Binding of (/sup 3/H)isradipine (PN 200-110) on smooth muscle cell membranes from different bovine arteries

Journal Article · Fri Apr 01 00:00:00 EST 1988 · J. Cardiovasc. Pharmacol.; (United States)

DOI:https://doi.org/10.1097/00005344-198804000-00004· OSTI ID:6924683

Pinquier, J L; Urien, S; Chaumet-Riffaud, P; Comte, A; Tillement, J P

The binding of (/sup 3/H)isradipine ((/sup 3/H)PN 200-110), a new dihydropyridine (DHP) calcium blocker on smooth muscle cell (SMC) membranes from different bovine arteries was saturable with comparable high affinities but different binding site densities (Bmax). The data were fitted to a model that provided a common estimation for the dissociation constant (Kd = 0.46 nM, SD = 0.03) but different Bmax values. Two groups of arteries could be distinguished, large-sized with high Bmax (aorta, 149 fmol/mg, SD = 4; intrapulmonary, 134 fmol/mg, SD = 4) and medium-sized with lower Bmax (mesenteric, 67 fmol/mg, SD = 2; internal carotid, 50 fmol/mg, SD = 2; renal artery, 29 fmol/mg, SD = 2). The Kd values were similar to those previously reported, but the Bmax value on aorta SMC was higher than usually reported with other DHPs, showing that isradipine was a high full antagonist of calcium channel. Our results also suggest that the increase in arterial compliance induced by DHPs will probably be more important on large-sized arteries than on medium-sized arteries because of higher DHP binding.

• Research Organization: Universite Paris XII, Creteil (France)
• OSTI ID: 6924683
• Journal Information: J. Cardiovasc. Pharmacol.; (United States), Vol. 11:4
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
ANTIHYPERTENSIVE AGENTS
BIOCHEMICAL REACTION KINETICS
RECEPTORS
PYRIDINES
AFFINITY
ARTERIES
CATTLE
CELL MEMBRANES
IN VITRO
MATHEMATICAL MODELS
MUSCLES
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMALS
AZINES
BLOOD VESSELS
BODY
CARDIOVASCULAR AGENTS
CARDIOVASCULAR SYSTEM
CELL CONSTITUENTS
DOMESTIC ANIMALS
DRUGS
HETEROCYCLIC COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PROTEINS
REACTION KINETICS
RUMINANTS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques