Biomaterial Database

Effects of the endothelin (ET) receptor antagonist BQ 123 on initial and delayed vascular responses induced by ET-1 in conscious, normotensive rats. 1993

J E Bird, and T L Waldron, and C R Dorso, and M M Asaad

Department of Pharmacology, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543.

The ETA receptor antagonist, BQ 123 was used to characterize depressor and initial and delayed pressor responses to ET-1 in conscious rats. BQ 123 (0.001-0.01 mumol/kg/min) dose-dependently inhibited the initial ET-1 (0.1 nmol/kg) pressor response, reaching a maximum after 0.01 BQ 123 (61 +/- 4% inhibition). Less inhibition of the pressor effects occurred after higher doses of BQ 123 (1: 10 +/- 6% inhibition). The depressor response to 1 nmol/kg ET-1 was unchanged by BQ 123 (0.01), but inhibited by BQ 123 (1). The initial pressor response to 1.0 nmol/kg ET-1 was inhibited by BQ 123 (0.01: 26 +/- 6%; 1.0: 41 +/- 3% inhibition). The delayed pressor response, 180 min post-ET-1 (+41 +/- 2% increase) was reduced by BQ 123 infused before the delayed peak (+14 +/- 5% increase). Plasma immunoreactive ET values were: control: 5.4 +/- 0.4; initial peak: 491.4 +/- 50.6; delayed peak: 8.2 +/- 0.6 fmol/ml. The delayed ET-1 response does not coincide with sustained high circulating levels of immunoreactive ET, but inhibition of the response by BQ 123 suggests that it may involve endothelin receptors.

UI	MeSH Term	Description	Entries
D007262	Infusions, Intravenous	The long-term (minutes to hours) administration of a fluid into the vein through venipuncture, either by letting the fluid flow by gravity or by pumping it.	Drip Infusions,Intravenous Drip,Intravenous Infusions,Drip Infusion,Drip, Intravenous,Infusion, Drip,Infusion, Intravenous,Infusions, Drip,Intravenous Infusion
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
D012016	Reference Values	The range or frequency distribution of a measurement in a population (of organisms, organs or things) that has not been selected for the presence of disease or abnormality.	Normal Range,Normal Values,Reference Ranges,Normal Ranges,Normal Value,Range, Normal,Range, Reference,Ranges, Normal,Ranges, Reference,Reference Range,Reference Value,Value, Normal,Value, Reference,Values, Normal,Values, Reference
D001794	Blood Pressure	PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.	Systolic Pressure,Diastolic Pressure,Pulse Pressure,Pressure, Blood,Pressure, Diastolic,Pressure, Pulse,Pressure, Systolic,Pressures, Systolic
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
D013997	Time Factors	Elements of limited time intervals, contributing to particular results or situations.	Time Series,Factor, Time,Time Factor
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
D044022	Receptor, Endothelin A	A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.	Endothelin A Receptors,Endothelin Receptors Type A,Receptor, Endothelin-1,Endothelin A Receptor,Endothelin-1 Receptor,Receptor, Endothelin 1,Receptors, Endothelin A