Cardiology Research and Practice

Review Article

Endothelium-Derived Hyperpolarizing Factor and Vascular Function

Table 1

Pharmacological inhibitors of EDHF. Pharmacological agents used as potential inhibitors of EDHF and their targets and limitations (modified from Torondel et al. [117]).
Pharmacological inhibitorsTargetsComments
Apamin S K + C a Highly specific
Charybdotoxin I K + C a - B K + C a Can inhibit some Kv channels
Iberiotoxin B K + C a Highly specific
Tetraethylammonium S K + C a - I K + C a - B K + C a Inhibit other K+  channels at >10−2) m
Tetraethybutylammonium S K + C a - I K + C a - B K + C a Inhibit other K+  channels at >10−2 m
BaCl2 K + I R —
OuabainNa+/K+ ATPaseCan affect gap junction activity at >10−4 m
KCLK+ currentsDilates at >10−2 m through K + I R and Na+/K+ ATPase activation
18 α-glycyrrhetic acidGap junctionsPossesses nonjunctional effects on membrane currents
Connexin mimetic peptidesGap junctionsHighly specific
CatalaseHydrogen peroxide—
17-octadecenoic acidCYPInhibits the synthesis of the vasoconstrictor 20-HETE
ClotrimazoleCYPCan inhibit K+ channels
MiconazoleCYPCan inhibit K+ channels
SulphaphenazoleCYP epoxygenaseHighly specific of CYP 2C9
FluconazoleCYP epoxygenaseCan inhibit other CYP isoforms at >10−4 m
MSPPOHEETs synthesis inhibitorHighly specific
14,15-EEZEEETs antagonistInhibits the vasodilator action of all EETs regioisomers
K+: potassium, S K + C a : small calcium-dependent potassium channels, I K + C a : intermediate calcium-dependent potassium channels, B K + C a : large calcium-dependent potassium channels, Kv: voltage dependent potassium channels, K + I R : inwardly rectifying potassium channels, BaCl2 barium chloride, KCL: potassium chloride, CYP: cytochrome, 20-HETE: 20-hydroxyeicosatetraenoic acids, MSPPOH: N-(methylsulfonyl)-2-(2-propynyloxy)-benzenehexanamide, EETs: epoxyeicosatrienoic acids, and 14,15-EEZE: 14,15-Epoxyeicosa-5(Z)-enoic Acid.