Interaction of SR 33557 with skeletal muscle calcium channel blocker receptors in the baboon: characterization of its binding sites
Journal Article
·
· Journal of Pharmacology and Experimental Therapeutics; (USA)
OSTI ID:5760590
- Sanofi Recherche, Montpellier, (France)
A procedure for the isolation of primate skeletal microsomal membranes was initiated. Membranes exhibited specific enzymatic markers such as 5'-nucleotidase, Ca{sup 2}{sup +},Mg({sup 2}{sup +})-adenosine triphosphatase and an ATP-dependent calcium uptake. Baboon skeletal microsomes bound specifically with high-affinity potent Ca{sup 2}{sup +} channel blockers such as dihydropyridine, phenylalkylamine and benzothiazepine derivatives. Scatchard analysis of equilibrium binding assays with ({sup 3}H)(+)-PN 200-110, ({sup 3}H)(-)-desmethoxyverapamil (( {sup 3}H)(-)-D888) and ({sup 3}H)-d-cis-dilitiazem were consistent with a single class of binding sites for the three radioligands. The pharmacological profile of SR 33557, an original compound with calcium antagonist properties, was investigated using radioligand binding studies. SR 33557 totally inhibited the specific binding of the three main classes of Ca{sup 2}{sup +} channel effectors and interacted allosterically with them. In addition, SR 33557 bound with high affinity to a homogeneous population of binding sites in baboon skeletal muscle.
- OSTI ID:
- 5760590
- Journal Information:
- Journal of Pharmacology and Experimental Therapeutics; (USA), Journal Name: Journal of Pharmacology and Experimental Therapeutics; (USA) Vol. 257:2; ISSN 0022-3565; ISSN JPETA
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ACID ANHYDRASES
AFFINITY
ANIMALS
ATP
ATP-ASE
BABOONS
BIOCHEMICAL REACTION KINETICS
CELL CONSTITUENTS
CELL MEMBRANES
CHEMICAL COMPOSITION
ENZYMES
HYDROGEN COMPOUNDS
HYDROLASES
ISOTOPE APPLICATIONS
KINETICS
LIGANDS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
MICROSOMES
MONKEYS
MUSCLES
NUCLEOTIDES
ORGANIC COMPOUNDS
PHOSPHOHYDROLASES
PORINS
PRIMATES
PROTEINS
RADIOASSAY
REACTION KINETICS
RECEPTORS
RIBOSOMES
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES
59 BASIC BIOLOGICAL SCIENCES
ACID ANHYDRASES
AFFINITY
ANIMALS
ATP
ATP-ASE
BABOONS
BIOCHEMICAL REACTION KINETICS
CELL CONSTITUENTS
CELL MEMBRANES
CHEMICAL COMPOSITION
ENZYMES
HYDROGEN COMPOUNDS
HYDROLASES
ISOTOPE APPLICATIONS
KINETICS
LIGANDS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
MICROSOMES
MONKEYS
MUSCLES
NUCLEOTIDES
ORGANIC COMPOUNDS
PHOSPHOHYDROLASES
PORINS
PRIMATES
PROTEINS
RADIOASSAY
REACTION KINETICS
RECEPTORS
RIBOSOMES
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES