Cardiovascular and electrophysiological analysis of a selective vasodilatory prostacyclin analogue, 5-nitro-PGI1

V. Kecskeméti, I. Stadler, P. Kormoczy

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Abstract

5-nitro-PGI1 is a selective vasodilatory analogue of prostacyclin which has no antiaggregatory potency. We examined the hemodynamics, antiaggregatory and electrophysiological effects of 5-nitro-PGI1, comparing them with those of PGI2-Na and nitroglycerin (NG). In anaesthetized open-chest cat and dog, PGI2-Na, 5-nitro-PGI1 and NG reduced the mean blood pressure (BP), BP(syst), BP(diast), left ventricular pressure, dp/dt(max) and coronary resistance, while their effect on heart rate and on cardiac output was inconsistent. ED50 values of the BP lowering effect of PGI2-Na, 5-nitro-PGI1 and NG were 4.6 x 10-10, 3.9 x 10-10 and 6 x 10-10 (M), respectively. IC50 values on ADP (10 μM) induced aggregation in rabbit platelet rich plasma of PGI2-Na, 5-nitro-PGI1 and NG were 5 x 10-9, 3.5 x 10-4 and 3.75 x 10-3 (M), respectively. The transmembrane action potential (AP) characteristics were not changed significantly by 10-6 M 5-nitro-PGI1. Higher concentrations (10-5, 10-6 M) slightly reduced the resting potential (RP) and maximum rate of rise (V̇(max)) of AP and shortened AP duration. NG in 10-6 M caused a slight hyperpolarization, while higher concentrations (10-5, 10-4 M) shortened only AP duration. PGI2-Na in all concentrations studied (1.6 x 10-6-10-4 M) caused a slight hyperpolarization, increased potently V̇(max) but shortened AP duration only in high concentration. The results show that 5-nitro-PGI1 exerted the same hemodynamic effect as PGI2-Na and NG, practically failed to exert antiaggregatory activity, and had similar electrophysiological effects to NG.

Original languageEnglish
JournalBiomedica Biochimica Acta
Volume43
Issue number8-9
Publication statusPublished - 1984

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Nitroglycerin
Epoprostenol
Action Potentials
Blood pressure
Blood Pressure
Hemodynamics
Membrane Potentials
Platelet-Rich Plasma
Pressure effects
Ventricular Pressure
Platelets
5-nitroprostaglandin I1
Cardiac Output
Adenosine Diphosphate
Inhibitory Concentration 50
Cats
Thorax
Agglomeration
Heart Rate
Dogs

ASJC Scopus subject areas

  • Biochemistry

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Cardiovascular and electrophysiological analysis of a selective vasodilatory prostacyclin analogue, 5-nitro-PGI1 . / Kecskeméti, V.; Stadler, I.; Kormoczy, P.

In: Biomedica Biochimica Acta, Vol. 43, No. 8-9, 1984.

Research output: Contribution to journalArticle

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