Antipsychotics differ in their ability to internalise human dopamine D2S and human serotonin 5-HT1A receptors in HEK293 cells.

PubWeight™: 0.80‹?›

🔗 View Article (PMID 18190908)

Published in Eur J Pharmacol on November 28, 2007

Authors

Peter Heusler1, Adrian Newman-Tancredi, Timothé Loock, Didier Cussac

Author Affiliations

1: Cellular and Molecular Biology Department, Pierre Fabre Research Center, F-81106 Castres, France. peter.heusler@pierre-fabre.com

Articles by these authors

Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther (2002) 1.87

Triptolide is an inhibitor of RNA polymerase I and II-dependent transcription leading predominantly to down-regulation of short-lived mRNA. Mol Cancer Ther (2009) 1.32

Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes. J Pharmacol Exp Ther (2002) 1.14

The role of dopamine D3 compared with D2 receptors in the control of locomotor activity: a combined behavioural and neurochemical analysis with novel, selective antagonists in rats. Psychopharmacology (Berl) (2004) 1.09

Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells. Eur J Pharmacol (2008) 1.06

Differential activation of Gq/11 and Gi(3) proteins at 5-hydroxytryptamine(2C) receptors revealed by antibody capture assays: influence of receptor reserve and relationship to agonist-directed trafficking. Mol Pharmacol (2002) 1.05

Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor. J Pharmacol Exp Ther (2002) 0.98

Novel antipsychotic agents with 5-HT(1A) agonist properties: role of 5-HT(1A) receptor activation in attenuation of catalepsy induction in rats. Neuropharmacology (2005) 0.97

S33138 [N-[4-[2-[(3aS,9bR)-8-cyano-1,3a,4,9b-tetrahydro[1]-benzopyrano[3,4-c]pyrrol-2(3H)-yl)-ethyl]phenylacetamide], a preferential dopamine D3 versus D2 receptor antagonist and potential antipsychotic agent: I. Receptor-binding profile and functional actions at G-protein-coupled receptors. J Pharmacol Exp Ther (2007) 0.94

Effects of antipsychotics and reference monoaminergic ligands on marble burying behavior in mice. Behav Pharmacol (2008) 0.92

Penile erection and yawning induced by dopamine D2-like receptor agonists in rats: influence of strain and contribution of dopamine D2, but not D3 and D4 receptors. Behav Pharmacol (2009) 0.91

Discovery of novel protease activated receptors 1 antagonists with potent antithrombotic activity in vivo. J Med Chem (2009) 0.91

5-HT(1A) [corrected] receptors in mood and anxiety: recent insights into autoreceptor versus heteroreceptor function. Psychopharmacology (Berl) (2013) 0.91

F15599, a highly selective post-synaptic 5-HT(1A) receptor agonist: in-vivo profile in behavioural models of antidepressant and serotonergic activity. Int J Neuropsychopharmacol (2010) 0.91

Pharmacological profiles in rats of novel antipsychotics with combined dopamine D2/serotonin 5-HT1A activity: comparison with typical and atypical conventional antipsychotics. Behav Pharmacol (2007) 0.90

Antipsychotic drug action on SREBPs-related lipogenesis and cholesterogenesis in primary rat hepatocytes. Naunyn Schmiedebergs Arch Pharmacol (2010) 0.90

Antipsychotic-like vs cataleptogenic actions in mice of novel antipsychotics having D2 antagonist and 5-HT1A agonist properties. Neuropsychopharmacology (2005) 0.90

The five choice serial reaction time task: comparison between Sprague-Dawley and Long-Evans rats on acquisition of task, and sensitivity to phencyclidine. Pharmacol Biochem Behav (2009) 0.89

Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols. Naunyn Schmiedebergs Arch Pharmacol (2002) 0.89

Differential profile of antipsychotics at serotonin 5-HT1A and dopamine D2S receptors coupled to extracellular signal-regulated kinase. Eur J Pharmacol (2006) 0.89

Contrasting contribution of 5-hydroxytryptamine 1A receptor activation to neurochemical profile of novel antipsychotics: frontocortical dopamine and hippocampal serotonin release in rat brain. J Pharmacol Exp Ther (2005) 0.89

Actions of novel antipsychotic agents on apomorphine-induced PPI disruption: influence of combined serotonin 5-HT1A receptor activation and dopamine D2 receptor blockade. Neuropsychopharmacology (2006) 0.88

Anatomically selective serotonergic type 1A and serotonergic type 2A therapies for Parkinson's disease: an approach to reducing dyskinesia without exacerbating parkinsonism? J Pharmacol Exp Ther (2011) 0.88

F15599, a preferential post-synaptic 5-HT1A receptor agonist: activity in models of cognition in comparison with reference 5-HT1A receptor agonists. Eur Neuropsychopharmacol (2010) 0.88

