ONO-54918-07, a stable prostacyclin analogue, mimics the effect of prostaglandin PGE1 on NG108-15 cells

Naunyn Schmiedebergs Arch Pharmacol. 2007 Nov;376(3):165-73. doi: 10.1007/s00210-007-0186-2. Epub 2007 Oct 19.

Abstract

The aim of this study was to explore the effect of 0NO-54918-07, a stable prostacyclin analogue, on the current-voltage (IV) curve and the intracellular Ca2+ concentration [Ca2+]i of NG108-15 neuroblastoma x glioma hybrid cells. The IV curve was measured with ramp pulses from -70 to 0 mV, and [Ca2+]i was determined with Fura 2. Bath application of 0.2 muM ONO-54918-07 reversibly increased the holding current at -70 mV by -81.1 +/- 14.8 pA (mean +/- SEM, n = 35) and the slope of the IV curve between -70 and -50 mV by the factor 2.24 +/- 0.24. The effect of 0.2 microM prostaglandin PGE1 was similar (DeltaI (hold) = -96.1 +/- 29.9 pA, g/g (control) = 2.72 +/- 0.44, n = 9). ONO-54918-07 concentrations of 0.04, 2 and 6 microM were also effective. From the dose-response curve, the concentration for the half maximal effect was obtained as 0.054 microM. When cells did not respond to ONO-54918-07, an effect could sometimes be elicited by a ramp pulse or by a second ONO-54918-07 application 30-50 min after the first. The effect of ONO-54918-07 was not affected by pre-treatment with the EP1 antagonists ONO-8713 or SC-51089. However, a 14-40 min pre-treatment with 1 microM RO3244794, a selective prostacyclin receptor (IP) antagonist, abolished the effect of 0.2 microM PGE1. The effect of 0.2 microM ONO-54918-07 vanished completely in the presence of 5 microM RO32446794. ONO-54918-07 and PGE1 produced a slow increase in [Ca2+]i that lasted at least 6 min. Delta[Ca2+]i induced by both substances reached approximately 12% of the peak Delta[Ca2+]i induced by application of bradykinin. In only a few cells, PGE1 produced a brief, transient rise of [Ca2+]i. Using reverse transcriptase polymerase chain reaction, a prominent expression of the IP was detected in NG108-15 cells. It is concluded that ONO-54918-07 mimics the effect of PGE1, supporting the notion that the PGE1 effect on NG108-15 cells is mediated by IP receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alprostadil / metabolism
  • Alprostadil / pharmacology*
  • Animals
  • Benzofurans / pharmacology
  • Calcium / metabolism
  • Cell Line, Tumor
  • Cinnamates / pharmacology
  • Cytosol / metabolism
  • Dose-Response Relationship, Drug
  • Hydrazines / pharmacology
  • Mice
  • Oxazepines / pharmacology
  • Patch-Clamp Techniques
  • Propionates / pharmacology
  • Prostaglandins F / pharmacology*
  • Receptors, Epoprostenol / antagonists & inhibitors*
  • Receptors, Epoprostenol / metabolism
  • Receptors, Prostaglandin E / antagonists & inhibitors
  • Receptors, Prostaglandin E / metabolism
  • Receptors, Prostaglandin E, EP1 Subtype
  • Vasodilator Agents / pharmacology

Substances

  • 15-cis-(4-n-propylcyclohexyl)-16,17,17,19,20-pentanor-9-deoxy-6,9-alpha-nitriloprostaglandin F1
  • Benzofurans
  • Cinnamates
  • Hydrazines
  • ONO 8713
  • Oxazepines
  • Propionates
  • Prostaglandins F
  • Ptger1 protein, mouse
  • RO3244794
  • Receptors, Epoprostenol
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP1 Subtype
  • Vasodilator Agents
  • SC 51089
  • Alprostadil
  • Calcium