Related Experiment Video

Updated: Apr 17, 2026

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

9.1K

Transient receptor potential vanilloid type 1 antagonists: a patent review (2011 - 2014)

Yoonji Lee1, Sunhye Hong, Minghua Cui

  • 1Ewha Womans University, National Leading Research Laboratory of Molecular Modeling and Drug Design, College of Pharmacy, Graduate School of Pharmaceutical Sciences, and Global Top 5 Research Program , Seoul 120-750 , Korea +82 2 3277 4503 ; +82 2 3277 2851 ; sunchoi@ewha.ac.kr.

Expert Opinion on Therapeutic Patents
|February 11, 2015
PubMed
Abstract

Insights

Transient receptor potential vanilloid type 1 (TRPV1) antagonists show promise for pain relief. Recent patents reveal novel small molecules that overcome side effects, advancing analgesic development.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Pain Therapeutics

Background:

  • Transient receptor potential vanilloid type 1 (TRPV1) channels integrate painful stimuli.
  • TRPV1 antagonists are explored as novel analgesics.

Purpose of the Study:

  • Review patents for TRPV1 antagonists from 2011-2014.
  • Summarize chemical entities and their efficacy data.

Main Methods:

  • Patent literature search (2011-2014).
  • Analysis of TRPV1 antagonist patents by applicant.
  • Summary of in vitro and in vivo data for key compounds.

Main Results:

  • Numerous pharmaceutical companies developing small molecule TRPV1 antagonists.
  • Advancement of several antagonists into clinical trials.
  • Identification of compounds overcoming previous side effects like hyperthermia.

Conclusions:

  • Recent TRPV1 antagonists show improved safety profiles.
  • Development of TRPV1 antagonists for pain management is increasingly promising.
  • Patented compounds from 2011-2014 offer new therapeutic avenues.
Keywords:
TRPV1TRPV1 antagonistVR1VR1 antagonistcapsaicintransient receptor potentialvanilloid

More Related Videos

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV412:09

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

Published on: December 31, 2013

10.8K
Establishing a Mouse Model of a Pure Small Fiber Neuropathy with the Ultrapotent Agonist of Transient Receptor Potential Vanilloid Type 109:39

Establishing a Mouse Model of a Pure Small Fiber Neuropathy with the Ultrapotent Agonist of Transient Receptor Potential Vanilloid Type 1

Published on: February 13, 2018

10.2K

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...
35.6K
Non-gated Ion Channels01:24

Non-gated Ion Channels

Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism....
9.2K
Patch Clamp01:18

Patch Clamp

Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
In this method, a glass micropipette containing electrolyte solution is tightly sealed against a small portion of the cell membrane. As a result, a patch of the cell...
7.7K
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

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...
788
Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein01:20

Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein

Antiepileptic drugs, such as levetiracetam (Keppra) and brivaracetam (Briviact), have emerged as crucial tools in managing epilepsy. These medications exert their therapeutic effects by targeting the synaptic vesicle protein SV2A, a transmembrane glycoprotein primarily found in the brain.
SV2A is a transmembrane glycoprotein located predominantly in the brain, modulating the release of neurotransmitters for neuronal communication. Both levetiracetam and brivaracetam exhibit a high affinity for...
1.2K
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...
5.7K