Last update 01 Nov 2024

5-HT3A receptor

Last update 01 Nov 2024

Basic Info

Synonyms

5-HT-3, 5-HT3-A, 5-HT3A

+ [10]

Introduction

This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.

Drugs associated with 5-HT3A receptor

HR-20013

Target

5-HT3A receptor x NK1R

Mechanism

5-HT3A receptor antagonists [+1]

Active Org.

Fujian Suncadia Pharmaceuticals Co Ltd.

Originator Org.

Fujian Suncadia Pharmaceuticals Co Ltd.

Active Indication

Chemotherapy-induced nausea and vomiting [+4]

Inactive Indication-

Drug Highest PhaseNDA/BLA

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Tubocurarine Chloride

Target

5-HT3A receptor x CHRNA2

Mechanism

5-HT3A receptor antagonists [+1]

Active Org.-

Originator Org.

Bristol Myers Squibb Co.

Active Indication-

Inactive Indication

Muscle Hypotonia

Drug Highest PhaseWithdrawn

First Approval Ctry. / Loc.

First Approval Date28 Nov 1947

YM-26308-2

Target

5-HT3A receptor

Mechanism

5-HT3A receptor antagonists

Active Org.-

Originator Org.

Yamanouchi Pharmaceutical Co., Ltd.

Active Indication-

Inactive Indication

Vomiting

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with 5-HT3A receptor

CTR20243064 / RecruitingPhase 3

以盐酸帕洛诺司琼为对照，评价注射用HR20013用于预防中致吐风险抗肿瘤药物引起恶心呕吐的有效性和安全性研究—多中心、随机、双盲双模拟、阳性对照Ⅲ期临床研究

[Translation] A multicenter, randomized, double-blind, double-dummy, positive-controlled phase III clinical study to evaluate the efficacy and safety of HR20013 for injection in preventing nausea and vomiting caused by anticancer drugs with moderate emetogenic risk, using palonosetron hydrochloride as a control

评价注射用HR20013用于预防中致吐风险抗肿瘤药物引起恶心呕吐的有效性；评价注射用HR20013用于预防中致吐风险抗肿瘤药物引起恶心呕吐的安全性和HR20013的群体药代动力学特征

[Translation]

To evaluate the effectiveness of HR20013 for injection in preventing nausea and vomiting caused by anticancer drugs with moderate emetogenic risk; to evaluate the safety of HR20013 for injection in preventing nausea and vomiting caused by anticancer drugs with moderate emetogenic risk and the population pharmacokinetic characteristics of HR20013

Start Date03 Sep 2024

Sponsor / Collaborator

Fujian Suncadia Pharmaceuticals Co Ltd.

NCT06554184 / RecruitingPhase 3

A Randomized Phase III Study Evaluating the Efficacy and Safety of HR20013 for Nausea and Vomiting Associated With Moderate Emetic Risk Anticancer Agents

This study is aimed to evaluate the efficacy and safety of HR20013 versus palonosetron for nausea and vomiting associated with moderate emetic risk anticancer agents

Start Date03 Sep 2024

Sponsor / Collaborator

Fujian Suncadia Pharmaceuticals Co Ltd.

CTR20241327 / CompletedPhase 1

利福平和伊曲康唑对注射用HR20013在健康受试者中的药代动力学影响研究

[Translation] Effects of rifampicin and itraconazole on the pharmacokinetics of HR20013 for injection in healthy subjects

在健康受试者中评价利福平和伊曲康唑对注射用HR20013药代动力学特征的影响及联合用药的安全性

[Translation]

To evaluate the effects of rifampicin and itraconazole on the pharmacokinetic characteristics of HR20013 for injection and the safety of combined use in healthy subjects

Start Date23 May 2024

Sponsor / Collaborator

Fujian Suncadia Pharmaceuticals Co Ltd.

100 Clinical Results associated with 5-HT3A receptor

100 Translational Medicine associated with 5-HT3A receptor

0 Patents (Medical) associated with 5-HT3A receptor

1,385

Literatures (Medical) associated with 5-HT3A receptor

01 Dec 2024·Fitoterapia

Effects of morroniside isolated from Cornus officinalis fruits on functional gastrointestinal disorders and gastric ulcer in mice

