Characteristics of the phenylalkylamine binding site in canine cardiac sarcolemmal preparations
Conference
·
· Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States)
OSTI ID:5497490
The phenylalkylamine binding site in canine cardiac sarcolemma was investigated using /sup 3/H(S)-desmethoxyverapamil (/sup 3/H(S)-D888) as labeled ligand. Radioligand binding experiments were carried out in a medium containing 1 mM EGTA and 10 mM Hepes-Na buffer, pH 7.4 at 20/sup 0/C. In 1 ml buffer, 75-100 ..mu..g protein were incubated for 1 hour and the bound /sup 3/H(S)-D888 was separated by rapid filtration through GF/C filters. A single high affinity binding site was identified for /sup 3/H(S)-D888 both by saturation and competition binding experiments. Several phenylalkylamine derivatives such as (-)D600, (+)D600, verapamil and (R)-D888 completely inhibited /sup 3/H(S)-D888 binding. The order of potency: (S)-D888 GAMMA (-)D600 > verapamil > (R)-D888 = (+)D600. In contrast to this, ronipamil produced only a 70% inhibition. /sup 3/H(S)-D888 binding was also inhibited by Ca/sup + +/ and by Mg/sup + +/. These data suggest the presence of a saturable, reversible and stereospecific phenylalkylamine binding site in canine cardiac sarcolemmal preparations which may be a receptor for the phenylalkylamine Ca/sup + +/ channel inhibitors.
- Research Organization:
- Univ. of Cincinnati College of Medicine, OH
- OSTI ID:
- 5497490
- Report Number(s):
- CONF-8604222-
- Conference Information:
- Journal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) Journal Volume: 45:3
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ALKALINE EARTH METAL COMPOUNDS
AMINES
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
CALCIUM COMPOUNDS
CARDIOVASCULAR SYSTEM
CATIONS
CHARGED PARTICLES
DOGS
FILTRATION
HEART
IONS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIGANDS
MAGNESIUM COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
ORGANIC COMPOUNDS
ORGANS
PROTEINS
REACTION KINETICS
RECEPTORS
SEPARATION PROCESSES
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ALKALINE EARTH METAL COMPOUNDS
AMINES
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
CALCIUM COMPOUNDS
CARDIOVASCULAR SYSTEM
CATIONS
CHARGED PARTICLES
DOGS
FILTRATION
HEART
IONS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIGANDS
MAGNESIUM COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
ORGANIC COMPOUNDS
ORGANS
PROTEINS
REACTION KINETICS
RECEPTORS
SEPARATION PROCESSES
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES