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Your search keyword '"C, Thurieau"' showing total 2 results
Start Over Author "C, Thurieau" Publisher elsevier science
2 results on '"C, Thurieau"'

1. In vitro effects of HOE 140 in human bronchial and vascular tissue.

Author

Félétou M, Martin CA, Molimard M, Naline E, Germain M, Thurieau C, Fauchère JL, Canet E, and Advenier C

Subjects
Binding Sites, Bradykinin metabolism, Bradykinin pharmacology, Bronchi metabolism, Endothelium, Vascular physiology, Humans, In Vitro Techniques, Isometric Contraction drug effects, Muscle Relaxation drug effects, Pulmonary Artery drug effects, Pulmonary Artery metabolism, Umbilical Arteries drug effects, Umbilical Arteries metabolism, Umbilical Veins drug effects, Umbilical Veins metabolism, Bradykinin analogs & derivatives, Bradykinin antagonists & inhibitors, Bronchi drug effects, Muscle, Smooth drug effects, Muscle, Smooth, Vascular drug effects
Abstract

Bradykinin is a potent inflammatory mediator which may be involved in various airway diseases. A selective and potent antagonist of the bradykinin B2 receptor has recently been discovered (HOE 140: D-Arg-[Hyp3,Thi5,D-Tic7,Oic8]bradykinin). The purpose of this study was to evaluate the potency of this compound in isolated human tissue (bronchus, pulmonary artery endothelium, umbilical artery and vein smooth muscle). Bradykinin induced contractions of the isolated human bronchus and umbilical artery and vein (the umbilical vessels were pretreated with indomethacin and L-nitro-arginine to inhibit prostaglandin and nitric oxide synthesis). It provoked an endothelium-dependent relaxation in the human pulmonary artery. HOE 140 was a non-competitive antagonist in human bronchial tissue (pKB: 8.19 +/- 0.30) and a competitive one in vascular tissue (pA2: 7.97 +/- 0.12, 8.16 +/- 0.16 and 8.00 +/- 0.11 in human pulmonary artery, umbilical artery and vein respectively). The effect of HOE 140 was selective as it did not influence the umbilical vein contractile response to serotonin and histamine. HOE 140 up to 3 x 10(-6) M was devoid of residual agonistic activity in the various human preparations studied. Furthermore, although the effects of HOE 140 were fully reversible, in isolated bronchial airways and umbilical veins, HOE 140 (10(-6) M) still possessed activity 1 h after being washed out in both tissues. Our results indicate that HOE 140 is a potent and potentially long-acting antagonist of the human bradykinin B2 receptor.

Published
1995
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2. Venous and arterial endothelial cells respond differently to thrombin and its endogenous receptor agonist.

Author

Simonet S, Bonhomme E, Laubie M, Thurieau C, Fauchère JL, and Verbeuren TJ

Subjects
Amino Acid Sequence, Animals, Coronary Vessels drug effects, Coronary Vessels physiology, Dogs, Endothelins pharmacology, Endothelium, Vascular physiology, Molecular Sequence Data, Receptors, Cell Surface drug effects, Receptors, Cell Surface metabolism, Receptors, Thrombin, Saphenous Vein drug effects, Saphenous Vein physiology, Vasoconstriction drug effects, Vasodilation drug effects, Endothelium, Vascular drug effects, Muscle Contraction drug effects, Peptide Fragments pharmacology, Peptides pharmacology, Thrombin pharmacology
Abstract

The effects of thrombin and a peptide mimicking the amino terminus of its receptor, Res (42-55), on vascular reactivity were compared in isolated canine blood vessels. In saphenous veins contracted with endothelin-1, both thrombin and Res (42-55) caused relaxation in rings with endothelium and contraction in rings without endothelium. In coronary arteries, thrombin caused similar responses while Res (42-55) only caused contraction. These data suggest that different thrombin receptors are present on venous and arterial endothelial cells.

Published
1992
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