Ca2+Channel Antagonists and Agonists

Specific Pharmacology of Calcium in Myocardium, Cardiac Pacemakers, and Vascular Smooth Muscle

1977 • 1,745 citations

Primary structure of the receptor for calcium channel blockers from skeletal muscle

1987 • 1,359 citations

Calcium Channel

1981 • 1,184 citations

Novel dihydropyridines with positive inotropic action through activation of Ca2+ channels

1983 • 1,010 citations

Regulation and modulation of calcium channels in cardiac, skeletal, and smooth muscle cells

1994 • 998 citations

P-type calcium channels blocked by the spider toxin ω-Aga-IVA

1992 • 877 citations

Mechanism of calcium channel blockade by verapamil, D600, diltiazem and nitrendipine in single dialysed heart cells

1983 • 869 citations

Mechanism of ion permeation through calcium channels

1984 • 850 citations

Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state.

1984 • 834 citations

Peptide Neurotoxins from Fish-Hunting Cone Snails

1985 • 742 citations

CALCIUM CHANNEL DIVERSITY AND NEUROTRANSMITTER RELEASE: The ω-Conotoxins and ω-Agatoxins

1994 • 734 citations

Calcium channel selectivity for divalent and monovalent cations. Voltage and concentration dependence of single channel current in ventricular heart cells.

1986 • 594 citations

Voltage-dependent block of calcium channel current in the calf cardiac Purkinje fiber by dihydropyridine calcium channel antagonists.

1984 • 553 citations

Blockade of current through single calcium channels by Cd2+, Mg2+, and Ca2+. Voltage and concentration dependence of calcium entry into the pore.

1986 • 549 citations

Mechanisms of calcium channel modulation by β-adrenergic agents and dihydropyridine calcium agonists

1986 • 493 citations

Purification of the calcium antagonist receptor of the voltage-sensitive calcium channel from skeletal muscle transverse tubules

1984 • 469 citations

All ErbB Receptors Other Than the Epidermal Growth Factor Receptor Are Endocytosis Impaired

1996 • 452 citations

Amiloride Selectively Blocks the Low Threshold (T) Calcium Channel

1988 • 395 citations

MOLECULAR DETERMINANTS OF DRUG BINDING AND ACTION ON L-TYPE CALCIUM CHANNELS

1997 • 385 citations

Receptor sites for Ca2+ channel antagonists

1992 • 382 citations

Mechanism of Block and Identification of the Verapamil Binding Domain to HERG Potassium Channels

1999 • 359 citations

Dihydropyridine‐sensitive low‐threshold calcium channels in isolated rat hypothalamic neurones.

1989 • 357 citations

Distribution and functional significance of the P-type, voltage-dependent Ca2+ channels in the mammalian central nervous system

1992 • 335 citations

Dihydropyridine derivatives prolong the open state of Ca channels in cultured cardiac cells.

1984 • 323 citations

History of calcium antagonists.

1983 • 318 citations

Calcium channels: direct identification with radioligand binding studies

1982 • 302 citations

Localization of P-type calcium channels in the central nervous system.

1991 • 297 citations

Does the organic calcium channel blocker D600 act from inside or outside on the cardiac cell membrane?

1982 • 254 citations

Calciseptine, a peptide isolated from black mamba venom, is a specific blocker of the L-type calcium channel.

1991 • 226 citations

Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967).

1995 • 224 citations

Frequency and voltage-dependent inhibition of type IIA Na+ channels, expressed in a mammalian cell line, by local anesthetic, antiarrhythmic, and anticonvulsant drugs.

1991 • 222 citations

Studies on Ca channels in intact cardiac cells: voltage-dependent effects and cooperative interactions of dihydropyridine enantiomers.

1986 • 217 citations

Alternatively Spliced IS6 Segments of the α _1C Gene Determine the Tissue-Specific Dihydropyridine Sensitivity of Cardiac and Vascular Smooth Muscle L-Type Ca ²⁺ Channels

1997 • 215 citations

Inhibition of T-type voltage-gated calcium channels by a new scorpion toxin

1998 • 199 citations

Control of the light-regulated current in rod photoreceptors by cyclic GMP, calcium, and l-cis-diltiazem.

