Expression of 5‐HT<sub>3A</sub>receptors in cells of the immune system

Fiebich, Bernd L.; Akundi, Ravi Shankar; Seidel, Matthias; Geyer, Verena; Haus, Utz-Uwe; Müller, Werner A.; Stratz, T; Candelario‐Jalil, Eduardo

doi:10.1080/03009740410006952

Cited by 83 publications

(66 citation statements)

References 6 publications

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“…Five 5-HT 3 receptor subunits (A-E) have been identified to date, and whereas the A subunit can form functional homomeric receptors, subunits B to E function only as heteromeric receptors in combination with the A subunit (Davies et al, 1999;Niesler et al, 2003). In the human nervous system, 5-HT 3 A subunits have been found throughout the adult brain, but are also widely distributed in extraneuronal cells (Miyake et al, 1995;Fiebich et al, 2004). 5-HT 3 B receptor subunits are not as widespread, but are still detectable in a range of tissues (Davies et al, 1999;Dubin et al, 1999;Niesler et al, 2003;Tzvetkov et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

Varenicline Is a Potent Agonist of the Human 5-Hydroxytryptamine₃ Receptor

Lummis¹,

Thompson²,

Bencherif³

et al. 2011

J Pharmacol Exp Ther

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Varenicline, a widely used and successful smoking cessation agent, acts as a partial agonist at nicotinic acetylcholine receptors. Here, we explore the effects of varenicline at human and mouse 5-Hydroxytryptamine 3 (5-HT 3 ) receptors. Application of varenicline to human 5-HT 3 receptors expressed in Xenopus laevis oocytes reveal it is almost a full agonist (R max ϭ 80%) with an EC 50 (5.9 M) 3-fold higher than 5-HT. At mouse 5-HT 3 receptors varenicline is a partial agonist (R max ϭ 35%) with an EC 50 (18 M) 20-fold higher than 5-HT. Displacement of the competitive 5-HT 3 receptor antagonist [ 3 H]granisetron reveals similar IC 50 values for varenicline at mouse and human receptors expressed in human embryonic kidney 293 cells, although studies in these cells using a membrane potential-sensitive dye show that again varenicline is a 4-or 35-fold less potent agonist than 5-HT in human and mouse receptors, respectively. Thus the data suggest that the efficacy, but not the affinity, of varenicline is greater at human 5-HT 3 receptors compared with mouse. Docking studies provide a possible explanation for this difference, because they suggest distinct orientations of the ligand in the mouse versus human 5-HT 3 agonist binding sites. Additional binding selectivity studies in a broad panel of recombinant receptors and enzymes confirmed an interaction with 5-HT 3 receptors but revealed no additional interactions of varenicline. Therefore, activation of human 5-HT 3 receptors may be responsible for some of the side effects that preclude use of higher doses during varenicline treatment.

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Section: Introductionmentioning

confidence: 99%

Varenicline Is a Potent Agonist of the Human 5-Hydroxytryptamine₃ Receptor

Lummis¹,

Thompson²,

Bencherif³

et al. 2011

J Pharmacol Exp Ther

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“…5HT 3 receptors have been detected on mononuclear cells, lymphocytes and are present on peripheral and central neurons [12][13][14]. Evidence for analgesic and anti-inflammatory activity of 5-HT 3 receptor antagonists has been found in clinical studies in recent years [15][16][17].…”

Section: Introductionmentioning

confidence: 99%

The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation

Maleki‐Dizaji

Eteraf-Oskouei

Fakhrjou

et al. 2010

International Immunopharmacology

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“…HTR3 is the target of a widely used anti-emetic class of compounds [26] . In hematopoietic cells, monocytes and T cells are known to express HTR3A [28] . 5-HT affects the function of B and T cells [29][30][31][32][33] .…”

Section: Discussionmentioning

confidence: 99%

Serotonin Receptor 3A Expression in Normal and Neoplastic B Cells

et al. 2010

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Chromosome 11q21–qter is a very gene-rich region and is often targeted by genomic aberrations in a variety of human cancers, including B cell lymphoid neoplasms. In order to identify genes which could be deregulated in diffuse large B cell lymphomas (DLBCL), we analyzed the expression levels of genes mapped on chromosome 11q21–qter across a series of publicly available DLBCL expression data sets. We identified HTR3A, the gene coding for 5-hydroxytryptamine receptor 3A, as the most frequently differentially expressed. Since HTR3A expression had not been previously characterized in normal and neoplastic B cells, we evaluated its expression by real-time PCR and by immunohistochemistry. The gene is expressed by B cells and it seems to be regulated during the mature B cell differentiation, being overexpressed during the germinal center phase. Lymphomas derived from germinal center B cells maintain the expression, with the level of expression varying among different patients.

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Expression of 5‐HT_3Areceptors in cells of the immune system

Cited by 83 publications

References 6 publications

Varenicline Is a Potent Agonist of the Human 5-Hydroxytryptamine₃ Receptor

Varenicline Is a Potent Agonist of the Human 5-Hydroxytryptamine₃ Receptor

The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation

Serotonin Receptor 3A Expression in Normal and Neoplastic B Cells

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Expression of 5‐HT3Areceptors in cells of the immune system

Cited by 83 publications

References 6 publications

Varenicline Is a Potent Agonist of the Human 5-Hydroxytryptamine3 Receptor

Varenicline Is a Potent Agonist of the Human 5-Hydroxytryptamine3 Receptor

The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation

Serotonin Receptor 3A Expression in Normal and Neoplastic B Cells

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Product

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Expression of 5‐HT_3Areceptors in cells of the immune system

Varenicline Is a Potent Agonist of the Human 5-Hydroxytryptamine₃ Receptor

Varenicline Is a Potent Agonist of the Human 5-Hydroxytryptamine₃ Receptor