A Novel Carbamoyloxy Arylalkanoyl Arylpiperazine Compound (SKL-NP) Inhibits Hyperpolarization-Activated Cyclic Nucleotide-Gated (HCN) Channel Currents in Rat Dorsal Root Ganglion Neurons
The Korean Journal of Physiology and Pharmacology
;
: 237-241, 2012.
Article
Dans Anglais
| WPRIM
| ID: wpr-728094
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 (Ih) that plays important roles in neuropathic pain. In small or medium-sized dorsal root ganglion (DRG) neurons (<40 microm in diameter) exhibiting tonic firing and prominent Ih, SKL-NP inhibited Ih and spike firings in a concentration dependent manner (IC50=7.85 microM). SKL-NP-induced inhibition of Ih 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 Ih 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.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Racines des nerfs spinaux
/
Groupes homogènes de malades
/
Toxine pertussique
/
N-Éthyl-maléimide
/
Incendies
/
Ganglions sensitifs des nerfs spinaux
/
Membranes
/
Névralgie
/
Neurones
Limites du sujet:
Animaux
langue:
Anglais
Texte intégral:
The Korean Journal of Physiology and Pharmacology
Année:
2012
Type:
Article
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