AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPsychiatry and PsychologyPhenomena and ProcessesDisciplines and OccupationsInformation ScienceHealth Care
DopamineSerotoninReceptors, Dopamine D2Receptor, Serotonin, 5-HT2ADopamine AntagonistsReceptors, Dopamine D1Receptor, Serotonin, 5-HT1AReceptors, SerotoninDopamine AgonistsReceptors, DopamineSerotonin AntagonistsReceptors, Dopamine D3Serotonin 5-HT2 Receptor AntagonistsReceptor, Serotonin, 5-HT1BReceptor, Serotonin, 5-HT2CReceptors, Serotonin, 5-HT1Receptors, Serotonin, 5-HT3Serotonin Plasma Membrane Transport ProteinsSerotonin Receptor AgonistsInterleukin 1 Receptor Antagonist ProteinDopamine Plasma Membrane Transport ProteinsSerotonin Uptake InhibitorsSerotonin 5-HT3 Receptor AntagonistsDopamine AgentsSerotonin 5-HT1 Receptor AntagonistsRats, Sprague-DawleyNeurokinin-1 Receptor AntagonistsDose-Response Relationship, DrugSerotonin AgentsSerotonin 5-HT1 Receptor AgonistsSerotonin 5-HT2 Receptor AgonistsReceptor, Serotonin, 5-HT2BPiperidinesDopamine Uptake InhibitorsReceptors, Serotonin, 5-HT2BenzazepinesReceptors, Dopamine D5Purinergic P1 Receptor AntagonistsExcitatory Amino Acid AntagonistsCorpus StriatumHistamine H2 AntagonistsKetanserinRats, WistarChromatography, AffinityAngiotensin Receptor AntagonistsDopamine beta-HydroxylaseAdenosine A2 Receptor AntagonistsBehavior, AnimalHormone AntagonistsReceptors, Serotonin, 5-HT4Binding, CompetitiveReceptor, Serotonin, 5-HT1DNeurons8-Hydroxy-2-(di-n-propylamino)tetralinSerotonin SyndromeAdenosine A1 Receptor AntagonistsRadioligand AssayNarcotic AntagonistsQuinpiroleHaloperidolSulpirideMicrodialysisPiperazinesHistamine H1 AntagonistsMuscarinic AntagonistsSerotonin 5-HT4 Receptor AntagonistsNucleus AccumbensPurinergic P2 Receptor AntagonistsCocaineBrainGABA AntagonistsDrug InteractionsTryptophan HydroxylaseSalicylamidesSpiperoneReceptors, EndothelinKineticsHistamine AntagonistsGABA-A Receptor AntagonistsReceptors, N-Methyl-D-AspartateRacloprideHydroxyindoleacetic AcidPyridinesProtein BindingMotor ActivityApomorphineIndolesDizocilpine MaleateRaphe NucleiSialoglycoproteinsMolecular Sequence DataNeostriatumMethysergideFluoxetineGuinea PigsLeukotriene AntagonistsReceptor, Endothelin ANicotinic AntagonistsNorepinephrinePyrrolidines
AgonistSSRIsSelective serotoninSerotonergic receptorsPotentNonselectiveHistamineAtypical antipsychoticsNeuronsSelectivelyCyproheptadineNeurotransmitterInhibitExcitatoryMental DisordersPhysiologicalHeadachePharmacologicalCommonlySynthesisAntidepressantSensoryDepressionMechanismsSpecificInvolvementLevelsResultsLevelHumanSuggestEvidence
Agonist12
  • Reserpine Depletes serotonin stores in the brain, heart, and many other organs and has been used in hypertension and psychosis Gamma-mangostin from Garcinia mangostana Serotonin receptor agonist Lindley, C. (wikipedia.org)
  • A selective agonist for serotonin 5-HT1 receptors, naratriptan has higher bioavailability and a longer half-life than sumatriptan, which may contribute to a lower rate of headache recurrences. (medscape.com)
  • A selective agonist for serotonin 5-HT1 receptors in cranial arteries, zolmitriptan suppresses the inflammation associated with migraine headaches. (medscape.com)
  • A selective 5-HT1B/1D receptor agonist, almotriptan results in cranial vessel constriction, inhibition of neuropeptide release, and reduced pain transmission in trigeminal pathways. (medscape.com)
  • Frovatriptan is a selective 5-HT1B/1D receptor agonist with a long half-life (26-30 h) and a low headache recurrence rate within 24 hours of taking the drug. (medscape.com)
  • Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D 2L receptor with K i s of 0.12 nM and 0.3 nM, respectively. (medchemexpress.com)
  • Lurasidone (SM-13496) is also a partial agonist of 5-HT 1A receptor with an IC 50 of 6.75 nM. (medchemexpress.com)
  • Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM). (medchemexpress.com)
  • Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT 2A receptor ( K i =0.6 nM) and dopamine D 2 receptor ( K i =1.4 nM), and also a partial agonist of 5-HT 1A receptor ( K i =2.9 nM). (medchemexpress.com)
  • BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with K i values of 1 nM and 49 nM, respectively. (medchemexpress.com)
  • UNC9994 hydrochloride is a functionally selective, β-arrestin-biased dopamine D 2 receptor ( D 2 R ) agonist that selectively activates β-arrestin recruitment and signaling. (medchemexpress.com)
  • UNC9994 hydrochloride shows a binding affinity with a K i of 79 nM for D 2 R . UNC9994 hydrochloride is also an antagonist of G i -regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. (medchemexpress.com)
SSRIs1
  • Selective serotonin reuptake inhibitors (SSRIs) are commonly considered suitable first-line therapy for premenstrual disorders. (medscape.com)