Native rat hippocampal 5-HT1A receptors show constitutive activity. Mol Pharmacol (2006) 0.87

Protease-activated receptor-1 mediates thrombin-induced persistent sodium current in human cardiomyocytes. Mol Pharmacol (2008) 0.86

Effects of novel antipsychotics with mixed D(2) antagonist/5-HT(1A) agonist properties on PCP-induced social interaction deficits in the rat. Neuropharmacology (2005) 0.86

Direct protective effects of poly-unsaturated fatty acids, DHA and EPA, against activation of cardiac late sodium current: a mechanism for ischemia selectivity. Basic Res Cardiol (2007) 0.86

[18F]F15599, a novel 5-HT1A receptor agonist, as a radioligand for PET neuroimaging. Eur J Nucl Med Mol Imaging (2009) 0.85

Partial agonist properties of the antipsychotics SSR181507, aripiprazole and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release. Eur J Pharmacol (2006) 0.85

Antibody capture assay reveals bell-shaped concentration-response isotherms for h5-HT(1A) receptor-mediated Galpha(i3) activation: conformational selection by high-efficacy agonists, and relationship to trafficking of receptor signaling. Mol Pharmacol (2002) 0.85

A postmortem study to compare agonist and antagonist 5-HT1A receptor-binding sites in Alzheimer's disease. CNS Neurosci Ther (2014) 0.84

WAY-100635 has high selectivity for serotonin 5-HT(1A) versus dopamine D(4) receptors. Eur J Pharmacol (2007) 0.84

Differential agonist and inverse agonist profile of antipsychotics at D2L receptors coupled to GIRK potassium channels. Neuropharmacology (2007) 0.84

Milnacipran is active in models of irritable bowel syndrome and abdominal visceral pain in rodents. Eur J Pharmacol (2011) 0.84

The antipsychotics clozapine and olanzapine increase plasma glucose and corticosterone levels in rats: comparison with aripiprazole, ziprasidone, bifeprunox and F15063. Eur J Pharmacol (2008) 0.84

Dual, hyperalgesic, and analgesic effects of the high-efficacy 5-hydroxytryptamine 1A (5-HT1A) agonist F 13640 [(3-chloro-4-fluoro-phenyl)-[4-fluoro-4-{[(5-methyl-pyridin-2-ylmethyl)-amino]-methyl}piperidin-1-yl]methanone, fumaric acid salt]: relationship with 5-HT1A receptor occupancy and kinetic parameters. J Pharmacol Exp Ther (2004) 0.83

Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. J Med Chem (2007) 0.83

Anticataleptic properties of alpha2 adrenergic antagonists in the crossed leg position and bar tests: differential mediation by 5-HT1A receptor activation. Psychopharmacology (Berl) (2004) 0.83

Evaluation of milnacipran, in comparison with amitriptyline, on cold and mechanical allodynia in a rat model of neuropathic pain. Eur J Pharmacol (2011) 0.83

The central serotonin 2B receptor: a new pharmacological target to modulate the mesoaccumbens dopaminergic pathway activity. J Neurochem (2010) 0.82

In vivo occupancy of dopamine D2 receptors by antipsychotic drugs and novel compounds in the mouse striatum and olfactory tubercles. Naunyn Schmiedebergs Arch Pharmacol (2006) 0.82

Clozapine, ziprasidone and aripiprazole but not haloperidol protect against kainic acid-induced lesion of the striatum in mice, in vivo: role of 5-HT1A receptor activation. Brain Res (2005) 0.81

S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic characterization. J Pharmacol Exp Ther (2011) 0.81

High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. J Med Chem (2007) 0.81

Differential profile of typical, atypical and third generation antipsychotics at human 5-HT7a receptors coupled to adenylyl cyclase: detection of agonist and inverse agonist properties. Naunyn Schmiedebergs Arch Pharmacol (2007) 0.81

Region-specific changes in 5-HT1A agonist-induced Extracellular signal-Regulated Kinases 1/2 phosphorylation in rat brain: a quantitative ELISA study. Neuropharmacology (2008) 0.81

Cellular BRET assay suggests a conformational rearrangement of preformed TrkB/Shc complexes following BDNF-dependent activation. Cell Signal (2009) 0.81

Action of novel antipsychotics at human dopamine D3 receptors coupled to G protein and ERK1/2 activation. Neuropharmacology (2007) 0.80

Agonist and antagonist properties of antipsychotics at human dopamine D4.4 receptors: G-protein activation and K+ channel modulation in transfected cells. Int J Neuropsychopharmacol (2007) 0.80

Serotonin 5-HT1A Receptors and Antipsychotics - An Update in Light of New Concepts and Drugs. Curr Pharm Des (2015) 0.80