1986 • 180 citations

Molecular localization of ion selectivity sites within the pore of a human L-type cardiac calcium channel

1993 • 173 citations

Identification of a phenylalkylamine binding region within the alpha 1 subunit of skeletal muscle Ca2+ channels.

1990 • 171 citations

Calcicludine, a venom peptide of the Kunitz-type protease inhibitor family, is a potent blocker of high-threshold Ca2+ channels with a high affinity for L-type channels in cerebellar granule neurons.

1994 • 162 citations

Interaction of tetrandrine with slowly inactivating calcium channels. Characterization of calcium channel modulation by an alkaloid of Chinese medicinal herb origin.

1988 • 153 citations

Transfer of 1,4-Dihydropyridine Sensitivity from L-Type to Class A (BI) Calcium Channels

1996 • 151 citations

HERG and KvLQT1/IsK, the cardiac K+ channels involved in long QT syndromes, are targets for calcium channel blockers.

1998 • 149 citations

Block of the cyclic GMP-gated channel of vertebrate rod and cone photoreceptors by l-cis-diltiazem.

1992 • 149 citations

Identification of 1,4-dihydropyridine binding regions within the alpha 1 subunit of skeletal muscle Ca2+ channels by photoaffinity labeling with diazipine.

1991 • 144 citations

Dihydropyridine receptor of L-type Ca2+ channels: identification of binding domains for [3H](+)-PN200-110 and [3H]azidopine within the alpha 1 subunit.

1991 • 144 citations

Three-dimensional Structure in Solution of the Calcium Channel Blocker ω-Conotoxin

1993 • 138 citations

A dihydropyridine (Bay k 8644) that enhances calcium currents in guinea pig and calf myocardial cells. A new type of positive inotropic agent.

1985 • 137 citations

Cannabinoid Inhibition of Adenylate Cyclase-mediated Signal Transduction and Interleukin 2 (IL-2) Expression in the Murine T-cell Line, EL4.IL-2

1996 • 136 citations

Molecular Determinants of High Affinity Phenylalkylamine Block of L-type Calcium Channels

1995 • 136 citations

Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker

1997 • 132 citations

Subunit-dependent modulation of recombinant L-type calcium channels. Molecular basis for dihydropyridine tissue selectivity.

1993 • 128 citations

Low‐voltage‐activated calcium current in rat aorta smooth muscle cells in primary culture.

1989 • 126 citations

Ca2+ channel antagonists and neuroprotection from cerebral ischemia

1998 • 123 citations

The IVS6 segment of the L-type calcium channel is critical for the action of dihydropyridines and phenylalkylamines.

1996 • 122 citations

Effect of cilnidipine, a novel dihydropyridine Ca++-channel antagonist, on N-type Ca++ channel in rat dorsal root ganglion neurons.

1997 • 121 citations

Calcium channels and calcium channel drugs: recent biochemical and biophysical findings.

1985 • 120 citations

Molecular Determinants of High Affinity Dihydropyridine Binding in L-type Calcium Channels

1996 • 118 citations

Comparison of location and binding for the positively charged 1,4-dihydropyridine calcium channel antagonist amlodipine with uncharged drugs of this class in cardiac membranes.

1989 • 117 citations

The calcium channel blocker nitrendipine blocks sodium channels in neonatal rat cardiac myocytes.

1985 • 116 citations

Molecular Determinants of High Affinity Phenylalkylamine Block of l-type Calcium Channels in Transmembrane Segment IIIS6 and the Pore Region of the α1Subunit

1997 • 115 citations

Identification of the site of interaction of the dihydropyridine channel blockers nitrendipine and azidopine with the calcium-channel alpha 1 subunit.

1991 • 112 citations

Block of L-type calcium channels by charged dihydropyridines. Sensitivity to side of application and calcium.

1991 • 110 citations

Solution structure of .omega.-conotoxin GVIA using 2-D NMR spectroscopy and relaxation matrix analysis

1993 • 107 citations

Permeation and interaction of divalent cations in calcium channels of snail neurons.

