Vasodilatation produced by fasudil mesylate in vivo and in vitro

Qin Li; Yuhua Chen; Li Sun; Gang Fu; Lianjun Guo

doi:10.1016/j.vph.2011.06.005

Vasodilatation produced by fasudil mesylate in vivo and in vitro

Vascul Pharmacol. 2011 Nov-Dec;55(5-6):121-6. doi: 10.1016/j.vph.2011.06.005. Epub 2011 Jul 6.

Authors

Qin Li¹, Yuhua Chen, Li Sun, Gang Fu, Lianjun Guo

Affiliation

¹ Department of Pharmacology, Tongji Medical College of Huazhong University of Science and Technology, Wuhan, China.

PMID: 21763460
DOI: 10.1016/j.vph.2011.06.005

Abstract

To investigate the vasorelaxant effect of fasudil mesylate (FM) in vivo and in vitro. The relaxation effect of FM was studied using cerebral vasospasm (CVS) model in vivo and isolated aortic rings in vitro. FM (0.35, 1.2, 3.5 mg·kg⁻¹) increased cerebrovascular flow (CVF) and femoral blood flow (FBF) dose-dependently in vivo, however, the relaxation effects of FM on cerebral vessels were much stronger than on peripheral vessels; FM showed dose-dependent relaxation of isolated aortic rings contracted by Methoxamine (Met) or KCl in vitro. The relaxation IC₅₀ of FM and Prasozin (Pra) to the rabbit aortic rings contracted by Met are 27.54 μM and 0.01 μM respectively, and the relaxation IC₅₀ of FM to the rabbit and rat aortic rings contracted by KCl are 37.15 μM and 0.74 μM respectively. In addition, there is no obvious difference between endothelium-intact and endothelium-removal groups. The Met dose-effect relationship curve was significantly shifted to right by FM (0.3, 3 μM), and E(max) was decreased (P<0.05). The relaxation effect of FM on cerebral vessels was much stronger than on peripheral vessels in vivo, and the action is in an endothelium-independent manner.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / administration & dosage
1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / adverse effects
1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / analogs & derivatives*
1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / pharmacology
1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / therapeutic use
Animals
Aorta, Thoracic / drug effects
Blood Pressure / drug effects
Cerebrovascular Circulation / drug effects*
Dogs
Dose-Response Relationship, Drug
Femoral Artery / drug effects
Femoral Vein / drug effects
Heart Rate / drug effects
In Vitro Techniques
Mesylates / administration & dosage
Mesylates / adverse effects
Mesylates / pharmacology
Mesylates / therapeutic use*
Muscle, Smooth, Vascular / drug effects
Rabbits
Rats
Rats, Wistar
Regional Blood Flow / drug effects
Vascular Resistance / drug effects
Vasodilation / drug effects*
Vasodilator Agents / administration & dosage
Vasodilator Agents / adverse effects
Vasodilator Agents / pharmacology
Vasodilator Agents / therapeutic use*
Vasospasm, Intracranial / drug therapy*
Vasospasm, Intracranial / physiopathology

Substances

Mesylates
Vasodilator Agents
1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
fasudil