Home
Resources
Publications
Novel Charged Sodium and Calcium Channel Inhibitor Active Against Neurogenic Inflammation

Novel Charged Sodium and Calcium Channel Inhibitor Active Against Neurogenic Inflammation

Seungkyu Lee, Sooyeon Jo, Sébastien Talbot, Han-Xiong Bear Zhang, Masakazu Kotoda, Nick A Andrews, Michelino Puopolo, Pin W Liu, Thomas Jacquemont, Maud Pascal, Laurel M Heckman, Aakanksha Jain, Jinbo Lee, etc.

Elife. 2019 Nov 25;8:e48118.

PMID: 31765298

Abstract:

Voltage-dependent sodium and calcium channels in pain-initiating nociceptor neurons are attractive targets for new analgesics. We made a permanently charged cationic derivative of an N-type calcium channel-inhibitor. Unlike cationic derivatives of local anesthetic sodium channel blockers like QX-314, this cationic compound inhibited N-type calcium channels more effectively with extracellular than intracellular application. Surprisingly, the compound is also a highly effective sodium channel inhibitor when applied extracellularly, producing more potent inhibition than lidocaine or bupivacaine. The charged inhibitor produced potent and long-lasting analgesia in mouse models of incisional wound and inflammatory pain, inhibited release of the neuropeptide calcitonin gene-related peptide (CGRP) from dorsal root ganglion neurons, and reduced inflammation in a mouse model of allergic asthma, which has a strong neurogenic component. The results show that some cationic molecules applied extracellularly can powerfully inhibit both sodium channels and calcium channels, thereby blocking both nociceptor excitability and pro-inflammatory peptide release.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
CS310327	Bupivacaine Related Compound A			Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: