4-Chlorophenylguanidine is an ASIC3 agonist and positive allosteric modulator.

Abstract:

:Acid-sensing ion channels (ASICs) are proton-sensitive sodium channels that open in response to lowered extracellular pH and are expressed in the central and peripheral nervous systems. The ASIC3 subtype is found primarily in the periphery where the channel mediates pain signals caused by ischemia and inflammation. Here, we provide identify 4-chlorophenylguanidine (4-CPG) as an ASIC3 positive allosteric modulator and newest member of the growing group of guanidine modulators of ASICs. Furthermore, the 4-CPG reversed the effects of ASIC3 desensitization. The molecule 4-CPG offers a novel chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo.

journal_name

J Pharmacol Sci

authors

Agharkar AS,Gonzales EB

doi

10.1016/j.jphs.2017.02.007

subject

Has Abstract

pub_date

2017-03-01 00:00:00

pages

184-186

issue

3

eissn

1347-8613

issn

1347-8648

pii

S1347-8613(17)30022-1

journal_volume

133

pub_type

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