GR-125487

GR-125487

GR-125487 is a selective antagonist of the 5-HT4 receptor, a subtype of the serotonin receptor. It is primarily used in scientific research to study the physiological and pharmacological roles of the 5-HT4 receptor in various biological systems.

Chemical Structure and Properties

GR-125487 is a chemical compound with the molecular formula C19H23N3O2. It is characterized by its high affinity and selectivity for the 5-HT4 receptor, making it a valuable tool in receptor binding studies.

Pharmacology

GR-125487 acts as a competitive antagonist at the 5-HT4 receptor. By binding to this receptor, it inhibits the action of serotonin, a neurotransmitter that plays a crucial role in modulating gastrointestinal motility, cardiac function, and central nervous system processes.

Mechanism of Action

The 5-HT4 receptor is a G protein-coupled receptor (GPCR) that, when activated by serotonin, stimulates adenylate cyclase activity, leading to an increase in cyclic AMP (cAMP) levels. GR-125487 blocks this pathway by preventing serotonin from binding to the receptor, thereby reducing cAMP production and downstream signaling effects.

Therapeutic Implications

While GR-125487 itself is not used therapeutically, its role in research has provided insights into potential treatments for conditions such as irritable bowel syndrome (IBS), gastroesophageal reflux disease (GERD), and certain cardiac arrhythmias. By understanding how 5-HT4 receptor antagonists can modulate these conditions, new therapeutic agents can be developed.

Research Applications

GR-125487 is widely used in preclinical studies to:

• Investigate the role of 5-HT4 receptors in gastrointestinal motility and secretion.
• Explore the effects of 5-HT4 receptor modulation on cardiac function, particularly in the context of arrhythmias.
• Study the involvement of 5-HT4 receptors in cognitive processes and potential implications for neurodegenerative diseases.

Safety and Handling

As with many research chemicals, GR-125487 should be handled with care. Appropriate safety measures, including the use of personal protective equipment (PPE) and adherence to laboratory safety protocols, are recommended when working with this compound.

Also see

• 5-HT4 receptor
• Serotonin
• G protein-coupled receptor
• Irritable bowel syndrome
• Cardiac arrhythmia