Studies of the voltage-sensitive calcium channels in smooth muscle, neuronal, and cardiac tissues using 1,4-dihydropyridine calcium channel antagonists and activators

Thesis/Dissertation · Fri Jan 01 00:00:00 EST 1988

OSTI ID:6983883

Wei, X

This study describes the investigation of the voltage-sensitive Ca{sup +} channels in vascular and intestinal smooth muscle, chick neural retina cells and neonatal rat cardiac myocytes using 1,4-dihydropyridine Ca{sup 2+} channel antagonists and activators. In rat aorta, the tumor promoting phorbol ester, 12-O-tetradecanoylphorbol-13-acetate (TPA) produced Ca{sup 2+}-dependent contractile responses. The responses to TPA were blocked by the Ca{sup 2+} channel antagonists. The effects of the enantiomers of Bay K 8644 and 202-791 were characterized in both rat tail artery and guinea pig ileal longitudinal smooth muscle preparations using pharmacologic and radioligand binding assays. The (S)-enantiomers induced contraction and potentiated the responses to K{sup +} depolarization. The (R)-enantiomers inhibited the tension responses to K{sup +}. All the enantiomers inhibited specific ({sup 3}H)nitrendipine binding. The pharmacologic activities of both activator and antagonist ligands correlated on a 1:1 basis with the binding affinities. In chick neural retina cells the (S)-enantiomers of Bay K 8644 and 202-791 enhanced Ca{sup 2+} influx. In contrast, the (R)-enantiomers inhibited Ca{sup 2+} influx. The enantiomers of Bay K 8644 and 202-791 inhibited specific ({sup 3}H)PN 200-110 binding competitively. Binding of 1,4-dihydropyridines was characterized in neonatal rat heart cells.

• Research Organization: State Univ. of New York, Buffalo, NY (USA)
• OSTI ID: 6983883
• Resource Relation: Other Information: Thesis (Ph. D.)
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
PHORBOL ESTERS
BIOLOGICAL EFFECTS
PHOSPHOTRANSFERASES
ENZYME ACTIVITY
PYRIDINES
BIOCHEMICAL REACTION KINETICS
AORTA
CALCIUM COMPOUNDS
CHICKENS
GUINEA PIGS
HEART
MUSCLES
NEONATES
NERVE CELLS
RADIOASSAY
RATS
RETINA
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ALKALINE EARTH METAL COMPOUNDS
ANIMAL CELLS
ANIMALS
ARTERIES
AZINES
BIRDS
BLOOD VESSELS
BODY
BODY AREAS
CARCINOGENS
CARDIOVASCULAR SYSTEM
ENZYMES
ESTERS
EYES
FACE
FOWL
HEAD
HETEROCYCLIC COMPOUNDS
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
MAMMALS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PHOSPHORUS-GROUP TRANSFERASES
REACTION KINETICS
RODENTS
SENSE ORGANS
SOMATIC CELLS
TRANSFERASES
VERTEBRATES
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