Selective serotonin2
  • Although some non-selective serotonin antagonists may have a particular affinity for a specific 5-HT receptor (and thus may be listed below e.g., methysergide), they still may also possess a generalised non-selective action. (wikipedia.org)
  • These drugs are selective serotonin agonists, specifically acting at 5-hydroxytryptamine 1B/1D/1F (5-HT 1B/1D/1F ) receptors on intracranial blood vessels and sensory nerve endings. (medscape.com)
Serotonergic receptors2
  • Most Axon Ligands™ in this category of compounds are labeled antipsychotic (typical, or atypical), since many of the common drugs to treat this class of mental disorders show affinity for both dopaminergic and serotonergic receptors (among several others). (axonmedchem.com)
  • These results show that in the BA 5-HT7Rs stimulate an activity-dependent enhancement of inhibitory input from local interneurons to BA principal neurons and provide insights about the possible involvement of BA serotonergic receptors in neuronal mechanisms underlying fear memory. (bvsalud.org)
Potent2
  • Brexpiprazole also shows potent antagonist activity at human noradrenergic α 1B (K i =0.17 nM) and α 2C receptors (K i =0.59 nM). (medchemexpress.com)
  • Pet1, an obligatory enhancer for serotonergic differentiation, has been identified as a potent activator of 5-HT1A autoreceptor expression. (biomedcentral.com)
Nonselective1
  • Methysergide is a 5-HT2A antagonist and nonselective 5-HT1 receptor blocker. (wikipedia.org)
Histamine1
Atypical antipsychotics2
  • Antagonists of the 5-HT2A receptor are sometimes used as atypical antipsychotics (contrast with typical antipsychotics, which are purely dopamine antagonists). (wikipedia.org)
  • 5] Side effects of atypical antipsychotics: a brief overview. (axonmedchem.com)
Neurons8
  • In such cases, the dendrites (a neuron's receiving branches) on the postsynaptic neurons release neurotransmitters that affect receptors on the presynaptic neurons. (msdmanuals.com)
  • The serotonin-1A (5-HT1A) receptor is among the most abundant and widely distributed 5-HT receptors in the brain, but is also expressed on serotonin neurons as an autoreceptor where it plays a critical role in regulating the activity of the entire serotonin system. (biomedcentral.com)
  • this is flanked by a series of upstream repressor elements for REST, Freud-1/CC2D1A and Freud-2/CC2D1B factors that not only restrict its expression to neurons, but may also regulate the level of expression of 5-HT1A receptors in various subsets of neurons, including serotonergic neurons. (biomedcentral.com)
  • Elevated 5-HT1A autoreceptor expression would tend to reduce the activity of 5-HT neurons, while reduced post-synaptic 5-HT1A receptors would result in a blunted behavioral response to 5-HT. (biomedcentral.com)
  • The effects of 5-HT7 receptor (5-HT7R) activation and blockade on the activity of BA neurons have not yet been investigated. (bvsalud.org)
  • In the present study, a transgenic mouse line carrying green fluorescent protein (GFP) reporter gene was used to identify neurons that express the 5-HT7R. (bvsalud.org)
  • Activation of 5-HT7Rs resulted in a depolarization and/or occurrence of spontaneous spiking activity of BA interneurons that was accompanied by an increase in the mean frequency and mean amplitude of spontaneous inhibitory postsynaptic currents (sIPSCs) recorded from BA principal neurons. (bvsalud.org)
  • Activation of 5-HT7Rs also decreased the mean frequency of spontaneous excitatory postsynaptic currents (sEPSCs) recorded from BA principal neurons, which was blocked by the GABAA receptor antagonist picrotoxin. (bvsalud.org)
Selectively2
  • Risperidone antipsychotic Trazodone Nefazodone Another subclass consists of drugs selectively acting at the 5-HT3 receptors, and thus are known as 5-HT3 antagonists. (wikipedia.org)
  • Taken together, these results highlight an integrated regulation of 5-HT1A autoreceptors that differs in several aspects from regulation of post-synaptic 5-HT1A receptors, and could be selectively targeted to enhance serotonergic neurotransmission. (biomedcentral.com)
Cyproheptadine3
  • They include, but are not limited to: Cyproheptadine blocks 5-HT2A, H1 and is a mild anticholinergic. (wikipedia.org)
  • They include, but are not limited to: Chlorpromazine Cyproheptadine Metergoline Methysergide Mianserin Mirtazapine Oxetorone Pizotifen Propranolol Ritanserin Spiperone Carbinoxamine Cinnarizine Cyproheptadine Hydroxyzine Methdilazine Pizotifen Promethazine Pizotifen is a 5-HT2C antagonist, H1 blocker and anticholinergic useful in migraine prophylaxis. (wikipedia.org)
