Discovery of Non-pungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic.

07:00 EST 8th November 2019 | BioPortfolio

Summary of "Discovery of Non-pungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic."

Paradoxically, some TRPV1 agonists are, at the organismal level, both non-pungent and clinically useful as topical analgesics. Here, we describe the scaled-up synthesis and characterization in mouse models of a novel, non-pungent vanilloid. Potent analgesic ac-tivity was observed in models of neuropathic pain, and the compound blocked capsaicin induced allodynia, showing dermal accu-mulation with little transdermal absorption. Finally, it displayed much weaker systemic toxicity compared to capsaicin and was negative in assays of genotoxicity.


Journal Details

This article was published in the following journal.

Name: Journal of medicinal chemistry
ISSN: 1520-4804


DeepDyve research library

PubMed Articles [16419 Associated PubMed Articles listed on BioPortfolio]

A New Target to Ameliorate the Damage of Periodontal Disease: The Role of Transient Receptor Potential Vanilloid Type-1 in Contrast to That of Specific Cannabinoid Receptors in Rats.

Transient receptor potential vanilloid type-1 (TRPV1) is expressed in oral tissues cells and its activity can be regulated by inflammation products and anandamide. The aim of the present study was to ...

Structural Mechanism Underlying TRPV1 Activation by Pungent Compounds in Gingers.

Like chili peppers, gingers produce pungent stimuli by a group of vanilloid compounds that activate the nociceptive TRPV1 ion channel. How these compounds interact with TRPV1 remains unclear.

Chalcone derivatives as non-canonical ligands of TRPV1.

Transient receptor potential vanilloid 1 (TRPV1) is a polymodal cation channel activated by heat, voltage, and ligands. Also known as the capsaicin receptor, TRPV1 is expressed in numerous tissues by ...

Effects of early intravesical administration of resiniferatoxin to spinal cord-injured rats in neurogenic detrusor overactivity.

To investigate if intravesical administration during spinal shock of resiniferatoxin (RTX), an ultrapotent desensitizing agonist of transient receptor potential vanilloid-1 (TRPV1), would silence TRPV...

The Transient Receptor Potential Vanilloid 4 Agonist RN-1747 Inhibits the Calcium Response to Histamine.

Sensitization of transient receptor potential (TRP) cation channels probably contributes to intestinal hypersensitivity, a hallmark of gastrointestinal disorders. Histamine acting via histamine 1 rece...

Clinical Trials [5260 Associated Clinical Trials listed on BioPortfolio]

Transient Receptor Potential Vanilloid One (TRPV1) Receptor Expression in Children With Retrosternal Pain

We would like to evaluate the changes in nerve innervation and TRPV1 receptor expression along with microscopic changes associated with heart burn and abdominal pain

A Study on the Mechanism of Cough Hypersensitivity

The aim of this study is described as follows, 1. To establish a validated method to test cough reflex sensitivity conducted by transient receptor potential vanilloid 1(TRPV1). ...

The Functional Consequences of the CTNS-deletion for the TRPV1-receptor in Cystinosis Patients

Cystinosis is a rare autosomal recessive disorder, characterized by the abnormal accumulation of cystine in the lysosomes. Cystinosis is mostly caused by mutations in the cystinosin gene (...

TRPV2 Agonists in the Fontan Circulation

There are currently very few proven pharmacologic options available for these patients. The recent discovery of transient receptor potential vanilloid (TRPV) channels, particularly TRPV2 c...

Mannitol Cream for Post Herpetic Neuralgia

30% mannitol cream has shown its ability to reduce the activation of the Capsaicin (TRPV1) (Transient Receptor Potential Vanilloid 1) receptor, a likely cause of the pain of post-herpetic ...

Medical and Biotech [MESH] Definitions

A plant genus of the family SOLANACEAE. The hot peppers yield CAPSAICIN, which activates vanilloid receptors. Several varieties have sweet or pungent edible fruits that are used as vegetables when fresh and spices when the pods are dried.

A broad group of eukaryotic six-transmembrane cation channels that are classified by sequence homology because their functional involvement with SENSATION is varied. They have only weak voltage sensitivity and ion selectivity. They are named after a DROSOPHILA mutant that displayed transient receptor potentials in response to light. A 25-amino-acid motif containing a TRP box (EWKFAR) just C-terminal to S6 is found in TRPC, TRPV and TRPM subgroups. ANKYRIN repeats are found in TRPC, TRPV & TRPN subgroups. Some are functionally associated with TYROSINE KINASE or TYPE C PHOSPHOLIPASES.

The process of finding chemicals for potential therapeutic use.

The systematic search and discovery of natural substances which may have potential commercial applications.

A subgroup of TRP cation channels named after vanilloid receptor. They are very sensitive to TEMPERATURE and hot spicy food and CAPSAICIN. They have the TRP domain and ANKYRIN repeats. Selectivity for CALCIUM over SODIUM ranges from 3 to 100 fold.

Quick Search

DeepDyve research library

Relevant Topics

Pain is defined by the International Association for the Study of Pain as “an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage”. Some illnesses can be excruci...

An anesthesiologist (US English) or anaesthetist (British English) is a physician trained in anesthesia and perioperative medicine. Anesthesiologists are physicians who provide medical care to patients in a wide variety of (usually acute) situations. ...

Searches Linking to this Article