ArticleBritish journal of pharmacology1999
Inhibition by genistein of the hyperpolarization-activated cation current in porcine sino-atrial node cells.
Article in British journal of pharmacology, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 21 citations in OpenAlex.
- Comparative study of hyperpolarization-activated currents in pulmonary vein cardiomyocytes isolated from rat, guinea pig, and rabbit.The journal of physiological sciences : JPS · 2020Article
- Voltage-dependent opening of HCN channels: Facilitation or inhibition by the phytoestrogen, genistein, is determined by the activation status of the cyclic nucleotide gating ring.Biochimica et biophysica acta · 2009Article
- Age-dependent differences in the inhibition of HCN2 current in rat ventricular myocytes by the tyrosine kinase inhibitor erbstatin.Pflugers Archiv : European journal of physiology · 2009Article
- Constitutively active Src tyrosine kinase changes gating of HCN4 channels through direct binding to the channel proteins.Journal of cardiovascular pharmacology · 2006Article
- Direct inhibition of the pacemaker (If) current in rabbit sinoatrial node cells by genistein.British journal of pharmacology · 2006Article
- Regulation of recombinant and native hyperpolarization-activated cation channels.Molecular neurobiology · 2004Review
- Properties of the delayed rectifier potassium current in porcine sino-atrial node cells.The Journal of physiology · 2000Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1 The hyperpolarization-activated cation current (If) was recorded in single pacemaker cells of the porcine sino-atrial node, and the effects of genistein, an isoflavone inhibitor of tyrosine-specific protein kinases was investigated by the whole-cell patch clamp technique. 2 Genistein (20-500 microM) decreased If in a dose-dependent manner with an IC50 value of 62.3 microM and a maximum inhibition of 45.3%. 3 The effect on If appeared without altering the half-activation potential (control, -88.3+/-2.8 mV; genistein, -87.0+/-1.8 mV) and the slope factor (control, 8.0+/-0.3 mV; genistein, 8.6+/-0.7 mV) of the steady-state activation curve. No significant voltage-dependency was detected in the fully-activated current-voltage relation measured by the double-pulse protocols. 4 The inactive form of genistein analogue, daidzein (500 microM) or genistin (200 microM), were without effect. If was not affected by another tyrosine kinase inhibitor, tryphostin-47 (100 microM), but tyrphostin-25 (100-200 microM) suppressed If in an irreversible manner. 5 Neither bath nor intracellular application of the tyrosine phosphatase inhibitor, orthovanadate, affected If, and subsequent application of genistein inhibited If significantly. 6 These data indicate that the inhibition of If by genistein is not mediated through tyrosine kinase inhibition but through nonselective block of the If channels.
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