The vanilloid receptor TRPV1: role in cardiovascular and gastrointestinal protection

Jun Peng1, Yuan-Jian Li

  • 1Department of Pharmacology, School of Pharmaceutical Sciences, Central South University, Changsha 410078, China.

Insights

The transient receptor potential channel vanilloid type 1 (TRPV1) plays a key role in pain and cardiovascular/gastrointestinal functions. TRPV1 activation offers therapeutic potential for various diseases, but potential side effects require careful consideration.

Area of Science:

  • Pharmacology
  • Physiology
  • Neuroscience

Background:

  • Transient receptor potential channel vanilloid type 1 (TRPV1) senses diverse stimuli and has roles in physiological and pathophysiological processes.
  • TRPV1 is crucial in pain signaling and influences cardiovascular and gastrointestinal functions.
  • TRPV1 can be activated by endogenous ligands (e.g., anandamide) and exogenous agonists (e.g., capsaicin).

Purpose of the Study:

  • To explore the multifaceted roles of TRPV1 beyond pain signaling.
  • To investigate TRPV1's involvement in cardiovascular and gastrointestinal physiology and pathophysiology.
  • To assess TRPV1 as a therapeutic target for cardiovascular and gastrointestinal diseases.

Main Methods:

  • Review of existing literature on TRPV1 activation and its downstream effects.
  • Analysis of studies investigating TRPV1's role in cardiovascular and gastrointestinal systems.
  • Examination of neurotransmitter release (e.g., CGRP, substance P) following TRPV1 activation.

Main Results:

  • TRPV1 activation by endogenous or exogenous compounds can lead to hypotensive effects.
  • TRPV1 activation demonstrates protective effects against cardiac and gastrointestinal injury.
  • Stimulation of neurotransmitter synthesis and release (CGRP, substance P) is a key mechanism.

Conclusions:

  • TRPV1 is a significant target for pain management and drug development for cardiovascular and gastrointestinal diseases.
  • TRPV1 activation may offer therapeutic benefits for conditions like hypertension and organ injury.
  • Potential side effects, including gastrointestinal inflammation, must be addressed in novel TRPV1 agonist development.

Related Concept Videos

Thermosensation01:43

Thermosensation

Peripheral thermosensation is the perception of external temperature. A change in temperature (on the surface of the skin and other tissues) is detected by a family of temperature-sensitive ion channels called Transient Receptor Potential, or TRP, receptors. These receptors are located on free nerve endings. Those detecting cold temperatures are closer to the surface of the skin than the nerve endings detecting warmth. These thermoTRP channels, while temperature selective, have relatively...
Mechanically-gated Ion Channels01:12

Mechanically-gated Ion Channels

Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
Enteric Nervous System: Regulation of GI Motor Activity01:11

Enteric Nervous System: Regulation of GI Motor Activity

The Enteric Nervous System (ENS) plays a pivotal role in regulating gastrointestinal or GI motor activity. This complex network of nerves, deeply embedded within the gut wall, responds to changes in the gut environment and receives input from both the autonomic nervous system and the central nervous system. By doing so, the ENS operates various programs tailored to the body's nutritional status and needs.
During periods of fasting, the ENS initiates the migrating myoelectric complex, a program...
Drugs for Peptic Ulcer Disease: Prostaglandin Analogs as Mucosal Protective Agents01:20

Drugs for Peptic Ulcer Disease: Prostaglandin Analogs as Mucosal Protective Agents

The gastric mucosa produces prostaglandins E2 (PGE2) and prostacyclin (PGI2), crucial in maintaining gastric health. They exert cytoprotective effects, including increasing bicarbonate secretion, releasing protective mucin, reducing gastric acid output, and preventing harmful vasoconstriction. These effects are mediated through various receptors, such as EP1, EP2, EP3, and EP4.
Non-steroidal anti-inflammatory drugs (NSAIDs) can induce peptic ulcers by inhibiting cyclooxygenase, decreasing...
Physiology of Enteric Nervous System and Gut Health01:05

Physiology of Enteric Nervous System and Gut Health

The gastrointestinal tract, responsible for the digestion and absorption of nutrients, is safeguarded by the intestinal barrier, which consists of secretory, physical, and immune components. At the forefront is the secretory barrier, composed of essential elements such as mucus, gut microbiota, and defense proteins. They collaborate to break down food particles, facilitate nutrient absorption, and maintain optimal gut health. These secretory components ensure the smooth functioning of the...