What Do We Really Know About 5-HT1A Receptor Signaling in Neuronal Cells?

Rojas, Paulina S.; Fiedler, Jenny L.

doi:10.3389/fncel.2016.00272

Cited by 72 publications

(43 citation statements)

References 64 publications

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“…Unlike other atypical antipsychotics approved by FDA (e.g., clozapine, olanzapine, quetiapine, ziprasidone, and risperidone), which are D 2 R antagonists, 7 behaves as a D 2 R and D 3 R partial agonist. Moreover, it shows partial agonism at 5-HT 1A Rs and, similarly to the other atypical antipsychotics, is an antagonist at 5-HT 2A Rs and 5-HT 7 Rs as well as a partial agonist at 5-HT 2C Rs [23].…”

Section: Modification Of the Spacermentioning

confidence: 95%

“…Nevertheless, various other pathways are coupled to this receptor depending on the target cell. Indeed, 5-HT 1A R stimulation activates or inhibits different enzymes, channels, and kinases, as well as modulates the production of several second messengers ( Figure 4) [6,7].…”

Section: Signal Transduction Pathways Of 5-ht 1a Rsmentioning

confidence: 99%

“…On the contrary, presynaptic 5-HT 1A R activation reduces 5-HT release and exerts pro-cognitive effects. 5-HT 1A R antagonism facilitates memory retention, probably by the activation of 5-HT 7 Rs, and evidence is provided that 5-HT 7 Rs can facilitate emotional memory upon reduced 5-HT 1A R 4WD to Travel Inside the 5-HT 1A Receptor World http://dx.doi.org/10.5772/intechopen.69348…”

Section: Memorymentioning

confidence: 99%

“…This template has been duplicated to successfully obtain selective homo-and heterobivalent ligands [18]. Indeed, compound 15 shows high affinity for 5-HT 1A Rs and selectivity over 5-HT 7 Rs, whereas compound 16 selectively targets 5-HT 7 Rs (pK i = 7.4) (Figure 12). …”

Section: Modification Of the Piperazine Ringmentioning

confidence: 99%

“…1,2,4-Triazine-6(1H)-one derivatives also display dual affinity for 5-HT 1A Rs and 5-HT 7 Rs. SAR studies have revealed that receptor affinity and selectivity depend on the nature of the substituent in position 3 of the triazinone fragment as well as on the substitution pattern of the phenylpiperazine moiety [35].…”

Section: Modification Of the Terminal Fragmentmentioning

confidence: 99%

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4WD to Travel Inside the 5-HT1A Receptor World

Quaglia¹,

Cifani²,

Bello³

et al. 2017

Serotonin - A Chemical Messenger Between All Types of Living Cells

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5-HT 1A receptor is one of the most important members of the numerous families of serotoninergic receptors. Though it was the first 5-HT receptor to be identified and cloned, the knowledge of its activation/transduction mechanisms, mediated effects, and connection with other systems is still uncompleted. For this reason, relevant is the study of the four Ws of the title: first of all "who" this receptor is, then "why" it continues to be a so attractive target after several years after its identification, then "where" is 5-HT 1A receptor expressed within the body, and, finally, "what" effects this receptor can elicit under physiological and pathological conditions. Obviously, more and more potent, safe, and selective "drugs" might be discovered once the responses to these questions are given.

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Section: Modification Of the Spacermentioning

confidence: 95%

Section: Signal Transduction Pathways Of 5-ht 1a Rsmentioning

confidence: 99%

Section: Memorymentioning

confidence: 99%

Section: Modification Of the Piperazine Ringmentioning

confidence: 99%

Section: Modification Of the Terminal Fragmentmentioning

confidence: 99%

See 3 more Smart Citations

4WD to Travel Inside the 5-HT1A Receptor World

Quaglia¹,

Cifani²,

Bello³

et al. 2017

Serotonin - A Chemical Messenger Between All Types of Living Cells

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Uncarialins J—M from Uncaria rhynchophylla and Their Anti‐depression Mechanism in Unpredictable Chronic Mild Stress‐Induced Mice via Activating 5‐HT_1A Receptor

Bai

Zhou

et al. 2021

Chin. J. Chem.

