ReceptorsPost-synapticAutoreceptorsSerotonin 1A receptorReceptor antagonistAutoreceptorNeuronsBuspironeSingle-nucleotide pReuptake inhibitorsSSRIsUnclearSubtypeTranscriptionalDifferentialNorepinephrinePostsynapticAlterationsAntidepressantMiceModulatoryAmygdalaHippocampusInhibitionIncreasesEfficacyVivoFunctionalChronicCommonlyStudyEffectLearning and memoryRoleStudiesBrainSuggestCellsJournal
Receptors28
- The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, that binds serotonin, also known as 5-HT, a neurotransmitter. (wikipedia.org)
- The 5-HT1A receptor is the most widespread of all the 5-HT receptors. (wikipedia.org)
- In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus. (wikipedia.org)
- The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors. (wikipedia.org)
- These effects are the result of activation of 5-HT1A receptors within the rostral ventrolateral medulla. (wikipedia.org)
- Activation of central 5-HT1A receptors triggers the release or inhibition of norepinephrine depending on species, presumably from the locus coeruleus, which then reduces or increases neuronal tone to the iris sphincter muscle by modulation of postsynaptic α2-adrenergic receptors within the Edinger-Westphal nucleus, resulting in pupil dilation in rodents, and pupil constriction in primates including humans. (wikipedia.org)
- Mice lacking 5-HT1A receptors altogether (knockout) show increased anxiety but lower depressive-like behaviour. (wikipedia.org)
- 5-HT1A receptors in the dorsal raphe nucleus are co-localized with neurokinin 1 (NK1) receptors and have been shown to inhibit the release of substance P, their endogenous ligand. (wikipedia.org)
- The activation of 5-HT1A receptors has been demonstrated to impair certain aspects of memory (affecting declarative and non-declarative memory functions) and learning (due to interference with memory-encoding mechanisms), by inhibiting the release of glutamate and acetylcholine in various areas of the brain. (wikipedia.org)
- 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)
- 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)
- 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)
- However, it is unclear whether 5-HT1A receptor antagonists not discriminating between pre- and post-synaptic 5-HT 1A receptors would be clinically effective. (uab.cat)
- Key results: DU-125530 showed equal (low nM) potency to displace agonist and antagonist binding to pre- and post-synaptic 5-HT1A receptors in rat and human brain. (uab.cat)
- DU-125530 augmented SSRI-induced increases in extracellular 5-HT as effectively as in mice lacking 5-HT1A receptors, indicating a silent, maximal occupancy of pre-synaptic 5-HT1A receptors at the dose used. (uab.cat)
- However, blockade of post-synaptic 5- HT1A receptors by DU-125530 cancels benefits obtained by enhancing pre-synaptic 5-hydroxytryptaminergic function. (uab.cat)
- 4 - 6 5-HT receptors are involved not only in normal physiological function of brain like, sleep, memory, feeding and etc., but also in various psychiatric problems. (j-epilepsy.org)
- Because of the putative role of the serotonergic system in central physiological and pathological functions and the crucial need of identifying a novel target to prevent memory deficit in epilepsy, some serotonergic excitatory (5-HT 2A/2C ) and inhibitory receptors (5-HT 1A ) were selected for the study. (j-epilepsy.org)
- Activated postsynaptic 5-HT1A receptors promote hyperpolarization to released 5-HT on pyramidal neurons.8, The anxiolytic action of buspirone is mainly thought to arise from the interaction at presynaptic 5-HT1A autoreceptors. (arlen.com.br)
- Some evidence has indicated 5-HT and its receptors regulate the cognitive functions, including learning and memory ( 4 - 7 ). (frontiersin.org)
- The 5-HT 1A receptors can influence the activity of cholinergic, glutamatergic and GABAergic neurons in the cerebral cortex and hippocampus to affect the declarative and non-declarative memory. (frontiersin.org)