  • Here we investigated the locomotor pattern during recovery from blockade of 5-HT7 or 5-HT2A receptors after intrathecal application of SB269970 or cyproheptadine in adult rats with chronic intrathecal cannula implanted in the lumbar spinal cord. (bvsalud.org)
Neurotransmitter1
  • The signal may stimulate or inhibit the receiving cell, depending on the neurotransmitter and receptor involved. (msdmanuals.com)
Inhibit1
Excitatory2
  • Depending on the receptor, the response may be excitatory or inhibitory. (msdmanuals.com)
  • Neither inhibitory nor excitatory miniature postsynaptic currents (mIPSCs/mEPSCs) were affected by 5-HT7R activation. (bvsalud.org)
Mental Disorders1
  • 1, 2] PMDD is listed as a mental disorder in the fifth edition of the American Psychiatric Association's Diagnostic and Statistical Manual of Mental Disorders (DSM-5), whereas PMS is not. (medscape.com)
Physiological1
  • Serotonin modulates several physiological and cognitive pathways throughout the human body that affect emotions, memory, sleep, and thermal regulation. (bvsalud.org)
Headache1
  • The American Headache Society released a list of 5 commonly performed tests or procedures that are not always necessary in the treatment of migraine and headache, as part of the American Board of Internal Medicine (ABIM) Foundation's Choosing Wisely campaign. (medscape.com)
Pharmacological2
  • Since DHE displays affinity for these receptors, this study investigated the pharmacological profile of DHE-induced inhibition of the vasodepressor sensory CGRPergic outflow. (eur.nl)
  • As discussed in this review, the serotonergic system offers great potential for the development of new antidepressant therapies based on the combination of SERT inhibition with different pharmacological activity towards the 5-HT system. (bvsalud.org)
Commonly1
  • Alterations in 5-HT1A receptor levels are commonly observed in depressed individuals. (biomedcentral.com)
Synthesis1
  • PCPA) An inhibitor of serotonin synthesis that has been used in the treatment of carcinoid syndrome. (wikipedia.org)
Antidepressant1
  • They include, but are not limited to: Dolasetron Granisetron Ondansetron Palonosetron Tropisetron Other 5-HT3 antagonists have been considered for use in the treatment of irritable bowel syndrome: Alosetron Cilansetron Also, the antidepressant mirtazapine acts as a 5-HT3 antagonist. (wikipedia.org)
Sensory1
  • furthermore, it inhibits the vasodepressor sensory CGRPergic outflow, but the receptors involved remain unknown. (eur.nl)
Depression3
  • Over-expression of the 5-HT1A autoreceptor has been implicated in reducing serotonergic neurotransmission, and is associated with major depression and suicide. (biomedcentral.com)
  • The complex nature of the serotonergic system and interactions with other neurochemical systems indicate that the development of depression may be mediated by various pathomechanisms, the common denominator of which is undoubtedly the disturbed transmission in central 5-HT synapses. (bvsalud.org)
  • The aim of this article is to summarize the search for new antidepressants in recent years, focusing primarily on the possibility of benefiting from interactions with various 5-HT receptors in the pharmacotherapy of depression. (bvsalud.org)
Mechanisms1
  • However, the mechanisms underlying these differential changes in 5-HT1A receptor expression remain unclear. (biomedcentral.com)
Specific2
  • Neurotransmitters diffuse across the synaptic cleft and bind briefly to specific receptors on the adjoining neuron or effector cell. (msdmanuals.com)
  • These effects were blocked by a specific 5-HT7R antagonist, SB269970 and were absent in slices from 5-HT7R knockout mice. (bvsalud.org)
Involvement1
  • In particular, we found correlations between three adrenergic receptor subtypes and alcohol deliveries which could indicate an involvement of stress in the choice to self-administer. (5dok.org)
Levels1
  • mRNA expression levels of a number of receptors was determined using real-time PCR. (5dok.org)
Results1
  • Prejunctional activation of α2A/2C-adrenergic, serotonin 5-HT1B/1F, or dopamine D2-like receptors results in inhibition of this CGRPergic outflow. (eur.nl)
Level1
  • The level of serotonin (5-HT) in the BA increases due to arousal and stress related to aversive stimuli. (bvsalud.org)
Human1
  • Phylogenetic analysis of 277 human G-protein-coupled receptors as a tool for the prediction of orphan receptor ligands. (axonmedchem.com)
Suggest1
  • We suggest that modulation of the 5-HT7 receptors on interneurons located in lamina VII with ascending projections to the forelimb spinal network can be responsible for the 2FL-1HL locomotor pattern. (bvsalud.org)
Evidence1
  • This review examines the evidence that alterations in transcriptional regulation of the 5-HT1A receptor could underlie its dys-regulation in mental illness. (biomedcentral.com)