Stereospecific effects of epoxyeicosatrienoic acids on renal vascular tone and K(+)-channel activity

Am J Physiol. 1996 May;270(5 Pt 2):F822-32. doi: 10.1152/ajprenal.1996.270.5.F822.

Abstract

The present study examined the effects of 11,12- and 14,15-epoxyeicosatrienoic acids (EETs) on the diameter of small renal arteries of the rat and assessed their action on K(+)-channel activity in vascular smooth muscle (VSM) cells isolated from these vessels. The R,S-isomer of 11,12-EET (1, 10, and 100 nM) increased the diameter of small renal arteries preconstricted with phenylephrine; however, the S,R-isomer was inactive. Both the R,S- and S,R-isomers of 14,15-EET had little effect on the diameter of these vessels even at a high concentration (100 nM). The vasodilator effect of 11(R),12(S)-EET was attenuated by tetraethylammonium (TEA, 1 mM) and iberiotoxin (100 nM), selective inhibitors of the large-conductance Ca(2+)-activated K+ (KCa) channel. In contrast, apamin (100 nM) and 4-aminopyridine (2 mM), which are inhibitors of other types of K+ channels, had no effect on the vasodilatory effect of 11,12-EET. In patch-clamp experiments, 100 nM racemic 11,12-EET increased outward K+ currents in VSM cells. Addition of the R,S-isomer or racemic 11,12-EET (1-100 nM), but not the S,R-isomer, increased the activity of KCa channel recorded from renal VSM cells with cell-attached patches. However, racemic EET had no effect on this channel when added to the internal (inside-out) or external (outside-out) face of excised membrane patches. These results suggest that 11,12-EET is a potent dilator of small renal arteries and that the R,S-isomer is the active enantiomer. The vasodilator effect of 11,12-EET appears to involve activation of KCa channel.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 8,11,14-Eicosatrienoic Acid / analogs & derivatives*
  • 8,11,14-Eicosatrienoic Acid / pharmacology
  • Animals
  • Calcium / pharmacology
  • Electric Conductivity
  • Muscle Tonus / drug effects
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / metabolism
  • Patch-Clamp Techniques
  • Potassium Channels / drug effects*
  • Potassium Channels / physiology
  • Rats
  • Rats, Sprague-Dawley
  • Renal Artery / drug effects*
  • Renal Artery / physiology
  • Stereoisomerism
  • Vasoconstriction

Substances

  • Potassium Channels
  • 11,12-epoxy-5,8,14-eicosatrienoic acid
  • 14,15-epoxy-5,8,11-eicosatrienoic acid
  • 8,11,14-Eicosatrienoic Acid
  • Calcium