Autoradiographic localization of endothelin-1 binding sites in the cardiovascular and respiratory systems

Journal Article · Sat Dec 31 23:00:00 EST 1988 · J. Cardiovasc. Pharmacol.; (United States)

DOI:https://doi.org/10.1097/00005344-198900135-00013· OSTI ID:5822929

Power, R F; Wharton, J; Zhao, Y; Bloom, S R; Polak, J M

Specific high-affinity binding sites for endothelin-1 (ET-1) have been demonstrated in peripheral tissues using the technique of in vitro receptor autoradiography. Binding was time dependent and saturable and inhibited by coincubation with an excess of unlabeled ET-1 but resistant to dissociation. Binding sites were localized to blood vessels of all sizes including coronary arteries, intrapulmonary vessels, and intrarenal and intrasplenic arteries. In addition, high-affinity binding sites were identified on airway smooth muscle, over alveolar septa, and on nerve trunks. Scatchard analysis of the data revealed a Bmax of 250 amol/mm2 and a Kd of 0.1 nM for the binding of rat tracheal smooth muscle, with similar values for porcine coronary artery. The localization of binding sites is consistent with the known effects of ET-1 and suggests a direct action on specific receptors.

• Research Organization: Hammersmith Hospital, London (England)
• OSTI ID: 5822929
• Journal Information: J. Cardiovasc. Pharmacol.; (United States), Journal Name: J. Cardiovasc. Pharmacol.; (United States) Vol. 13 Suppl 5; ISSN JCPCD
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ANIMALS
AUTORADIOGRAPHY
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL LOCALIZATION
BLOOD VESSELS
BODY
CARDIOVASCULAR AGENTS
CARDIOVASCULAR SYSTEM
DOMESTIC ANIMALS
DRUGS
GUINEA PIGS
IODINE ISOTOPES
ISOTOPES
KINETICS
MAMMALS
MAN
MEMBRANE PROTEINS
MUSCLES
ORGANIC COMPOUNDS
ORGANS
PEPTIDES
PRIMATES
PROTEINS
RATS
REACTION KINETICS
RECEPTORS
RODENTS
SPECIFICITY
SWINE
TIME DEPENDENCE
VASODILATORS
VERTEBRATES