1985 • 104 citations

Pharmacological, radioligand binding, and electrophysiological characteristics of FPL 64176, a novel nondihydropyridine Ca2+ channel activator, in cardiac and vascular preparations.

1991 • 103 citations

Binding of Ca2+ entry blockers to cardiac sarcolemmal membrane vesicles. Characterization of diltiazem-binding sites and their interaction with dihydropyridine and aralkylamine receptors.

1986 • 102 citations

Blockade of N‐type Ca²⁺ current by cilnidipine (FRC‐8653) in acutely dissociated rat sympathetic neurones

1997 • 102 citations

Purification of the putative calcium channel from skeletal muscle with the aid of [3H]-nimodipine binding

1983 • 98 citations

Analysis of the Dihydropyridine Receptor Site ofl-type Calcium Channels by Alanine-scanning Mutagenesis

1997 • 98 citations

Structure and properties of omega-agatoxin IVB, a new antagonist of P-type calcium channels.

1993 • 97 citations

Die Bedeutung der energiereichen Phosphate für Kontraktilität und Tonus des Myokards

1964 • 96 citations

Temperature‐dependent regulation of d‐cis‐[³H]diltiazem binding to Ca²⁺ channels by 1,4‐dihydropyridine channel agonists and antagonists

1983 • 96 citations

Cat ventricular muscle treated with D600: characteristics of calcium channel block and unblock.

1984 • 95 citations

A molluskivorous Conus toxin: conserved frameworks in conotoxins

1989 • 95 citations

Influence of pHo on calcium channel block by amlodipine, a charged dihydropyridine compound. Implications for location of the dihydropyridine receptor.

1989 • 94 citations

Molecular Pharmacology of Voltage-Dependent Calcium Channels

1996 • 93 citations

(-)-[3H] desmethoxyverapamil labels multiple calcium channel modulator receptors in brain and skeletal muscle membranes: differentiation by temperature and dihydropyridines.

1986 • 92 citations

Transfer of High Sensitivity for Benzothiazepines from L-type to Class A (BI) Calcium Channels

1996 • 91 citations

Stereoselective photoaffinity labelling of the purified 1,4‐dihydropyridine receptor of the voltage‐dependent calcium channel

1986 • 90 citations

Photoaffinity labelling of Ca²⁺ channels with [³H]azidopine

1984 • 90 citations

The pharmacology of ion channels: with particular reference to voltage-gated Ca2+ channels

1999 • 88 citations

Tetrandrine: A new ligand to block voltage-dependent Ca2+ and Ca2+-activated K+ channels

1994 • 87 citations

Construction of a high-affinity receptor site for dihydropyridine agonists and antagonists by single amino acid substitutions in a non- <scp>l</scp> -type Ca ²⁺ channel

1997 • 87 citations

Dihydropyridines, phenylalkylamines and benzothiazepines block N-, P/Q- and R-type calcium currents

1995 • 86 citations

Calcium Binding in the Pore of L-type Calcium Channels Modulates High Affinity Dihydropyridine Binding

1995 • 82 citations

Molecular mechanism of use-dependent calcium channel block by phenylalkylamines: Role of inactivation

1997 • 82 citations

Two Amino Acid Residues in the IIIS5 Segment of L-Type Calcium Channels Differentially Contribute to 1,4-Dihydropyridine Sensitivity

1996 • 81 citations

The action of calcium channel blockers on recombinant L‐type calcium channel α₁‐subunits

1998 • 77 citations

Ca²⁺ channel sensitivity towards the blocker isradipine is affected by alternative splicing of the human α_1C subunit gene

1998 • 76 citations

Motif III S5 of L-type Calcium Channels Is Involved in the Dihydropyridine Binding Site

1997 • 75 citations

Antagonism of synaptosomal calcium channels by subtypes of omega-agatoxins.

