Servier, Psychopharmacology Department, Paris, France
Psychopharmacology (Berl) 156:58-62. 2001
..57 nM. CONCLUSIONS: SCH23390 is a potent and high efficacy agonist at h5-HT2C receptors. Activation of 5-HT2C receptors by SCH23390 may contribute to its functional properties both in animals and in humans...
- Interaction of the anxiogenic agent, RS-30199, with 5-HT1A receptors: modulation of sexual activity in the male rat
M Spedding
Institut de Internationales, Servier, Croissy Research Centre, Paris, France
Neuropharmacology 37:769-80. 1998
..RS-30199 can be considered an atypical agonist at 5-HT1A receptors...
