1-Phenylbiguanide, 5-HT3 receptor agonist

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

The 5-HT3 receptor a serotonin receptor subtype mechanically functions as a ligand-gated ion channel. Alternate names for this receptor include 5HT3A 5HT3B HTR3C and 5HT3E. The receptor mainly consists of a pentameric structure made up of these five subunits which together allow the flow of cations across the cell membrane. The exact mass of the individual receptor subunits can vary but they roughly range between 50 and 60 kDa. The 5-HT3 receptors primarily express in the gastrointestinal tract and the central nervous system where they mediate fast excitatory synaptic transmission.

Biological function summary

The 5-HT3 receptor plays a critical role in neurotransmission and is part of a complex involved in mediating various physiological processes. It functions by binding to serotonin causing the receptor to open and allowing cation influx which depolarizes the neuron's membrane. Moreover the receptor is involved in processes like vomiting and anxiety regulation. As a member of a larger family of neurotransmitter receptors it influences how neurons communicate and ultimately impacts functions like mood and gut motility.

Pathways

5-HT3 receptors integrate into the serotonin signaling pathway which is essential in regulating mood cognition and perception. They also play a role in the emetic response pathway involving other proteins like the cytochrome P450 enzymes such as cytochrome P450 2C8 2C9 2C12 and 2C19 which are involved in drug metabolism and detoxification processes. The interaction between these pathways highlights the receptor's importance in maintaining neurotransmitter balance and drug interactions inside the body.

Associated diseases and disorders

The 5-HT3 receptor has implications for conditions like irritable bowel syndrome (IBS) and chemotherapy-induced nausea and vomiting (CINV). Dysregulation of this receptor can lead to altered neurotransmission affecting both gastrointestinal and neurological health. In IBS abnormal receptor activity can cause disrupted gut motility while connection with cytochrome P450 enzymes influences susceptibility to CINV. The receptor's modulation provides therapeutic targets where 5-HT3 receptor antagonists and agonists like phenylbiguanide and other compounds serve as treatment options to alleviate symptoms associated with these disorders.