Regional vasodilation to endothelin-1 is mediated by a non-ETA receptor subtype in the anaesthetized rat: effect of BQ-123 on systemic haemodynamic responses. 1992

S A Douglas, and J D Elliott, and E H Ohlstein
Department of Cardiovascular Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939.

The sustained infusion of 75 nmol/kg per min BQ-123 selectively attenuates the systemic pressor responses to i.v. bolus endothelin-1 in the anaesthetized rat; the initial systemic vasodepression is only attenuated when a 10-fold higher dose of this ETA-selective antagonist is infused. These doses of BQ-123 do not antagonize the haemodynamic actions of angiotensin II or calcitonin gene-related peptide nor do they alter basal systemic haemodynamics. The secondary increase in carotid vascular resistance associated with the systemic pressor actions of endothelin-1 is selectively attenuated by the bolus i.v. administration of BQ-123 (1.6 mumol/kg); the maximum degree of the vasorelaxation that precedes this more sustained constriction is unaltered. Thus, the initial carotid vasodilation observed to endothelin-1, and the associated systemic vasodepression, is mediated by a non-ETA receptor subtype. Furthermore, subtle differences might exist between the receptors mediating mesenteric and carotid vasoconstriction since only the latter is sensitive to BQ-123.

UI MeSH Term Description Entries
D008297 Male Males
D010456 Peptides, Cyclic Peptides whose amino acid residues are linked together forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS; some are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL). Circular Peptide,Cyclic Peptide,Cyclic Peptides,Cyclopeptide,Orbitide,Circular Peptides,Cyclopeptides,Orbitides,Peptide, Circular,Peptide, Cyclic,Peptides, Circular
D006439 Hemodynamics The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM. Hemodynamic
D000758 Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D014664 Vasodilation The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE. Vasodilatation,Vasorelaxation,Vascular Endothelium-Dependent Relaxation,Endothelium-Dependent Relaxation, Vascular,Relaxation, Vascular Endothelium-Dependent,Vascular Endothelium Dependent Relaxation
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
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats
D017466 Receptors, Endothelin Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells. Endothelin Receptors,Receptors, Endothelium-Derived Vasoconstrictor Factor,Endothelin Receptor,Endothelium Derived Vasoconstrictor Factor Receptors,Receptors, Endothelins,Receptor, Endothelin,Receptors, Endothelium Derived Vasoconstrictor Factor
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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