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 Scijournal_title
Journal of pharmacological sciencesauthors
Agharkar AS,Gonzales EBdoi
10.1016/j.jphs.2017.02.007subject
Has Abstractpub_date
2017-03-01 00:00:00pages
184-186issue
3eissn
1347-8613issn
1347-8648pii
S1347-8613(17)30022-1journal_volume
133pub_type
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