Abstract
We have studied voltage-dependent calcium channels in the A7r5 smooth muscle cell line by measuring the high-affinity binding of radiolabelled dihydropyridines (DHPs), whole-cell and single-channel currents in patch-clamped cells, as well as cytosolic calcium ([Ca2+]i) in fura-2-loaded cell suspensions and monolayers. Intact A7r5 cells express saturable, high-affinity, voltage-sensitive DHP binding sites with pharmacological properties characteristic of L-type calcium channels. When cells were voltage clamped in the whole-cell configuration with near normal intra- and extracellular solutions, a DHP-sensitive inward current resembling the L-type calcium current was dominant. With barium (10 mM) as the charge carrier, peak inward currents were typically recorded at test potentials between 0 and +20 mV. Currents were blocked by extracellular cadmium with a half-maximal inhibitory concentration of approximately 1 microM. Isoproterenol (1 microM) or forskolin (10 microM) increased currents in approximately half of the cells tested. Forskolin (10 microM) increased single-channel activity in five of eight cell-attached patches. After cells had been quiescent for several weeks, cell suspensions showed changes in resting [Ca2+]i in response to DHPs and increased potassium. Most confluent monolayers of cells showed spontaneous transient elevations in [Ca2+]i. Bath application of Bay K 8644 increased the frequency and magnitude of these [Ca2+]i transients, whereas nifedipine abolished the transients. These data suggest that the [Ca2+]i transients were due to synchronous action potentials in electrically coupled cell monolayers.
MeSH Terms
3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester/pharmacology
Animals
Aorta
Biological Transport/drug effects,physiology
Calcium/analysis,metabolism,pharmacokinetics
Calcium Channels/drug effects,physiology
Cell Line
Colforsin/pharmacology
Cytosol/chemistry,metabolism
Dihydropyridines/metabolism,pharmacology
Electric Conductivity/drug effects,physiology
Fluorescence
Isoproterenol/pharmacology
Ligands
Muscle, Smooth, Vascular/cytology,metabolism,physiology
Nifedipine/pharmacology
Potassium/pharmacology
Chemicals
Calcium Channels
Dihydropyridines
Ligands
Colforsin
3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
1,4-dihydropyridine
Nifedipine
Isoproterenol
Potassium
Calcium
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Marks T N
Department of Physiology and Biophysics, Case Western Reserve University, Cleveland, OH 44106.
Dubyak G R
Jones S W
References (31)
31 references, click to expand
-
Depolarization-dependent binding of the calcium channel antagonist, (+)-[3H]PN200-110, to intact cultured PC12 cells.
J Pharmacol Exp Ther. 1986 Sep;238(3):1021-7
PMID: 2427685
-
Statistical estimations in enzyme kinetics.
Biochem J. 1961 Aug;80:324-32
PMID: 13785321
-
Beta-adrenergic increase in the calcium conductance of cardiac myocytes studied with the patch clamp.
Pflugers Arch. 1984 Jun;401(2):111-8
PMID: 6089094
-
Noradrenaline modulation of calcium channels in single smooth muscle cells from rabbit ear artery.
J Physiol. 1988 Oct;404:767-84
PMID: 2855354
-
Injection of subunits of cyclic AMP-dependent protein kinase into cardiac myocytes modulates Ca2+ current.
Nature. 1982 Aug 5;298(5874):576-8
PMID: 6285199
-
Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state.
Proc Natl Acad Sci U S A. 1984 Oct;81(20):6388-92
PMID: 6093100
-
Density-dependent hyperpolarization in cultured aortic smooth muscle cells.
Am J Physiol. 1989 Mar;256(3 Pt 1):C644-51
PMID: 2923198
-
Characterization of two putative smooth muscle cell lines from rat thoracic aorta.
Exp Cell Res. 1976 Mar 15;98(2):349-66
PMID: 943301
-
Regulation of calcium channels in aortic muscle cells by protein kinase C activators (diacylglycerol and phorbol esters) and by peptides (vasopressin and bombesin) that stimulate phosphoinositide breakdown.
J Biol Chem. 1987 May 25;262(15):6947-50
PMID: 2438272
-
Repetitive transient rises in cytoplasmic free calcium in hormone-stimulated hepatocytes.