Ligand modulation of [35S]GTPgammaS binding at human alpha(2A), alpha(2B) and alpha(2C) adrenoceptors. Cell Signal (2002) 0.80

Actions of the prototypical 5-HT1A receptor agonist 8-OH-DPAT at human alpha2-adrenoceptors: (+)8-OH-DPAT, but not (-)8-OH-DPAT is an alpha2B subtype preferential agonist. Eur J Pharmacol (2010) 0.79

Overweight induced by chronic risperidone exposure is correlated with overexpression of the SREBP-1c and FAS genes in mouse liver. Naunyn Schmiedebergs Arch Pharmacol (2011) 0.79

F15063, a potential antipsychotic with dopamine D(2)/D(3) receptor antagonist and 5-HT(1A) receptor agonist properties: influence on immediate-early gene expression in rat prefrontal cortex and striatum. Eur J Pharmacol (2009) 0.79

Antipsychotic, antidepressant, and cognitive-impairment properties of antipsychotics: rat profile and implications for behavioral and psychological symptoms of dementia. Naunyn Schmiedebergs Arch Pharmacol (2014) 0.78

Radiosynthesis and preclinical evaluation of 18F-F13714 as a fluorinated 5-HT1A receptor agonist radioligand for PET neuroimaging. J Nucl Med (2012) 0.78

Activation of G proteins and extracellular signal-regulated kinase 1/2 phosphorylation via human dopamine D4.4 receptors: differential pathway-dependent potencies of receptor agonists. Naunyn Schmiedebergs Arch Pharmacol (2008) 0.78

Does endoplasmic reticulum stress participate in APD-induced hepatic metabolic dysregulation? Neuropharmacology (2011) 0.78

In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat. Psychopharmacology (Berl) (2011) 0.78

Stimulation by antipsychotic agents of mitogen-activated protein kinase (MAPK) coupled to cloned, human (h)serotonin (5-HT)(1A) receptors. Psychopharmacology (Berl) (2002) 0.78

Effects of milnacipran, duloxetine and indomethacin, in polyarthritic rats using the Randall-Selitto model. Behav Pharmacol (2011) 0.78

Differential ion current activation by human 5-HT(1A) receptors in Xenopus oocytes: evidence for agonist-directed trafficking of receptor signalling. Neuropharmacology (2005) 0.78

Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols. J Med Chem (2002) 0.77

Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors disrupt basal PPI of the startle reflex in rats. Psychopharmacology (Berl) (2007) 0.77

Neuropharmacological profile of bifeprunox: merits and limitations in comparison with other third-generation antipsychotics. Curr Opin Investig Drugs (2007) 0.77

[(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand. Naunyn Schmiedebergs Arch Pharmacol (2010) 0.77

S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole. J Pharmacol Exp Ther (2004) 0.77

Pharmacological characterization of protease activated receptor-1 by a serum responsive element-dependent reporter gene assay: major role of calmodulin. Biochem Pharmacol (2006) 0.76

h5-HT(1B) receptor-mediated constitutive Galphai3-protein activation in stably transfected Chinese hamster ovary cells: an antibody capture assay reveals protean efficacy of 5-HT. Br J Pharmacol (2003) 0.76

The clozapine metabolite N-desmethylclozapine displays variable activity in diverse functional assays at human dopamine D₂ and serotonin 5-HT₁A receptors. Eur J Pharmacol (2011) 0.76

Competitive interaction of 5-HT(1A) receptors with G-protein subtypes in CHO cells demonstrated by RNA interference. Cell Signal (2010) 0.76

Apomorphine-induced emesis in dogs: differential sensitivity to established and novel dopamine D2/5-HT(1A) antipsychotic compounds. Eur J Pharmacol (2008) 0.76

Differences among conventional, atypical and novel putative D(2)/5-HT(1A) antipsychotics on catalepsy-associated behaviour in cynomolgus monkeys. Behav Brain Res (2009) 0.75

Potencies and unblocking kinetic properties of antagonists at recombinant human NMDA receptors in a Xenopus oocytes model. Naunyn Schmiedebergs Arch Pharmacol (2015) 0.75

F15063, a potential antipsychotic with dopamine D(2)/D(3) antagonist, 5-HT(1A) agonist and D(4) partial agonist properties: (IV) duration of brain D2-like receptor occupancy and antipsychotic-like activity versus plasma concentration in mice. Naunyn Schmiedebergs Arch Pharmacol (2007) 0.75

F15063, a potential antipsychotic with dopamine D2/D3 receptor antagonist, 5-HT1A receptor agonist and dopamine D4 receptor partial agonist properties: influence on neuronal firing and neurotransmitter release. Eur J Pharmacol (2009) 0.75

Rigid analogues of the α2-adrenergic blocker atipamezole: small changes, big consequences. J Med Chem (2010) 0.75