1992 • 74 citations

Ca2+ channel block and inactivation: common molecular determinants

1998 • 73 citations

Nine L-type Amino Acid Residues Confer Full 1,4-Dihydropyridine Sensitivity to the Neuronal Calcium Channel α1ASubunit

1997 • 72 citations

Three-dimensional Solution Structure of the Calcium Channel Antagonist ω-Agatoxin IVA: Consensus Molecular Folding of Calcium Channel Blockers

1995 • 68 citations

Cloning and Functional Expression of a Voltage-gated Calcium Channel α1 Subunit from Jellyfish

1998 • 66 citations

NMR and Restrained Molecular Dynamics Study of the Three-Dimensional Solution Structure of Toxin FS2, a Specific Blocker of the L-Type Calcium Channel, Isolated from Black Mamba Venom

1995 • 64 citations

Voltage and pH dependent block of cloned N‐type Ca²⁺ channels by amlodipine

1997 • 64 citations

Application of Physiologically Active Substances Isolated from Natural Resources to Pharmacological Studies.

1997 • 63 citations

Transfer of the High Affinity Dihydropyridine Sensitivity from L-Type To Non-L-Type Calcium Channel

1997 • 61 citations

Inhibitory Effect of Cilnidipine on Vascular Sympathetic Neurotransmission and Subsequent Vasoconstriction in Spontaneously Hypertensive Rats

1995 • 61 citations

Prolongation of calcium channel open time by the dihydropyridine derivative BAY K 8644 in cardiac myocytes.

1984 • 58 citations

A new site for the activation of cardiac calcium channels defined by the nondihydropyridine FPL 64176.

1991 • 53 citations

Pharmacology of bepridil

1992 • 52 citations

Transfer of L-type Calcium Channel IVS6 Segment Increases Phenylalkylamine Sensitivity of α1A

1996 • 51 citations

Distinct effects of mutations in transmembrane segment IVS6 on block of L-type calcium channels by structurally similar phenylalkylamines.

1996 • 51 citations

Identification of 1,4‐dihydropyridine binding domains within the primary structure of the α₁ subunit of the skeletal muscle L‐type calcium channel

1993 • 50 citations

Coordination of Ca2+ by the Pore Region Glutamates Is Essential for High-Affinity Dihydropyridine Binding to the Cardiac Ca2+ Channel a1 Subunit

1995 • 48 citations

Extracellular localization of the benzothiazepine binding domain of L-type Ca2+ channels.

1993 • 48 citations

Characterization of the effects of a new Ca2+ channel activator, FPL 64176, in GH3 cells.

1992 • 47 citations

Inhibition of Signal Ca2+ in Dog Coronary Arterial Vascular Muscle Cells by Ro 40–5967

1994 • 47 citations

Isoform-specific inhibition of L-type calcium channels by dihydropyridines is independent of isoform-specific gating properties.

1998 • 47 citations

Cyclic-AMP-dependent phosphorylation modulates the stereospecific activation of cardiac Ca channels by Bay K 8644

1990 • 46 citations

A unique fluorescent phenylalkylamine probe for L-type Ca2+ channels. Coupling of phenylalkylamine receptors to Ca2+ and dihydropyridine binding sites.

1992 • 45 citations

Azidobutyryl clentiazem, a new photoactivatable diltiazem analog, labels benzothiazepine binding sites in the α₁ subunit of the skeletal muscle calcium channel

1993 • 45 citations

Functional importance of the dihydropyridine‐sensitive, yet voltage‐insensitive store‐operated Ca²⁺ influx of U937 cells

1996 • 45 citations

Tetrandrine, a Ca++ antagonist: effects and mechanisms of action in vascular smooth muscle cells.

1995 • 45 citations

Benzazepinone calcium channel blockers. 4. Structure-activity overview and intracellular binding site

1992 • 44 citations

Bay K 8644 Increases Resting Ca ²⁺ Spark Frequency in Ferret Ventricular Myocytes Independent of Ca Influx

1998 • 44 citations

Inhibition of Recombinant Ca²⁺Channels by Benzothiazepines and Phenylalkylamines: Class-Specific Pharmacology and Underlying Molecular Determinants

1997 • 44 citations

L-type calcium channels: asymmetrical intramembrane binding domain revealed by variable length, permanently charged 1,4-dihydropyridines.

1994 • 44 citations

Voltage-and frequency-dependent block of diltiazem on the slow inward current and generation of tension in frog ventricular muscle

1983 • 43 citations

Dual action (stimulation, inhibition) of D600 on contractility and calcium channels in guinea‐pig and cat heart cells.