Article

Author: Taniguchi, Masahiko ; Kimura, Yoshiyuki

The dried fruits of Cornus officinalis (Cornaceae) are used in Kampo medicine (e.g. Hachimigan and Goshajinkigan) to treat senile osteoporosis, diabetes, gastric atony, frequent urination, and diarrhea/constipation associated with aging. The present study investigated the effects of a C. officinalis fruit extract and morroniside, an iridoid compound from isolated these fruits, on the reduction in gastric emptying small intestinal motility caused by 5-hydroxytryptamine (5-HT) and 1-(3-chlorophenyl) biguanide (5-HT₃ receptor agonist), and gastric ulcers induced by 150 or 75 mM HCl/90 % EtOH (HCl-EtOH) and/or 5-HT in mice. C. officinalis extract (500 mg/kg) and morroniside (20 and 50 mg/kg) suppressed the reduction in gastric emptying induced by 5-HT- and 5-HT₃ agonist. C. officinalis extract, morroniside and 5-HT₃ receptor antagonist (ramosetron) attenuated 5-HT-induced diarrhea. Furthermore, morroniside (20 and 50 mg/kg) prevented EtOH/HCl-induced gastric ulcers and those caused by 5-HT. Morroniside (20 and 50 mg/kg) attenuated elevations in the plasma levels of corticosterone, corticotropin-releasing factor (CRF), and adrenocorticotropic hormone (ACTH) in 75 mM HCl/90 % EtOH- and 5-HT-treated mice. The results obtained herein suggest the potential of morroniside as an effective treatment for irritable bowel syndrome, such as diarrhea and functional dyspepsia (reductions in gastric emptying and small intestinal motility), caused by 5-HT. The present study suggests a role for morroniside in the regulation of elevations in CRF, ACTH, and corticosterone levels through hypothalamic-pituitary-adrenal axis activity induced by stress loading, such as a 5-HT treatment and/or HCl/EtOH stimulation.

01 Nov 2024·European Journal of Pharmaceutical Sciences

Genetic polymorphisms and their association with methotrexate polyglutamates during maintenance treatment in Korean children and young adults with acute lymphoblastic leukemia

Article

Author: Choi, Rihwa ; Ju, Hee Young ; Kim, Min-Ji ; Lee, Ji Won ; Lee, Soo-Youn

The aim of this study was to investigate the impact of genetic polymorphisms on methotrexate (MTX) metabolism in Korean children and young adults with acute lymphoblastic leukemia, specifically focusing on MTX polyglutamates (MTX-PGs) in erythrocytes, which have been rarely studied. Korean children and young adult patients undergoing maintenance therapy for acute lymphoblastic leukemia, who were receiving weekly oral MTX doses of 20 mg/m²/week, were prospectively included. We investigated erythrocyte MTX-PG (PG1 to PG5) levels, MTX-PG/MTX dose ratios, and 222 genetic polymorphisms spanning 78 genes and three intergenic areas related to MTX transport, folate cycle metabolism, purine/pyrimidine pathways, and non-pathway genes (including TPMT and NUDT15 genotypes) to explore their association with MTX metabolism. MTX-PG levels were associated with MTX dose (p < 0.05), and MTX-PG3 comprised the majority of the total MTX-PGs, with a median of 39.3%. Various polymorphisms within the same gene demonstrated differing associations with each type of MTX-PG, underscoring the complexity of MTX pharmacogenetics. Among the polymorphisms examined, 14 across 13 genes showed significant associations with MTX-PG2-5 levels, even after adjusting for the false discovery rate (ABCC5, ATG16L1, CEP72, FSTL5, GMPS, HTR3A, IMPDH1, NT5C2, SLC28A3, SLCO1B3, SUCLA2, TPMT, and TYMS). This study enhances our understanding of genetic polymorphisms in MTX metabolism and therapeutic monitoring for MTX maintenance, promoting personalized medicine in acute lymphoblastic leukemia patients.

19 Sep 2024·Cells

Cannabinol (CBN) Influences the Ion Channels and Synaptic-Related Genes in NSC-34 Cell Line: A Transcriptomic Study.

Article

Author: Trainito, Alessandra ; Gugliandolo, Agnese ; D'Angiolini, Simone ; Salamone, Stefano ; Muscarà, Claudia ; Chiricosta, Luigi ; Mazzon, Emanuela ; Pollastro, Federica

Neurological disorders such as Alzheimer's, Parkinson's, amyotrophic lateral sclerosis, and schizophrenia are associated with altered neuronal excitability, resulting from dysfunctions in the molecular architecture and physiological regulation of ion channels and synaptic transmission. Ion channels and synapses are regarded as suitable therapeutic targets in modern pharmacology. Cannabinoids have received great attention as an original therapeutic approach for their effects on human health due to their ability to modulate the neurotransmitter release through interaction with the endocannabinoid system. In our study, we explored the effect of cannabinol (CBN) through next-generation sequencing analysis of NSC-34 cell physiology. Our findings revealed that CBN strongly influences the ontologies related to ion channels and synapse activity at all doses tested. Specifically, the genes coding for calcium and potassium voltage-gated channel subunits, and the glutamatergic and GABAergic receptors (Cacna1b, Cacna1h, Cacng8, Kcnc3, Kcnd1, Kcnd2, Kcnj4, Grik5, Grik1, Slc17a7, Gabra5), were up-regulated. Conversely, the genes involved into serotoninergic and cholinergic pathways (Htr3a, Htr3b, Htr1b, Chrna3, Chrnb2, Chrnb4), were down-regulated. These findings highlight the influence of CBN in the expression of genes involved into ion influx and synaptic transmission.

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