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SerotoninReceptor, Serotonin, 5-HT2AReceptor, Serotonin, 5-HT1AReceptors, SerotoninSerotonin AntagonistsSerotonin 5-HT2 Receptor AntagonistsReceptor, Serotonin, 5-HT1BReceptors, Serotonin, 5-HT1Receptor, Serotonin, 5-HT2CReceptors, Serotonin, 5-HT3Interleukin 1 Receptor Antagonist ProteinSerotonin Plasma Membrane Transport ProteinsSerotonin Receptor AgonistsSerotonin 5-HT3 Receptor AntagonistsSerotonin Uptake InhibitorsSerotonin 5-HT1 Receptor AntagonistsNeurokinin-1 Receptor AntagonistsSerotonin 5-HT1 Receptor AgonistsSerotonin 5-HT2 Receptor AgonistsSerotonin AgentsReceptor, Serotonin, 5-HT2BReceptors, Serotonin, 5-HT2Rats, Sprague-DawleyPiperidinesDose-Response Relationship, DrugPurinergic P1 Receptor AntagonistsHistamine H2 AntagonistsExcitatory Amino Acid AntagonistsKetanserinDopamine AntagonistsAngiotensin Receptor AntagonistsAdenosine A2 Receptor AntagonistsHormone AntagonistsReceptors, Serotonin, 5-HT4Receptor, Serotonin, 5-HT1DSerotonin SyndromeRats, WistarAdenosine A1 Receptor Antagonists8-Hydroxy-2-(di-n-propylamino)tetralinSerotonin 5-HT4 Receptor AntagonistsNarcotic AntagonistsHistamine H1 AntagonistsPurinergic P2 Receptor AntagonistsMuscarinic AntagonistsReceptors, EndothelinTryptophan HydroxylaseHistamine AntagonistsGABA-A Receptor AntagonistsGABA AntagonistsRaphe NucleiPiperazinesSialoglycoproteinsReceptors, N-Methyl-D-AspartateLeukotriene AntagonistsPyridinesReceptor, Endothelin ADizocilpine MaleateBehavior, AnimalMethysergideIndolesHydroxyindoleacetic AcidBiphenyl CompoundsDrug InteractionsFluoxetineBenzazepinesAdrenergic alpha-1 Receptor AntagonistsReceptors, Interleukin-1Serotonin 5-HT3 Receptor AgonistsNeuronsTetrazoles5-HydroxytryptophanGuinea PigsRitanserinRadioligand AssayDopamineHT29 CellsSulfonamidesNicotinic AntagonistsAdrenergic alpha-2 Receptor AntagonistsXanthinesHistamine H3 AntagonistsPyrazolesSubstance PSerotonin 5-HT4 Receptor AgonistsPeptides, CyclicTime FactorsBinding, CompetitiveCitalopramReceptors, Dopamine D2HistamineReceptors, Neurokinin-1AzepinesBrainElectric StimulationLosartanGABA-B Receptor AntagonistsCells, CulturedEndothelin-1FenclonineQuinoxalines

Selective 5HT2A and 5HT6 receptor antagonists promote sleep in rats. (65/197)

STUDY OBJECTIVES: Serotonin (5-HT) has long been implicated in the control of sleep and wakefulness. This study evaluated the hypnotic efficacy of the 5-HT6 antagonist RO4368554 (RO) and the 5-HT2A receptor antagonist MDL100907 (MDL) relative to zolpidem. DESIGN: A randomized, repeated-measures design was utilized in which Wistar rats received intraperitoneal injections of RO (1.0, 3.0, and 10 mg/kg), MDL (0.1, 1.0 and 3.0 mg/kg), zolpidem (10 mg/kg), or vehicle in the middle of the dark (active) period. Electroencephalogram, electromyogram, body temperature (Tb) and locomotor activity were analyzed for 6 hours after injection. MEASUREMENTS AND RESULTS: RO, MDL, and zolpidem all produced significant increases in sleep and decreases in waking, compared with vehicle control. All 3 doses of MDL produced more consolidated sleep, increased non-rapid eye movement sleep (NREM) sleep, and increased electroencephalographic delta power during NREM sleep. The highest dose of RO (10.0 mg/kg) produced significant increases in sleep and decreases in waking during hour 2 following dosing. These increases in sleep duration were associated with greater delta power during NREM sleep. ZO Zolpidem induced sleep with the shortest latency and significantly increased NREM sleep and delta power but also suppressed rapid eye movement sleep sleep; in contrast, neither RO nor MDL affected rapid eye movement sleep. Whereas RO did not affect Tb, both zolpidem and MDL reduced Tb relative to vehicle-injected controls. CONCLUSIONS: These results support a role for 5-HT2A receptor modulation in NREM sleep and suggest a previously unrecognized role for 5-HT6 receptors in sleep-wake regulation.  (+info)

Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. (66/197)

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Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. (67/197)

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High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand. (68/197)

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Stress impairs 5-HT2A receptor-mediated serotonergic facilitation of GABA release in juvenile rat basolateral amygdala. (69/197)

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Human embryonic stem cell-derived oligodendrocyte progenitor cells express the serotonin receptor and are susceptible to JC virus infection. (70/197)

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5-Hydroxytryptamine 2A receptor signaling cascade modulates adiponectin and plasminogen activator inhibitor 1 expression in adipose tissue. (71/197)

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Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation. (72/197)

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