- And the 5-HT 1A receptors regulate several transduction mechanisms in the memory formation. (frontiersin.org)
- The firing of 5-HT neurons is known to be under 5-HT1A receptor-mediated autoinhibition, but functional consequences of coexpressed receptors are unknown. (bvsalud.org)
- Using co-immunoprecipitation, BRET, confocal, and super-resolution microscopy in hippocampal and 5-HT neurons, we present evidence that 5-HT1A and 5-HT2B receptors can form heterodimers and co-cluster at the plasma membrane of dendrites. (bvsalud.org)
- Selective agonist stimulation of coexpressed 5-HT1A and 5-HT2B receptors prevents 5-HT1A receptor internalization and increases 5-HT2B receptor membrane clustering. (bvsalud.org)
- Current clamp recordings of 5-HT neurons revealed that 5-HT1A receptor stimulation of acute slices from mice lacking 5-HT2B receptors in 5-HT neurons increased their firing activity trough Ca2+-activated potassium channel inhibition compared to 5-HT neurons from control mice. (bvsalud.org)
- This work supports the hypothesis that the relative expression of 5-HT1A and 5-HT2B receptors tunes the neuronal excitability of serotonergic neurons through potassium channel regulation. (bvsalud.org)
Post-synaptic2
- In this review, we describe major adaptive changes in pre- and post-synaptic 5-HT neurotransmission as well as alterations in gene transcription and neurotrophic factors in response to long-term treatment with conventional antidepressants, new putative ones or novel promising drug candidates, all acting via 5-HT system. (heraldopenaccess.us)
- Conclusions and implications: DU-125530 is an excellent pre- and post-synaptic 5-HT1A receptor antagonist. (uab.cat)
Autoreceptors1
- 5-HT1A receptor antagonists augment antidepressant-like effects in rodents by preventing this negative feedback, and the mixed β-adrenoceptor/5-HT1A receptor antagonist pindolol improves clinical antidepressant effects by preferentially interacting with 5-HT 1A autoreceptors. (uab.cat)
Serotonin 1A receptor2
- In humans, the serotonin 1A receptor is encoded by the HTR1A gene. (wikipedia.org)
- In this study, the association between a single-nucleotide polymorphism (SNP) of the serotonin 1A receptor gene (HTR1A) rs6295 and TD was investigated. (kjsr.org)
Receptor antagonist4
- The sympatholytic antihypertensive drug urapidil is an α1-adrenergic receptor antagonist and 5-HT1A receptor agonist, and it has been demonstrated that the latter property contributes to its overall therapeutic effects. (wikipedia.org)
- Experimental approach: We characterized the pharmacological properties of the 5-HT1A receptor antagonist DU-125530 using receptor autoradiography, intracerebral microdialysis and electrophysiological recordings. (uab.cat)
- 5-HT 1A receptor agonist improved the memory functions while seizure severity was not improved, and the opposite effect was observed with 5-HT 1A receptor antagonist. (j-epilepsy.org)
- 8 Typically, 5-HT 1A receptor antagonist has been reported to impair memory, whereas agonist has been found reverse memory deficit. (j-epilepsy.org)
Autoreceptor3
- Over-expression of the 5-HT1A autoreceptor has been implicated in reducing serotonergic neurotransmission, and is associated with major depression and suicide. (biomedcentral.com)
- Pet1, an obligatory enhancer for serotonergic differentiation, has been identified as a potent activator of 5-HT1A autoreceptor expression. (biomedcentral.com)
- abstract = "Background and purpose: The antidepressant efficacy of selective 5-HT reuptake inhibitors (SSRI) and other 5-HT-enhancing drugs is compromised by a negative feedback mechanism involving 5-HT1A autoreceptor activation by the excess 5-HT produced by these drugs in the somatodendritic region of 5-HT neurones. (uab.cat)
Neurons1
