Effects of calcium antagonists and agonists on isolated human v. saphena magna used for coronary artery bypass grafting and guinea pig’s papillary muscle

Vida Garaliene; Vygantas Barsys; Povilas Jakuška; Aivars Krauze; Gunar Duburs

doi:10.1055/s-0031-1296216

Arzneimittelforschung, Inhaltsverzeichnis

Arzneimittelforschung 2011; 61(7): 386-392
DOI: 10.1055/s-0031-1296216

Cardiac Drugs · Cardiac Stimulants · Coronary Drugs

Editio Cantor Verlag Aulendorf (Germany)

Effects of calcium antagonists and agonists on isolated human v. saphena magna used for coronary artery bypass grafting and guinea pig’s papillary muscle

Vida Garaliene

¹Institute of Cardiology at Medical Academy of Lithuanian University of Health Sciences, Kaunas, Lithuania

,

Vygantas Barsys

¹Institute of Cardiology at Medical Academy of Lithuanian University of Health Sciences, Kaunas, Lithuania

,

Povilas Jakuška

²Department of Cardiothoracic and Vascular Surgery at Lithuanian University of Health Sciences, Kaunas, Lithuania

,

Aivars Krauze

³Latvian Institute of Organic Synthesis, Riga, Latvia

,

Gunar Duburs

³Latvian Institute of Organic Synthesis, Riga, Latvia

› Institutsangaben

Abstract

Background:

The goal of this study was to investigate the movement of contraction-relaxation effects on isolated human blood vessel samples by the actions of amlodipine (CAS 88150-42-9), cerebrocrast (CAS 118790-71-9), diltiazem (CAS 42399-41-7), and a benzimidazole derivative. Additionally, their effects on isometric contraction force and the duration of the action potential (AP) were measured.

Methods:

The experiments were carried out on isolated human v. saphena magna samples and papillary muscles of adult guinea pigs. Isometric contraction and the AP were recorded using a force transducer and standard microelectrode technique.

Results:

Phenylephrine (10⁻⁴ M) caused contractions of vein rings to 928 ± 76.5 mg. All the tested agents at a concentration of 10⁻⁷–10⁻⁴ M significantly relaxed the smooth muscle in a dose-dependent manner. The weakest response was shown by amlodipine. Pre-treatment with 50 >M of amlodipine, diltiazem and benzimidazole for 30 min significantly increased the magnitude of the contraction induced by phenylephrine in concentration-dependent (10⁻⁶–10⁻⁴) fashion but only in the benzimidazole group versus other tested agents and the control. The benzimidazole derivative caused augmentation of isometric contraction of the papillary muscles and negligible lengthening of AP duration; the other agents tested showed opposite effects.

Conclusion:

These results show that agents possessing positive or negative inotropic action significantly relaxed the isolated vein samples precontracted with phenylephrine. These responses point to a different mechanism of action underlying both calcium antagonist and agonist effects even though their action ultimately resulted in vasodilatation.

Key words

1-Acetyl-5,6-dimethoxy-2-methylthiobenzimidazole - Amlodipine - Cerebrocrast - Diltiazem - Guinea pig papillary muscles - Human v. saphena magna

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Referenzen

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