1989 • 43 citations

Effects of Ca2+ channel antagonists on sinus node: Prolongation of late phase 4 depolarization by efonidipine

1997 • 43 citations

Identification of Benz(othi)azepine-binding Regions within L-type Calcium Channel α1 Subunits

1996 • 43 citations

Photoaffinity labeling of the purified skeletal muscle calcium antagonist receptor by a novel benzothiazepine, [3H]azidobutyryl diltiazem

1989 • 41 citations

1,5-Benzothiazepine Binding Domain Is Located on the Extracellular Side of the Cardiac L-Type Ca²⁺ Channel

1997 • 40 citations

Effects of four diltiazem stereoisomers on binding of d-cis-[3H]diltiazem and (+)-[3H]PN200-110 to rabbit T-tubule calcium channels

1991 • 40 citations

Photoaffinity labelling of the cardiac calcium channel. (−)-[3H]azidopine labels a 165 kDa polypeptide, and evidence against a [3H]-1,4-dihydropyridine-isothiocyanate being a calcium-channel-specific affinity ligand

1987 • 38 citations

D 600 block of L-type Ca2+ channel in vascular smooth muscle cells: comparison with permanently charged derivative, D 890

1989 • 37 citations

Reversal of multidrug resistance by verapamil analogues

1995 • 37 citations

Dual effects of tetrandrine on cytosolic calcium in human leukaemic HL‐60 cells: intracellular calcium release and calcium entry blockade

1994 • 35 citations

Calciseptine Binding to a 1,4-Dihydropyridine Recognition Site of the L-Type Calcium Channel of Rat Synaptosomal Membranes

1993 • 34 citations

Flanking Proline Residues Identify the L-Type Ca²⁺ Channel Binding Site of Calciseptine and FS2

1998 • 34 citations

Effects of diltiazem on transmembrane potential and current of right ventricular papillary muscle of ferrets.

1984 • 33 citations

D600 blocks the Ca2+ channel from the outer surface of smooth muscle cell membrane of the rabbit intestine and portal vein

1987 • 33 citations

The reversal of doxorubicin resistance by verapamil is not due to an effect on calcium channels

1988 • 33 citations

Sequence Differences between α1C and α1S Ca2+ Channel Subunits Reveal Structural Determinants of a Guarded and Modulated Benzothiazepine Receptor

1999 • 32 citations

BAY K 8644 modifies Ca²⁺cross signaling between DHP and ryanodine receptors in rat ventricular myocytes

1999 • 30 citations

Evidence for an external location of the dihydropyridine agonist receptor site on smooth muscle and skeletal muscle calcium channels

1993 • 30 citations

Inhibitory effects of dihydropyridines on macroscopic K+ currents and on the large-conductance Ca2+-activated K+ channel in cultured cerebellar granule cells

1994 • 30 citations

Dihydropyridine Action on Voltage-dependent Potassium Channels Expressed in Xenopus Oocytes

1997 • 29 citations

New drug binding sites in Ca2+ channels

1995 • 29 citations

High affinity block of myocardial L-type calcium channels by the spider toxin omega-Aga-toxin IIIA: advantages over 1,4-dihydropyridines.

1992 • 29 citations

Effects of a novel, potent benzothiazepine Ca2+ channel antagonist, DTZ323, on guinea-pig ventricular myocytes

1997 • 28 citations

Increase in the slow inward current by intracellularly applied nifedipine and nicardipine in single ventricular cells of the guinea-pig heart

1984 • 28 citations

Calcium Channels in the Heart^a

1988 • 25 citations

Ionic mechanisms of tetrandrine in cultured rat aortic smooth muscle cells

1997 • 25 citations

Fast activation of cardiac Ca++ channel gating charge by the dihydropyridine agonist, BAY K 8644

1990 • 25 citations

The relationship between the binding site of [3H]-d-cis-diltiazem and that of other non-dihydropyridine calcium entry blockers in cardiac sarcolemma.

