Biomaterial Database

Effect of nisoldipine on contractions evoked by endothelin-1 in human isolated distal and proximal coronary arteries and veins. 1994

J L Balligand, and T Godfraind

Laboratoire de Pharmacologie, Université Catholique de Louvain, Brussels, Belgium.

We investigated the differences in the vasoconstrictor effect of endothelin-1 (ET-1) on small and large human coronary arteries and veins and blockade of ET's action with calcium antagonists. Rings from distal and proximal human coronary arteries and veins were suspended in organ baths and exposed to graded concentrations of ET-1 (0.1-30 nM). Coronary veins were the most sensitive to the constrictor action of ET-1. In addition, distal coronary arteries were more sensitive than proximal arteries (EC50 value-log M: 8.92 +/- 0.05 and 8.34 +/- 0.1, respectively). In proximal arteries, incubation with subthreshold concentrations of ET (300 pM) potentiated the vasoconstrictor effect of serotonin 1 microM (115 +/- 2.6% over contractile level before incubation). This potentiated contraction was fully blocked by nisoldipine, a calcium antagonist. In contrast, this potentiation was not observed in human coronary veins. Nisoldipine partly antagonized the contraction evoked by ET-1 in human coronary arteries, but ET-contracted coronary veins were completely resistant to calcium channel blockade. Low concentrations of ET-1 approximating reported circulating levels result in significant contraction of human coronary veins and potentiate the constrictor effect of serotonin in coronary arteries. The blocking effect of the calcium antagonist nisoldipine varies among distal and proximal coronary arteries and veins, suggesting a different mechanism of contraction for ET-1 among these vessels. Because of the suspected role of ET-1 in coronary ischemic syndromes, this differential sensitivity may have important therapeutic implications.

UI	MeSH Term	Description	Entries
D009119	Muscle Contraction	A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009131	Muscle, Smooth, Vascular	The nonstriated involuntary muscle tissue of blood vessels.	Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D003331	Coronary Vessels	The veins and arteries of the HEART.	Coronary Arteries,Sinus Node Artery,Coronary Veins,Arteries, Coronary,Arteries, Sinus Node,Artery, Coronary,Artery, Sinus Node,Coronary Artery,Coronary Vein,Coronary Vessel,Sinus Node Arteries,Vein, Coronary,Veins, Coronary,Vessel, Coronary,Vessels, Coronary
D004305	Dose-Response Relationship, Drug	The relationship between the dose of an administered drug and the response of the organism to the drug.	Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004357	Drug Synergism	The action of a drug in promoting or enhancing the effectiveness of another drug.	Drug Potentiation,Drug Augmentation,Augmentation, Drug,Augmentations, Drug,Drug Augmentations,Drug Potentiations,Drug Synergisms,Potentiation, Drug,Potentiations, Drug,Synergism, Drug,Synergisms, Drug
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D012701	Serotonin	A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.	5-HT,5-Hydroxytryptamine,3-(2-Aminoethyl)-1H-indol-5-ol,Enteramine,Hippophaine,Hydroxytryptamine,5 Hydroxytryptamine
D015737	Nisoldipine	A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.	Bay K 5552
D016232	Endothelins	21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.	Endothelium-Derived Vasoconstrictor Factors,Endothelin,Vasoconstrictor Factors, Endothelium-Derived
D066298	In Vitro Techniques	Methods to study reactions or processes taking place in an artificial environment outside the living organism.	In Vitro Test,In Vitro Testing,In Vitro Tests,In Vitro as Topic,In Vitro,In Vitro Technique,In Vitro Testings,Technique, In Vitro,Techniques, In Vitro,Test, In Vitro,Testing, In Vitro,Testings, In Vitro,Tests, In Vitro,Vitro Testing, In