Interaction of SR 33557 with skeletal muscle calcium channel blocker receptors in the baboon: characterization of its binding sites

Journal Article · Wed May 01 00:00:00 EDT 1991 · Journal of Pharmacology and Experimental Therapeutics; (USA)

OSTI ID:5760590

Sol-Rolland, J; Joseph, M; Rinaldi-Carmona, M ^[1]

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1. 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), Vol. 257:2; ISSN 0022-3565
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
PORINS
RECEPTORS
CHEMICAL COMPOSITION
AFFINITY
ATP
ATP-ASE
BABOONS
BIOCHEMICAL REACTION KINETICS
CELL MEMBRANES
LIGANDS
MICROSOMES
MUSCLES
RADIOASSAY
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ACID ANHYDRASES
ANIMALS
CELL CONSTITUENTS
ENZYMES
HYDROGEN COMPOUNDS
HYDROLASES
ISOTOPE APPLICATIONS
KINETICS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
MONKEYS
NUCLEOTIDES
ORGANIC COMPOUNDS
PHOSPHOHYDROLASES
PRIMATES
PROTEINS
REACTION KINETICS
RIBOSOMES
VERTEBRATES
550201* - Biochemistry- Tracer Techniques