Nature. 1986 Feb 13-19;319(6054):600-2
PMID: 3945348
-
Studies on Ca channels in intact cardiac cells: voltage-dependent effects and cooperative interactions of dihydropyridine enantiomers.
Mol Pharmacol. 1986 Dec;30(6):571-84
PMID: 2431263
-
Opposing effects of noradrenaline on the two classes of voltage-dependent calcium channels of single vascular smooth muscle cells in short-term primary culture.
Pflugers Arch. 1987 Nov;410(4-5):557-9
PMID: 2448744
-
Noradrenaline contracts arteries by activating voltage-dependent calcium channels.
Nature. 1988 Nov 24;336(6197):382-5
PMID: 2848201
-
The effects of isoproterenol on intracellular calcium concentration.
J Biol Chem. 1988 Jan 15;263(2):762-8
PMID: 3335525
-
Electrophysiology of smooth muscle.
Physiol Rev. 1963 Jul;43:482-527
PMID: 14017173
-
Effects of PDGF on inositol phosphates, Ca2+, and contraction of mesangial cells.
Am J Physiol. 1987 Sep;253(3 Pt 2):F458-63
PMID: 3631281
-
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.
Biochem Pharmacol. 1973 Dec 1;22(23):3099-108
PMID: 4202581
-
On the mechanism of beta-adrenergic regulation of the Ca channel in the guinea-pig heart.
Pflugers Arch. 1985 Oct;405(3):285-93
PMID: 2415919
-
Voltage-dependent block of calcium channel current in the calf cardiac Purkinje fiber by dihydropyridine calcium channel antagonists.
Circ Res. 1984 Sep;55(3):336-48
PMID: 6088117
-
Nimodipine block of calcium channels in rat vascular smooth muscle cell lines. Exceptionally high-affinity binding in A7r5 and A10 cells.
J Gen Physiol. 1989 Oct;94(4):669-92
PMID: 2559139
-
Phorbol ester-stimulated bidirectional transmembrane calcium flux in A7r5 vascular smooth muscle cells.
Mol Pharmacol. 1987 Jul;32(1):37-42
PMID: 2439892
-
A novel high affinity class of Ca2+ channel blockers.
Mol Pharmacol. 1988 Apr;33(4):363-9
PMID: 2965787
-
Oscillations of cytosolic Ca2+ in pituitary cells due to action potentials.
Nature. 1987 Oct 22-28;329(6141):719-21
PMID: 2444888
-
Dihydropyridine binding and calcium channel function in clonal rat adrenal medullary tumor cells.
Mol Pharmacol. 1987 Apr;31(4):401-9
PMID: 2437436
-
Effect of adrenergic agonists on Ca2+-channel currents in single vascular smooth muscle cells.
Pflugers Arch. 1987 Jun;409(1-2):7-12
PMID: 2441356
-
Prolonged depolarization increases the pharmacological effect of dihydropyridines and their binding affinity for calcium channels of vascular smooth muscle.
J Pharmacol Exp Ther. 1987 Nov;243(2):711-5
PMID: 2824756
-
Dihydropyridine receptors in muscle are voltage-dependent but most are not functional calcium channels.
Nature. 1985 Apr 25-May 1;314(6013):747-51
PMID: 2581141
-
A smooth muscle cell line suitable for the study of voltage sensitive calcium channels.
Biochem Biophys Res Commun. 1985 Jul 16;130(1):447-53
PMID: 2411261
-
Phorbol ester increases the dihydropyridine-sensitive calcium conductance in a vascular smooth muscle cell line.
Circ Res. 1988 May;62(5):1049-54
PMID: 2452033
-
Calcium channel current and its sensitivity to (+) isradipine in cultured pregnant rat myometrial cells. An electrophysiological and a binding study.
Pflugers Arch. 1989 Aug;414(4):477-83
PMID: 2552399
-
Vasopressin modulates the spontaneous electrical activity in aortic cells (line A7r5) by acting on three different types of ionic channels.
Proc Natl Acad Sci U S A. 1988 Dec;85(23):9365-9
PMID: 2461570