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Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates...
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Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
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Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
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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...
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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...
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Immunotherapy is a treatment that boosts or manipulates the immune system to fight diseases, including cancer. For instance, by stimulating an immune response through vaccinations against viruses that cause cancers, like hepatitis B virus and human papillomavirus, these diseases can be prevented. Nonetheless, some cancer cells can avoid the immune system due to their rapid mutation and division. The immune response to many cancers involves three phases: elimination, equilibrium, and escape.
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Related Experiment Video

Updated: Jun 26, 2025

Establishing a Mouse Model of a Pure Small Fiber Neuropathy with the Ultrapotent Agonist of Transient Receptor Potential Vanilloid Type 1
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Targeting TRPV4 Channels for Cancer Pain Relief.

Caren Tatiane de David Antoniazzi1, Náthaly Andrighetto Ruviaro2, Diulle Spat Peres1

  • 1Graduate Program in Pharmacology, Federal University of Santa Maria (UFSM), Santa Maria 97105-900, Brazil.

Cancers
|May 11, 2024
PubMed
Summary
This summary is machine-generated.

Transient Receptor Potential Vanilloid 4 (TRPV4) channels play a role in cancer pain. Targeting TRPV4 may offer new strategies for managing cancer-induced pain with fewer side effects.

Keywords:
CIBPCIPNTRP channelsnociceptionosmotransducertumor microenvironment

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Area of Science:

  • Neuroscience
  • Oncology
  • Pain Research

Background:

  • Cancer pain is complex and often inadequately managed.
  • Ion channels, including Transient Receptor Potential Vanilloid 4 (TRPV4), are implicated in pain signaling.
  • TRPV4 channels are expressed in sensory neurons and activated by various stimuli.

Purpose of the Study:

  • To summarize the role of TRPV4 in cancer etiology.
  • To elucidate the mechanisms of TRPV4 in cancer-induced pain.
  • To explore TRPV4 as a potential therapeutic target for cancer pain.

Main Methods:

  • Literature review focusing on TRPV4 expression and function in cancer pain models.
  • Analysis of studies investigating TRPV4 antagonists and knockdown effects on nociception.
  • Examination of TRPV4 involvement in chemotherapy-induced peripheral neuropathy (CIPN) and cancer-induced bone pain (CIBP).

Main Results:

  • TRPV4 antagonists and knockdown reduce nociception in CIPN models.
  • TRPV4 receptor expression is enhanced in CIBP, perineural, and orofacial cancer pain models.
  • Evidence suggests TRPV4 channels contribute to cancer pain mechanisms.

Conclusions:

  • TRPV4 channels are implicated in various cancer pain conditions.
  • Targeting TRPV4 modulation presents a promising avenue for novel cancer pain treatments.
  • Developing TRPV4-targeting agents could lead to improved analgesia with reduced adverse effects.