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Related Concept Videos

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists

5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists01:23

Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists

Serotonin, a crucial neurotransmitter synthesized by enterochromaffin cells, plays a cardinal role in regulating gastrointestinal (GI) motility. With over 90% of the body's total serotonin in the GI tract, its influence on digestive processes is profound. Serotonin is swiftly released upon various stimuli, such as food boluses or certain drugs, triggering intrinsic sensory neurons in the myenteric plexus and extrinsic vagal and spinal sensory neurons. This leads to the activation of the...
Antidepressant Drugs: MAOIs and Other Agents01:23

Antidepressant Drugs: MAOIs and Other Agents

Atypical antidepressants, including bupropion (Wellbutrin), mirtazapine (Remeron), nefazodone (Serzone), trazodone (Desyrel), and vilazodone (Viibryd), offer unique mechanisms of action. Bupropion weakly inhibits dopamine and norepinephrine reuptake, aiding depression treatment and smoking cessation, with a low risk of sexual dysfunction. Mirtazapine enhances serotonin and norepinephrine neurotransmission, leading to sedation, increased appetite, and weight gain. As a result, it helps treat...
Drugs Affecting GI Tract Motility: Dopamine Receptor Antagonists01:28

Drugs Affecting GI Tract Motility: Dopamine Receptor Antagonists

Prokinetic agents are specialized medications that stimulate gastrointestinal (GI) motility, promoting food movement through the GI tract. Dopamine, an inhibitory neurotransmitter, plays a significant role in this process, reducing GI motility and indirectly controlling the speed of digestion. Dopamine receptor antagonists, such as metoclopramide and domperidone, offer a unique advantage as prokinetic agents. By blocking the dopamine receptors, these drugs increase GI motility, improving food...
Antipsychotic Drugs: Typical and Atypical Agents01:21

Antipsychotic Drugs: Typical and Atypical Agents

Antipsychotic drugs are classified into first-generation (typical) drugs including phenothiazines; and second-generation (atypical) drugs. Chlorpromazine hydrochloride (Thorazine), a phenothiazine derivative, broadly impacts the central, autonomic, and endocrine systems. This drug, along with typical agents like haloperidol (Haldol), primarily works by antagonizing D2 receptors, thus reducing dopaminergic neurotransmission. However, typical antipsychotics can cause side effects such as sedation...
Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists01:29

Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists

Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
Phenothiazines, such as prochlorperazine...

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Related Experiment Video

Updated: Jun 8, 2026

The Use of Pharmacological-challenge fMRI in Pre-clinical Research: Application to the 5-HT System
11:27

The Use of Pharmacological-challenge fMRI in Pre-clinical Research: Application to the 5-HT System

Published on: April 25, 2012

5-HT₃ antagonists under development.

Youhoon Chong1, Hyunah Choo

  • 1Konkuk University, Bio/Molecular Informatics Center, Department of Bioscience and Biotechnology, 1 Hwayang-dong, Gwangjin-gu, Seoul 143-701, Republic of Korea.

Expert Opinion on Investigational Drugs
|October 19, 2010
PubMed
Summary

Novel 5-HT(3) receptor antagonists are needed due to upcoming patent expiries. Future research should focus on structurally diverse compounds to improve efficacy for conditions like CINV and IBS.

Area of Science:

  • Pharmacology and Medicinal Chemistry
  • Gastroenterology
  • Oncology

Background:

  • 5-HT(3) receptor antagonists are crucial for managing chemotherapy-induced nausea and vomiting (CINV) and irritable bowel syndrome (IBS).
  • These antagonists also show potential in treating central nervous system disorders, including anxiety and sleep disturbances.
  • Current applications leverage their ability to reduce gut transit, enhance fluid absorption, and alleviate pain.

Purpose of the Study:

  • To review the structures, in vitro activities, and in vivo effects of 5-HT(3) receptor antagonists in development.
  • To analyze clinical trial data for future research directions in 5-HT(3) antagonist development.
  • To highlight the need for novel, structurally diverse compounds.

Main Methods:

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The Use of Pharmacological-challenge fMRI in Pre-clinical Research: Application to the 5-HT System
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  • Review of existing literature on 5-HT(3) receptor antagonist structures and activities.
  • Analysis of in vitro and in vivo experimental data.
  • Evaluation of clinical trial outcomes for pipeline molecules.

    • Main Results:

    • Identification of future research directions based on clinical trial data of pipeline 5-HT(3) receptor antagonists.
    • Highlighting the imminent patent expiry of many current drug candidates.
    • Emphasizing the limited structural diversity among existing 5-HT(3) antagonists.

    Conclusions:

    • The development of novel 5-HT(3) receptor antagonists with improved efficacy is essential for future therapeutic success.
    • Structurally diverse compound libraries must be explored to identify new antagonists beyond existing benzamide, tricyclic, and bicyclic families.
    • Acquiring intellectual property for novel antagonists will be key to a bright future in this therapeutic area.