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The Korean Journal of Physiology and Pharmacology ; : 237-241, 2012.
Artigo em Inglês | WPRIM | ID: wpr-728094

RESUMO

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.


Assuntos
Animais , Ratos , Grupos Diagnósticos Relacionados , Etilmaleimida , Incêndios , Gânglios Espinais , Membranas , Neuralgia , Neurônios , Toxina Pertussis , Raízes Nervosas Espinhais
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