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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...
Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers01:22

Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers

α-Adrenergic antagonists, known as α-blockers, exert their effects by inhibiting α-adrenoceptors, leading to specific physiological actions. α1-blockers and α2-blockers have distinct pharmacological actions and therapeutic applications.
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally, α1-blockers effectively address urinary obstruction...
Cholinergic Antagonists: Pharmacological Actions01:28

Cholinergic Antagonists: Pharmacological Actions

Antimuscarinic drugs block muscarinic receptors in multiple systems, including the gut, eye, smooth muscles, respiratory tract, cardiovascular, and central nervous systems. They produce similar effects with varying selectivity depending on the specific agent and tissue. Here are the key pharmacological actions of antimuscarinics:
Gastrointestinal Effects: Antimuscarinics reduce gut contractions, increase gastric emptying, and slow intestinal transit. They partly inhibit gastric acid secretion...
Drug-Receptor Interaction: Antagonist01:28

Drug-Receptor Interaction: Antagonist

An antagonist is a drug that binds strongly to a receptor without activating it. An antagonist prevents other molecules, such as neurotransmitters or hormones, from binding to the receptor and triggering a cellular response. Such interaction effectively hinders the normal physiological processes mediated by the receptor, resulting in various pharmacological effects depending on the specific receptor targeted.
Antagonists can be classified as competitive or noncompetitive based on their...
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists

5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...

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Related Experiment Video

Updated: Jun 1, 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

TRPV4 agonists and antagonists.

Fabien Vincent1, Matthew A J Duncton

  • 1Renovis, Inc. (a wholly-owned subsidiary of Evotec AG), Two Corporate Drive, South San Francisco, CA 94066, USA. fabien_vincent_us@yahoo.com

Current Topics in Medicinal Chemistry
|June 16, 2011
PubMed
Summary

TRPV4 (Transient Receptor Potential Vanilloid 4) ion channels are crucial for various physiological functions. Research is exploring TRPV4 modulators for treating pain, bladder dysfunction, and lung injury.

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Intracerebroventricular Treatment with Resiniferatoxin and Pain Tests in Mice
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Intracerebroventricular Treatment with Resiniferatoxin and Pain Tests in Mice

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Last Updated: Jun 1, 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:

  • Ion channel research
  • Physiology
  • Pharmacology

Background:

  • TRPV4 is a polymodal ion channel activated by diverse stimuli like temperature, osmolarity, and lipids.
  • It plays significant roles in skin, kidney, vasculature, and bone.
  • Therapeutic targeting of TRPV4 is gaining interest due to its physiological importance.

Purpose of the Study:

  • To review known small molecule modulators of TRPV4.
  • To discuss progress in identifying potent and selective TRPV4 agonists and antagonists.
  • To highlight therapeutic potential for various conditions.

Main Methods:

  • Review of existing literature on TRPV4 modulators.
  • Analysis of studies using knockout mice and specific agonists (4αPDD, GSK1016790A).
  • Focus on small molecule identification for in vivo interrogation.

Main Results:

  • TRPV4 antagonism is considered for inflammatory and neuropathic pain.
  • TRPV4 modulation may target bladder dysfunctions.
  • Ventilator-induced lung injury is a potential indication for TRPV4 antagonists.

Conclusions:

  • TRPV4 ion channels have diverse physiological roles.
  • Development of selective TRPV4 modulators is advancing.
  • TRPV4 represents a promising therapeutic target for multiple diseases.