SB-203186

Overview

SB-203186 is a selective antagonist of the 5-HT₄ receptor, a subtype of the serotonin receptor. It is primarily used in research to study the physiological and pathological roles of the 5-HT₄ receptor in various systems of the body, including the gastrointestinal tract and the central nervous system.

Chemical Properties

SB-203186 is a chemical compound with the molecular formula C₁₉H₂₃ClN₂O₂. It is characterized by its ability to bind selectively to the 5-HT₄ receptor, thereby inhibiting the action of serotonin at this receptor site.

Mechanism of Action

The 5-HT₄ receptor is a G protein-coupled receptor that, when activated by serotonin, can influence various physiological processes. SB-203186 acts as an antagonist, meaning it binds to the receptor without activating it, thereby blocking serotonin from exerting its effects. This makes SB-203186 a valuable tool in research for understanding the role of 5-HT₄ receptors in health and disease.

Research Applications

SB-203186 is used extensively in preclinical studies to explore the role of 5-HT₄ receptors in:

• Gastrointestinal Motility: The 5-HT₄ receptor is known to play a role in the regulation of gastrointestinal motility. SB-203186 helps in studying conditions like irritable bowel syndrome (IBS) and other motility disorders.

• Cognitive Function: Research has suggested that 5-HT₄ receptors may be involved in cognitive processes. SB-203186 is used to investigate potential therapeutic targets for cognitive impairments and neurodegenerative diseases.

• Cardiovascular System: The role of 5-HT₄ receptors in the cardiovascular system is also a subject of study, with SB-203186 being used to understand its effects on heart rate and contractility.

Pharmacokinetics

The pharmacokinetic profile of SB-203186 includes its absorption, distribution, metabolism, and excretion. Detailed studies are conducted to understand its half-life, bioavailability, and the pathways through which it is metabolized.

Safety and Toxicology

As with any pharmacological agent, understanding the safety and potential toxicological effects of SB-203186 is crucial. Studies focus on its effects at various dosages, potential side effects, and any long-term impacts on health.

Also see

• 5-HT4 receptor
• Serotonin
• G protein-coupled receptor
• Irritable bowel syndrome
• Cognitive function

External Links

• [PubChem entry for SB-203186](https://pubchem.ncbi.nlm.nih.gov/compound/SB-203186)
• [Research articles on SB-203186](https://www.ncbi.nlm.nih.gov/pubmed/?term=SB-203186)