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Monoterpene indole alkaloids | Hirsuteine | Depression | 5-HT 1A receptor | Site-directed amino acid mutation Uncaria rhynchophylla has been widely used to treat central nervous system diseases for a long history. After investigation of U. rhynchophylla, eleven monoterpene indole alkaloids, including four new compounds uncarialins J-M (1-4) and seven known analogues (5-11), were isolated and identified. Their structural characterization was conducted using HRESIMS, 1D and 2D NMR, electronic circular dichroism (ECD) spectra, and quantum chemical computations. Compounds 1, 2, 7, and 9-11 displayed significant agonistic effects towards 5-HT 1A receptor, and their EC 50 values were 7.86, 7.32, 2.24, 1.18, 1.52, and 3.75 μmol/L, respectively. Furthermore, in vivo experimental results fully revealed that hirsuteine (7) displayed a significant antidepression effect in unpredictable chronic mild stress (UCMS)-induced depression mice mainly via regulating 5-HT 1A signaling pathway. Molecular docking and site-directed amino acid mutation verified that amino acid residues Asp116 and Asn386 were the binding sites of hirsuteine (7) with 5-HT 1A receptor. In addition, pre-treatment of mice with WAY 100635 also blocked the anti-depression effect of hirsuteine ( 7), which further demonstrated that 5-HT 1A receptor was a potential target of hirsuteine (7) to effectively treat depression. These findings indicated the therapeutic material basis of U. rhynchophylla and the anti-depression underlying mechanism of hirsuteine (7), and further provided the useful guidance for the development of hirsuteine (7) as a potential antidepressant candidate.

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5‐HT1A regulates axon outgrowth in a subpopulation of Drosophila serotonergic neurons

Long,

Kinser,

Olalde‐Welling

et al. 2023

Developmental Neurobiology

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Serotonergic neurons produce extensively branched axons that fill most of the central nervous system, where they modulate a wide variety of behaviors. Many behavioral disorders have been correlated with defective serotonergic axon morphologies. Proper behavioral output therefore depends on the precise outgrowth and targeting of serotonergic axons during development. To direct outgrowth, serotonergic neurons utilize serotonin as a signaling molecule prior to it assuming its neurotransmitter role. This process, termed serotonin autoregulation, regulates axon outgrowth, branching, and varicosity development of serotonergic neurons. However, the receptor that mediates serotonin autoregulation is unknown. Here we asked if serotonin receptor 5‐HT1A plays a role in serotonergic axon outgrowth and branching. Using cultured Drosophila serotonergic neurons, we found that exogenous serotonin reduced axon length and branching only in those expressing 5‐HT1A. Pharmacological activation of 5‐HT1A led to reduced axon length and branching, whereas the disruption of 5‐HT1A rescued outgrowth in the presence of exogenous serotonin. Altogether this suggests that 5‐HT1A is a serotonin autoreceptor in a subpopulation of serotonergic neurons and initiates signaling pathways that regulate axon outgrowth and branching during Drosophila development.

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What Do We Really Know About 5-HT1A Receptor Signaling in Neuronal Cells?

Cited by 72 publications

References 64 publications

4WD to Travel Inside the 5-HT1A Receptor World

4WD to Travel Inside the 5-HT1A Receptor World

Uncarialins J—M from Uncaria rhynchophylla and Their Anti‐depression Mechanism in Unpredictable Chronic Mild Stress‐Induced Mice via Activating 5‐HT_1A Receptor

5‐HT1A regulates axon outgrowth in a subpopulation of Drosophila serotonergic neurons

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What Do We Really Know About 5-HT1A Receptor Signaling in Neuronal Cells?

Cited by 72 publications

References 64 publications

4WD to Travel Inside the 5-HT1A Receptor World

4WD to Travel Inside the 5-HT1A Receptor World

Uncarialins J—M from Uncaria rhynchophylla and Their Anti‐depression Mechanism in Unpredictable Chronic Mild Stress‐Induced Mice via Activating 5‐HT1A Receptor

5‐HT1A regulates axon outgrowth in a subpopulation of Drosophila serotonergic neurons

Contact Info

Product

Resources

About

Uncarialins J—M from Uncaria rhynchophylla and Their Anti‐depression Mechanism in Unpredictable Chronic Mild Stress‐Induced Mice via Activating 5‐HT_1A Receptor