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Article

Enhancing inactivation rather than reducing activation of Nav1.7 channels by a clinically effective analgesic CNV1014802.

Acta pharmacologica Sinica - 1 Apr 2018

Zheng Yue-Ming, Wang Wan-Fu, Li Yan-Fen, Yu Yong, Gao Zhao-Bing

Abstract excerpt

The Nav1.7 channel represents a promising target for pain relief. In the recent decades, a number of Nav1.7 channel inhibitors have been developed. According to the effects on channel kinetics, these inhibitors could be divided into two major classes: reducing activation or enhancing inactivation. To date, however, only several inhibitors have moved forward into phase 2 clinical trials and most of them display a...

Topics

Analgesics
Animals
CHO Cells
Cricetulus
Electrophysiological Phenomena
HEK293 Cells
Humans
Mutagenesis, Site-Directed
Mutation
NAV1.7 Voltage-Gated Sodium Channel
Phenyl Ethers

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Proline

Voltage-Gated Sodium Channel Blockers

Source

Open in PubMed Open full text

Identifiers

PMID: 29094728
DOI: 10.1038/aps.2017.151
PMCID: PMC5888685

Genes

PEPD

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 29 Aug 2026. Prepared record publication-29094728-2026-08-29.1. Manifest publication-graph-cohort-2026-08-29.1.

Source receipt: PubMed via Helena Literature Corpus, retrieved 29 Aug 2026.

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