Inhibition of Kv1.3 channels by H-89 (N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide) independent of protein kinase A

Jin Sung Choi, Bok Hee Choi, Sang June Hahn, Shin Hee Yoon, Do Sik Min, Yang Hyeok Jo, Myung Suk Kim

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

The effects of H-89 (N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide), a potent and selective inhibitor of protein kinase A (PKA), were examined on Kv1.3 channels stably expressed in Chinese hamster ovary (CHO) cells using the patch clamp technique. In whole-cell recordings, H-89 decreased Kv1.3 currents and accelerated the decay rate of current inactivation in a concentration-dependent manner with an ic50 value of 1.70 μM. These effects were completely reversible after washout. Intracellular infusion with PKA inhibitors, adenosine 3′, 5′-cyclic phosphorothioate-Rp (Rp-cAMPS) or protein kinase A inhibitor 5-24 (PKI 5-24) had no effect on Kv1.3 currents and did not prevent the inhibitory action of H-89 on the current. H-89 applied to the cytoplasmic surface also inhibited Kv1.3 currents in excised inside-out patches. These findings suggest that H-89 inhibits Kv1.3 currents independently of PKA.

Original languageEnglish
Pages (from-to)1029-1032
Number of pages4
JournalBiochemical Pharmacology
Volume61
Issue number8
DOIs
Publication statusPublished - 2001 Apr 15

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Pharmacology

Fingerprint Dive into the research topics of 'Inhibition of Kv1.3 channels by H-89 (N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide) independent of protein kinase A'. Together they form a unique fingerprint.

  • Cite this