- Nociceptive information is transmitted through thinly myelinated Aδ-afferent and unmyelinated C-afferent fibers from the periphery to the spinal cord, especially substantia gelatinosa (SG) neurons, 5,6 where the information is modulated. (silverchair.com)
Buspirone3
- 5-HT1A receptor agonists like buspirone and flesinoxan show efficacy in relieving anxiety and depression, and buspirone and tandospirone are currently approved for these indications in various parts of the world. (wikipedia.org)
- Belonging to the azaspirodecanedione drug class, 2 buspirone is a serotonin 5-HT 1A receptor agonist that is not chemically or pharmacologically related to benzodiazepines, barbiturates, and other sedative/anxiolytic drugs. (arlen.com.br)
- Subjects receiving buspirone 5 mg b. (cemona.es)
Single-nucleotide p1
- In this study, we evaluated whether the single-nucleotide polymorphism (SNP) rs198585630 of 5-HT 1A receptor is associated with cognitive alterations in rats after microwave exposure with a frequency of 2.856 GHz and an average power density of 30 mW/cm 2 . (frontiersin.org)
Reuptake inhibitors1
- Some of the atypical antipsychotics like lurasidone and aripiprazole are also partial agonists at the 5-HT1A receptor and are sometimes used in low doses as augmentations to standard antidepressants like the selective serotonin reuptake inhibitors (SSRIs). (wikipedia.org)
SSRIs1
- It antagonized suppression of 5-hydroxytryptaminergic activity evoked by 8-OH-DPAT and SSRIs in vivo. (uab.cat)
Unclear1
- However, the mechanisms underlying these differential changes in 5-HT1A receptor expression remain unclear. (biomedcentral.com)
Subtype1
- The 5-HT 1A subtype is of particular interest since it plays an important regulatory role in the 5-HT system as one of the main mediators of the action of 5-HT and a potential target for enhancing cognition ( 8 , 10 - 12 ). (frontiersin.org)
Transcriptional4
- 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)
- Transcriptional activity of 5-HT 1A receptor promoter containing rs198585630 C/T allele was determined in vitro . (frontiersin.org)
- We demonstrated that transcriptional activity of 5-HT 1A receptor promoter containing rs198585630 C allele was higher than that of 5-HT 1A receptor promoter containing T allele. (frontiersin.org)
- The transcriptional activity of 5-HT 1A receptor promoter was stimulated by 30 mW/cm 2 microwave exposure, and rs198585630 C allele was more sensitive to microwave exposure, as it showed stronger transcriptional activation. (frontiersin.org)
Differential1
- Differential effect of 5-HT 1A receptor agonist has been reported in epilepsy. (j-epilepsy.org)
Norepinephrine2
- These drawbacks are largely due to the absence of diversity in the mode of action of conventional antidepressants, which act principally via an enhancement of synaptic transmission of the monoamines serotonin (5-HT) and/or Norepinephrine (NE) [21]. (heraldopenaccess.us)
- Both actions of norepinephrine were mimicked by an alpha2 adrenoceptor agonist, clonidine (10 microm), and an alpha 2A agonist, oxymetazoline (10 microm), but not by an alpha1 agonist, phenylephrine (10 microm), and a beta agonist, isoproterenol (40 microm). (silverchair.com)
Postsynaptic1
- Enhancement of dopamine release in these areas may also play a major role in the antidepressant and anxiolytic effects seen upon postsynaptic activation of the 5-HT1A receptor. (wikipedia.org)
Alterations1
- Alterations in 5-HT1A receptor levels are commonly observed in depressed individuals. (biomedcentral.com)
Antidepressant1
- In addition to being antidepressant and anxiolytic in effect, 5-HT1A receptor activation has also been demonstrated to be antiemetic and analgesic, and all of these properties may be mediated in part or full, depending on the property in question, by NK1 receptor inhibition. (wikipedia.org)
Mice2
