Synthesis and Development of Indole Based 5-HT3 Receptor Antagonists as Anti-Emetic Drugs in Oncology: An Update

2021 ◽  
Vol 28 ◽  
Author(s):  
Johana L. Rivera-Fonseca ◽  
Nelly González-Rivas ◽  
M. V. Basavanag Unnamatla ◽  
Marco A. García-Eleno ◽  
Horacio Reyes ◽  
...  
Keyword(s):  
Cancer Treatment ◽  
Receptor Antagonist ◽  
Serotonin Receptor ◽  
Biological Activities ◽  
Nausea And Vomiting ◽  
Secondary Effects ◽  
Antagonist Activity ◽  
Important Group ◽  
Type 3 ◽  
Serotonin Receptor Antagonist

: An important group of anti-emetic drugs used in the treatment of nausea and vomiting after chemotherapy contains an indole moiety in their structures, working as 5-hydroxytryptamine type 3 serotonin receptor antagonist (5-HT3). This revision is focused on compounds bearing an indole core that present a 5-HT3 receptor antagonist activity that has been successfully used as anti-emetic drugs, reducing chemotherapy adverse secondary effects during cancer treatment. Their synthesis, biological activities, and some outstanding characteristics are discussed, affording a general outlook towards the development of more efficient anti-emetic drugs.

scholarly journals Multi-Tissue Transcriptomic-Informed In Silico Investigation of Drugs for the Treatment of Dengue Fever Disease

Viruses ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1540
Author(s):  
Beatriz Sierra ◽  
Ana Cristina Magalhães ◽  
Daniel Soares ◽  
Bruno Cavadas ◽  
Ana B. Perez ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Dengue Fever ◽  
In Silico ◽  
Serotonin Receptor ◽  
Neglected Tropical Diseases ◽  
Dengue Infection ◽  
Severe Dengue ◽  
Functional Evaluation ◽  
Atpase Inhibitor ◽  
Serotonin Receptor Antagonist

Transcriptomics, proteomics and pathogen-host interactomics data are being explored for the in silico–informed selection of drugs, prior to their functional evaluation. The effectiveness of this kind of strategy has been put to the test in the current COVID-19 pandemic, and it has been paying off, leading to a few drugs being rapidly repurposed as treatment against SARS-CoV-2 infection. Several neglected tropical diseases, for which treatment remains unavailable, would benefit from informed in silico investigations of drugs, as performed in this work for Dengue fever disease. We analyzed transcriptomic data in the key tissues of liver, spleen and blood profiles and verified that despite transcriptomic differences due to tissue specialization, the common mechanisms of action, “Adrenergic receptor antagonist”, “ATPase inhibitor”, “NF-kB pathway inhibitor” and “Serotonin receptor antagonist”, were identified as druggable (e.g., oxprenolol, digoxin, auranofin and palonosetron, respectively) to oppose the effects of severe Dengue infection in these tissues. These are good candidates for future functional evaluation and clinical trials.

SEROTONIN RECEPTOR ANTAGONIST INDUCES INDEFINITE SURVIVAL OF FULLY-ALLOGENEIC CARDIAC GRAFTS.

2004 ◽  
Vol 78 ◽  
pp. 599-600
Author(s):  
T Akiyoshi ◽  
Q Zhang ◽  
F Inoue ◽  
K Tanaka ◽  
O Aramaki ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Serotonin Receptor ◽  
Serotonin Receptor Antagonist

Effectiveness of Serotonin-Receptor Antagonist Antiemetic Therapy over Successive Courses of Carboplatin-Based Chemotherapy

2002 ◽  
Vol 85 (3) ◽  
pp. 435-437 ◽  
Author(s):  
Margaret R. Markman ◽  
Gertrude Peterson ◽  
Barbara Kulp ◽  
Maurie Markman
Keyword(s):  
Receptor Antagonist ◽  
Serotonin Receptor ◽  
Antiemetic Therapy ◽  
Serotonin Receptor Antagonist

Granisetron: The Second Serotonin-Receptor Antagonist

1995 ◽  
Vol 29 (12) ◽  
pp. 1240-1251 ◽  
Author(s):  
Val R Adams ◽  
Amy W Valley
Keyword(s):  
Clinical Trials ◽  
Adverse Effects ◽  
Receptor Antagonist ◽  
Serotonin Receptor ◽  
English Language ◽  
Data Extraction ◽  
Optimal Dose ◽  
Nausea And Vomiting ◽  
Cost Comparison ◽  
Antiemetic Agents

Objective: To review the pharmacology, pharmacokinetics, clinical efficacy, and adverse effects of granisetron, focusing on critical analysis of published clinical trials and comparison with other antiemetic agents, including ondansetron. Data Sources: MEDLINE (1966–1995) and CANCERLIT (1991–1995) searches of English-language literature using the terms “granisetron” and “granisetron (m)” were performed. Study Selection And Data Extraction: All articles were considered for possible inclusion in this review. Abstracts of clinical trials were included only when they were judged to add critical information not otherwise available in the medical literature. For studies published more than once, the most recent publication was cited. Data Synthesis: Nausea and vomiting are rated by patients as the most distressing chemotherapy-related adverse effects and may produce potentially life-threatening complications. The discovery of the role of serotonin in nausea and vomiting and the development of selective serotonin3-receptor (5-HT3) antagonists has significantly diminished the incidence and consequences of chemotherapy-related nausea and vomiting. Granisetron is the second 5-HT3-receptor antagonist to be marketed in the US. Granisetron has been compared with other antiemetic agents, including ondansetron, against highly and moderately emetogenic chemotherapy. The results of these trials have shown granisetron to be superior to conventional antiemetics and as effective as ondansetron in the prevention of chemotherapy-induced nausea and vomiting. The optimal dose of granisetron has yet to be determined. Formulary decisions should be based on a cost comparison among the 5-HT3-receptor antagonists at individual institutions. Conclusions: Granisetron is a safe, effective antiemetic agent for the management of nausea and vomiting caused by cancer chemotherapy.

Sign in / Sign up

Export Citation Format

Share Document