Aims: Serotonin (5-hydroxytryptamine 3; 5-HT(3)) receptors are involved in chemotherapy-induced nausea and vomiting (CINV), and 5-HT(3) antagonists are part of the 'gold standard' antiemetic treatment during chemotherapy. We investigated the correlation of common variants in 5-HT(3) receptor subunit genes with the occurrence of CINV.
Materials & Methods: A total of 110 previously characterized chemotherapy-naive women with primary breast cancer treated with anthracycline-containing chemotherapy served as a study group for mutational analysis by direct sequencing. Eight common SNPs in the 5-HT(3) receptor genes, HTR3A, HTR3B, HTR3D and HTR3E, were selected for association analysis.
Results: A nonsynonymous variant in HTR3D, p.G36A (rs6443930), was found to be over-represented in nonresponders, assuming a log-additive inheritance model (p = 0.048). Cox proportional regression analysis resulted in a hazards ratio of 0.36 for homozygous carriers of the C allele to vomit within 24 h after first chemotherapy administration (p = 0.049).
Conclusion: Our data supports the hypothesis that 5-HT(3) receptors play an important role in the pathogenesis of CINV. Along with previously identified HTR3 polymorphisms, the HTR3D p.G36A variant could also contribute to facilitating individual risk predictions.
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http://dx.doi.org/10.2217/pgs.10.67 | DOI Listing |
Tissue Cell
January 2025
Pharmacology and Toxicology Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt.
Doxorubicin (DOX) is an anthracycline chemotherapy employed in treating malignancies. Unfortunately, the clinical application of DOX is limited due to its nephrotoxicity. Granisetron (GRAN) is a 5-HT3 receptor blocker used widely to manage post-chemotherapy nausea and vomiting with anti-inflammatory, anti-oxidant, and anti-apoptotic bioactivities.
View Article and Find Full Text PDFJ Microbiol Biotechnol
November 2024
Department of Biotechnology and Department of Integrative Food, Bioscience and Biotechnology (BK21 FOUR), Chonnam National University, Gwangju 61186, Republic of Korea.
This study investigates the modulatory effects of nicergoline, a major bioactive compound derived from ergot fungus, on the 5-hydroxytryptamine 3A (5-HT3A) receptor. Utilizing a two-electrode voltage-clamp technique, we evaluated the impact of nicergoline on the 5-HT-induced inward current (I) in 5-HT3A receptors. Our findings reveal that nicergoline inhibits I in a reversible and concentration-dependent manner.
View Article and Find Full Text PDFJ Pain Palliat Care Pharmacother
January 2025
Department of Palliative Medicine, S.M.S. Medical College, Jaipur, Rajasthan, India.
Mirtazapine is a selective serotonergic antidepressant that functions by blocking adrenergic alpha2-autoreceptors and heteroreceptors and inhibiting 5-HT2 and 5-HT3 receptors. It is a noradrenergic drug. Mirtazapine has anxiolytic or sleep-quality-improving effects, aggravates appetite-stimulation, and has stomach emptying functions.
View Article and Find Full Text PDFArch Razi Inst
June 2024
Medical Plants Research Center, Basic Health Sciences Institute, Shahrekord University of Medical Sciences, Shahrekord, Iran.
In the present study, the mechanisms involved in scopolamine-induced memory impairment have been investigated. The molecular events that take place during memory mostly include mechanisms that are seen in the acquisition phase. Results showed that one of the mechanisms of memory destruction caused by scopolamine, in addition to weakening the cholinergic system, is the indirect effect of scopolamine on other neurotransmitter systems, including the glutamatergic system.
View Article and Find Full Text PDFNeurosci Lett
January 2025
Neurobiology Unit, Institute for Biotechnology and Biomedicine (BIOTECMED), University of Valencia, Spain. Electronic address:
Neuronal structural plasticity gives the adult brain the capacity to adapt to internal or external factors by structural and molecular changes. These plastic processes seem to be mediated, among others, by the action of the neurotransmitter serotonin through specific receptors (5-HTRs). Previous studies have shown that the maturation of granule cells in the hippocampus is mediated by 5-HT3.
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