PMID: 20647690Jul 22, 2010Paper

Evidence of direct smooth muscle relaxant effects of the fibrate gemfibrozil

Journal of Smooth Muscle Research = Nihon Heikatsukin Gakkai Kikanshi
Laura E Phelps, J D Peuler

Abstract

Fibrates are commonly employed to treat abnormal lipid metabolism via their unique ability to stimulate peroxisome proliferator-activated receptor alpha (PPARalpha). Interestingly, they also decrease systemic arterial pressure, despite recent evidence that PPAR alpha may contribute to expression of renin and related hypertension. Yet, mechanisms responsible for their potential antihypertensive activity remain unresolved. Rapid decreases in arterial pressure following bolus intravenous injections of bezafibrate strongly suggest they may relax arterial smooth muscle directly. But since bezafibrate is highly susceptible to photodegradation in aqueous media, it has never been critically tested for this possibility in vitro with isolated arterial smooth muscle preparations. Accordingly, we tested gemfibrozil which is resistant to photodegradation. We examined it over a therapeutically-relevant range (50-400 microM) for both acute and delayed relaxant effects on contractions of the isolated rat tail artery; contractions induced by either depolarizing its smooth muscle cell membranes with high potassium or stimulating its membrane-bound receptors with norepinephrine and arginine-vasopressin. We also examined these same gemfibrozil lev...Continue Reading

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Citations

Sep 26, 2012·PPAR Research·Neerupma SilswalJon Andresen
Dec 6, 2016·Canadian Journal of Physiology and Pharmacology·Danjun SongAiming Liu
Jul 21, 2016·European Journal of Clinical Investigation·Usama ElewaAlberto Ortiz

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