1987 • 24 citations

Quaternary Diltiazem Can Act from Both Sides of the Membrane in Ventricular Myocytes

1993 • 23 citations

The benzazepine/benzothiazepine binding domain of the cardiac L-type Ca2+ channel is accessible only from the extracellular side

1993 • 22 citations

Effects of calciseptine on unitary barium channel currents in guinea-pig portal vein

1996 • 20 citations

Functional interactions between two Ca2+ channel activators, (S)-Bay K 8644 and FPL 64176, in smooth muscle.

1992 • 20 citations

Mechanisms of Inhibition of Calmodulin‐Stimulated Cyclic Nucleotide Phosphodiesterase by Dihydropyridine Calcium Antagonists

1997 • 19 citations

Allosteric Interaction of Semotiadil Fumarate, a Novel Benzothiazine, with 1,4-Dihydropyridines, Phenylalkylamines, and 1,5-Benzothiazepines at the Ca2+-Channel Antagonist Binding Sites in Canine Skeletal Muscle Membranes

1994 • 18 citations

Inactivation determinant in the I‐II loop of the Ca²⁺ channel α₁‐subunit and β‐subunit interaction affect sensitivity for the phenylalkylamine (−)gallopamil

1999 • 18 citations

Effects of Tetrandrine on Ca2+- and Na+-Currents of Single Bullfrog Cardiomyocytes

1993 • 17 citations

Extra‐ and intracellular action of quaternary devapamil on muscle L‐type Ca²⁺‐channels

1996 • 17 citations

1-benzazepin-2-one calcium channel blockers—VI. Receptor-binding model and possible relationship to desmethoxyverapamil.

1993 • 16 citations

Differential potentiation by depolarization of the effects of calcium antagonists on contraction and Ca²⁺ current in guinea‐pig heart

1994 • 16 citations

Selectivity of the action of calcium channel blockers in recombinant L-type calcium channels

1998 • 15 citations

Inhibitory effects of a new neuroprotective diltiazem analogue, T-477, on cloned brain Ca2+ channels expressed in Xenopus oocytes

1997 • 15 citations

Photochemical Identification of Transmembrane Segment IVS6 as the Binding Region of Semotiadil, a New Modulator for the L-type Voltage-dependent Ca2+ Channel

1998 • 15 citations

Cardiovascular selectivity of 1,4-dihydropyridine derivatives, efonidipine (NZ-105), nicardipine and structure related compounds in isolated guinea-pig tissues

1995 • 12 citations

A method for estimation of drug affinity constants to the open conformational state of calcium channels

1992 • 12 citations

High-affinity binding of DTZ323, a novel derivative of diltiazem, to rabbit skeletal muscle L-type Ca++ channels.

1997 • 12 citations

Interaction of diltiazem with single L-type calcium channels in guinea-pig ventricular myocytes.

1992 • 11 citations

Protective effect of l-cis-diltiazem on hypercontracture of rat myocytes induced by veratridine

1996 • 10 citations

Diltiazem derivatives modulate the dihydropyridine-binding to intact rat ventricular myocytes

1997 • 10 citations

l-cis Diltiazem attenuates intracellular Ca2+ overload by metabolic inhibition in guinea pig myocytes

1999 • 10 citations

Functional interaction between benzothiazepine- and dihydropyridine binding sites of cardiac L-type Ca2+ channels

1998 • 9 citations

Effects of clentiazem on cerebral ischemia induced by carotid artery occlusion in stroke-prone spontaneously hypertensive rats.

1994 • 7 citations

The response of single cardiac sodium channels in neonatal rats to the dihydropyridines CGP 28392 and (?)-Bay K 8644

1989 • 5 citations

Treatment With 1-cis Diltiazem Before Reperfusion Reduces Infarct Size in the Ischemic Rabbit Heart In Vivo

1999 • 4 citations

Functional expression of a protochordate L-type Ca2+ channel

1999 • 3 citations

The voltage-dependent effect of 1,4-dihydropyridine enantiomers on Ca channels in cardiac cells.

1986 • 1 citations

The mechanism for the voltage-dependent block of diltiazem on L-type Ca2+ channels in guinea-pig ventricular myocytes.

1999 • 1 citations