Two bradykinin binding sites with picomolar affinities
Journal Article
·
· J. Pharmacol. Exp. Ther.; (United States)
OSTI ID:5429920
Bradykinin (BK) and related peptides exert a wide range of effects on several organ systems. We have attempted to sort out these effects by studying the binding interaction of (/sup 3/H)BK at the membrane level with in vitro receptor binding techniques. High specific activity (/sup 3/H)BK and an enzyme inhibitor cocktail has enabled us to label two BK binding sites with different affinity and peptide specificity in several guinea-pig tissues. In the guinea-pig ileum the high-affinity site has an equilibrium dissociation constant (Kd) for (/sup 3/H)BK of 13 pM and a maximal number of binding sites of 8.3 pmol/g of tissue wet weight. The low-affinity guinea-pig ileum site displays a Kd of 910 pM, a maximum number of binding sites of 14 pmol/g of tissue wet weight and shows a greater selectivity for BK analogs over Lysyl-BK analogs. Two similar sites can also be discriminated in kidney and heart. The potencies of a series of BK analogs at the high-affinity guinea-pig ileum site correlate well with their potencies in contracting ileal smooth muscle. The binding of (/sup 3/H)BK in the guinea-pig ileum is inhibited by physiological concentrations of monovalent and divalent cations.
- Research Organization:
- Johns Hopkins Univ., Baltimore, MD
- OSTI ID:
- 5429920
- Journal Information:
- J. Pharmacol. Exp. Ther.; (United States), Journal Name: J. Pharmacol. Exp. Ther.; (United States) Vol. 2; ISSN JPETA
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
BRADYKININ
CARDIOVASCULAR SYSTEM
CATIONS
CHARGED PARTICLES
DIGESTIVE SYSTEM
GASTROINTESTINAL TRACT
GUINEA PIGS
HEART
IN VITRO
INTESTINES
IONS
KIDNEYS
KINETICS
KININS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
ORGANIC COMPOUNDS
ORGANS
PEPTIDES
POLYPEPTIDES
PROTEINS
REACTION KINETICS
RECEPTORS
RODENTS
SMALL INTESTINE
TRITIUM COMPOUNDS
VALENCE
VERTEBRATES
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
BRADYKININ
CARDIOVASCULAR SYSTEM
CATIONS
CHARGED PARTICLES
DIGESTIVE SYSTEM
GASTROINTESTINAL TRACT
GUINEA PIGS
HEART
IN VITRO
INTESTINES
IONS
KIDNEYS
KINETICS
KININS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
ORGANIC COMPOUNDS
ORGANS
PEPTIDES
POLYPEPTIDES
PROTEINS
REACTION KINETICS
RECEPTORS
RODENTS
SMALL INTESTINE
TRITIUM COMPOUNDS
VALENCE
VERTEBRATES