- Therefore, this study has been envisaged to explore the effect of 5-HT 1A and 5-HT 2A/2C receptor modulation on epilepsy and memory deficit in pentylenetetrazole-kindled mice. (j-epilepsy.org)
- In the present experimental approach, we examined the efficacy of modulation of 5-HT 1A and 5-HT 2A/2C receptor in pentylenetetrazole-induced kindling in male Swiss mice (n=75). (j-epilepsy.org)
Modulatory1
- The main mechanism underlying the modulatory effects of 5-HT is an alteration in 5-HT receptor density during memory formation and in amnesic states ( 8 , 9 ). (frontiersin.org)
Amygdala1
- 5-HT 1A receptor agonist has been reported to augment the latency to seizures in acute model of convulsions, while no effect has been observed in chronic amygdala kindling model. (j-epilepsy.org)
Hippocampus2
- 5-HT1A receptor activation has been shown to increase dopamine release in the medial prefrontal cortex, striatum, and hippocampus, and may be useful for improving the symptoms of schizophrenia and Parkinson's disease. (wikipedia.org)
- 5-HT 2A/2C receptor appears to be widely expressed in cortex and hippocampus which regulates central nervous system excitability. (j-epilepsy.org)
Inhibition1
- Rats carrying rs198585630 C allele exhibited increased mRNA and protein expression of 5-HT 1A receptor and were more susceptible to 30 mW/cm 2 microwave exposure, showing cognitive deficits and inhibition of brain electrical activity. (frontiersin.org)
Increases1
- Vasodilation of the blood vessels in the skin via central 5-HT1A activation increases heat dissipation from the organism out into the environment, causing a decrease in body temperature. (wikipedia.org)
Efficacy1
- As mentioned above, some of the atypical antipsychotics are 5-HT1A receptor partial agonists, and this property has been shown to enhance their clinical efficacy. (wikipedia.org)
Vivo1
- Electroencephalograms (EEGs), spatial learning and memory, and mRNA and protein expression of 5-HT 1A receptor were evaluated in vivo . (frontiersin.org)
Functional1
- The 5-HT receptor family includes at least 7 classes (5-HT 1−7 receptor) and 15 subtypes with different functional and transduction properties. (frontiersin.org)
Chronic1
- Chronic microwave exposure can induce cognitive deficits, and 5-HT system is involved in this effect. (frontiersin.org)
Commonly1
- 5-HT1A receptor activation likely plays a significant role in the positive effects of serotonin releasing agents (SRAs) like MDMA (commonly known as ecstasy) as well. (wikipedia.org)
Study2
- A recent study estimates the prevalence of MDD at 4.4% to 5% in the general population with an annual incidence of 2.4% to 3.8% [2]. (heraldopenaccess.us)
- The outcome of the study indicates the possible involvement of 5-HT 2A/2C receptor in the pathogenesis of epilepsy and associated memory deficit, which can be further explored for its management. (j-epilepsy.org)
Effect1
- 5-HT 1A receptor is predominantly distributed in limbic area and has been reported to exhibit antiepileptic effect. (j-epilepsy.org)
Learning and memory1
- 9 In contrast, some studies suggest that 5-HT 1A receptor agonist may impair learning and memory in normal animals. (j-epilepsy.org)
Role1
- The 5-hydroxytryptamine (5-HT) play an important role in the cognition, emotion and brain development. (frontiersin.org)
Studies1
- These studies implicate the 5-HT1A receptor as an important determinant of predisposition to mental illness. (biomedcentral.com)
Brain1
- 5-HT1A is expressed in the brain, spleen, and neonatal kidney. (wikipedia.org)
Suggest1
- These findings suggest SNP rs198585630 of the 5-HT 1A receptor is an important target for further research exploring the mechanisms of hypersensitivity to microwave exposure. (frontiersin.org)
Cells1
- PC12 cells and 293T cells were exposed to microwaves for 5 min up to 3 times at 2 intervals of 5 min. (frontiersin.org)
Journal1
- British Journal of Pharmacology , 167 (5), 1021-1034. (uab.cat)