Related Experiment Video
Updated: Jun 14, 2026

Intracerebroventricular Treatment with Resiniferatoxin and Pain Tests in Mice
Published on: September 2, 2020
Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists
Charles A Blum1, Timothy Caldwell, Xiaozhang Zheng
1Neurogen Corporation, 35 Northeast Industrial Road, Branford, Connecticut 06405, USA.
Abstract:
The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a nonselective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation in an attempt to identify novel agents for pain treatment. The design and synthesis of a series of novel TRPV1 antagonists with a variety of different 6,6-heterocyclic cores is described, and an extensive evaluation of the pharmacological and pharmacokinetic properties of a number of these compounds is reported. For example, the 1,8-naphthyridine 52 was characterized as an orally bioavailable and brain penetrant TRPV1 antagonist. In vivo, 52 fully reversed carrageenan-induced thermal hyperalgesia (CITH) in rats and dose-dependently potently reduced complete Freund's adjuvant (CFA) induced chronic inflammatory pain after oral administration.
Related Concept Videos
Thermosensation
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists
Non-gated Ion Channels
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
GPCR Desensitization
Opioid Receptors: Overview
