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A Novel Carbamoyloxy Arylalkanoyl Arylpiperazine Compound (SKL-NP) Inhibits Hyperpolarization-Activated Cyclic Nucleotide-Gated (HCN) Channel Currents in Rat Dorsal Root Ganglion Neurons

Title
A Novel Carbamoyloxy Arylalkanoyl Arylpiperazine Compound (SKL-NP) Inhibits Hyperpolarization-Activated Cyclic Nucleotide-Gated (HCN) Channel Currents in Rat Dorsal Root Ganglion Neurons
Author
정승준
Keywords
cAMP,; Gi-protein,; Hyperpolarization-activated cyclic nucleotide-gated channel; Ih; Neuropathic pain
Issue Date
2012-08
Publisher
The Korean Society of Pharmacology
Citation
The Korean journal of physiology & pharmacology, 2012, 16(4), P.237-241, 5P.
Abstract
In this study, we determined mode of action of a novel carbamoyloxy arylalkanoyl arylpiperazine compound (SKL-NP) on hyperpolarization-activated cyclic nucleotide-gated (HCN) channel currents ($I_h$) that plays important roles in neuropathic pain. In small or medium-sized dorsal root ganglion (DRG) neurons (< $40{\mu}m$ in diameter) exhibiting tonic firing and prominent $I_h$, SKL-NP inhibited $I_h$ and spike firings in a concentration dependent manner ($IC_{50}=7.85{\mu}M$). SKL-NP-induced inhibition of $I_h$ was blocked by pretreatment of pertussis toxin (PTX) and N-ethylmaleimide (NEM) as well as 8-Br-cAMP, a membrane permeable cAMP analogue. These results suggest that SKL-NP modulates $I_h$ in indirect manner by the activation of a Gi-protein coupled receptor that decreases intracellular cAMP concentration. Taken together, SKL-NP has the inhibitory effect on HCN channel currents ($I_h$) in DRG neurons of rats.
URI
https://synapse.koreamed.org/DOIx.php?id=10.4196/kjpp.2012.16.5.367http://hdl.handle.net/20.500.11754/48164
ISSN
0372-1582; 0377-9459; 1226-4512; 2093-3827
DOI
10.4196/kjpp.2012.16.5.367
Appears in Collections:
COLLEGE OF MEDICINE[S](의과대학) > MEDICINE(의학과) > Articles
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