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Related Concept Videos

Analgesia and Pain Management01:25

Analgesia and Pain Management

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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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...
Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
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Opioid Analgesics: Morphine and Other Natural Cogeners

Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
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Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
Pain01:20

Pain

Pain serves as a critical warning signal that alerts the body to potential or actual harm. When mechanical pressure on the skin is intense, such as from a sharp pinch, the sensation transitions from touch to pain. Similarly, extreme temperatures, like a hot pot handle, convert the sensation of heat into pain. Pain can also result from overstimulation of other senses, such as blinding light, loud noise, or the intense heat from habañero peppers. This ability to sense pain is essential for...

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Updated: Jun 24, 2026

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
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Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4

Published on: December 31, 2013

TRPV1: a target for next generation analgesics.

Louis S Premkumar1, Parul Sikand

  • 1Department of Pharmacology, Southern Illinois University School of Medicine Springfield, IL 62702, USA. lpremkumar@siumed.edu

Current Neuropharmacology
|March 24, 2009
PubMed
Summary

Transient Receptor Potential Vanilloid 1 (TRPV1) channels are key to sensing pain and temperature. Understanding TRPV1

Keywords:
TRPV1inflammatory mediatorsnociceptive ion channels.nociceptorspainprotein kinases

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Last Updated: Jun 24, 2026

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
12:09

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4

Published on: December 31, 2013

Intracerebroventricular Treatment with Resiniferatoxin and Pain Tests in Mice
06:04

Intracerebroventricular Treatment with Resiniferatoxin and Pain Tests in Mice

Published on: September 2, 2020

Area of Science:

  • Neuroscience
  • Molecular Biology
  • Pharmacology

Background:

  • Transient Receptor Potential Vanilloid 1 (TRPV1) is a calcium-permeant cation channel found in primary afferent neurons.
  • TRPV1 plays a crucial role in detecting thermal and chemical stimuli, particularly those associated with inflammatory pain.
  • Its distribution extends to both peripheral and central nervous system terminals, influencing action potential initiation and neurotransmitter release.

Purpose of the Study:

  • To discuss the distribution and functions of TRPV1.
  • To explore the potential of TRPV1 agonists and antagonists as analgesics.
  • To highlight non-nociceptive functions of TRPV1 that may cause adverse effects.

Main Methods:

  • Gene deletion studies to reveal TRPV1's role in pain detection.
  • Analysis of TRPV1 distribution in neuronal terminals and the central nervous system.
  • Review of current research on TRPV1 antagonists for analgesic development.

Main Results:

  • TRPV1 deletion significantly impacts the detection of nociceptive and thermal inflammatory pain.
  • TRPV1's presence in non-thermal sensory pathways suggests roles beyond pain sensing.
  • TRPV1 is a promising target for novel analgesic therapies.

Conclusions:

  • TRPV1 is a critical sensor for pain and temperature.
  • Further research into TRPV1's diverse functions is needed to optimize analgesic strategies.
  • Understanding non-nociceptive roles is essential for predicting and mitigating potential side effects of TRPV1-targeting drugs.