The Link between Drug Binding and Response: Theories and Observations

A quantitative description of membrane current and its application to conduction and excitation in nerve

1952 • 21,965 citations

THE ADSORPTION OF GASES ON PLANE SURFACES OF GLASS, MICA AND PLATINUM.

1918 • 20,900 citations

On the nature of allosteric transitions: A plausible model

1965 • 8,699 citations

Handbook of Psychopharmacology

1988 • 2,778 citations

Single-channel currents recorded from membrane of denervated frog muscle fibres

1976 • 2,456 citations

Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction.

1977 • 1,746 citations

A study of the ‘desensitization’ produced by acetylcholine at the motor end‐plate

1957 • 1,457 citations

An analysis of the end‐plate potential recorded with an intra‐cellular electrode

1951 • 1,389 citations

A MODIFICATION OF RECEPTOR THEORY

1956 • 1,126 citations

Handbook of Psychopharmacology

1978 • 1,034 citations

Voltage clamp analysis of acetylcholine produced end‐plate current fluctuations at frog neuromuscular junction

1973 • 992 citations

The statistical nature of the acetylcholine potential and its molecular components

1972 • 960 citations

Interaction of Tetraethylammonium Ion Derivatives with the Potassium Channels of Giant Axons

1971 • 930 citations

Handbuch der Experimentellen Pharmakologie

1939 • 889 citations

Local anaesthetics transiently block currents through single acetylcholine‐receptor channels.

1978 • 864 citations

TURNOVER OF TRANSMITTER AND SYNAPTIC VESICLES AT THE FROG NEUROMUSCULAR JUNCTION

1973 • 835 citations

The normal membrane potential of frog sartorius fibers

1949 • 741 citations

The Inhibition of Sodium Currents in Myelinated Nerve by Quaternary Derivatives of Lidocaine

1973 • 660 citations

Relaxation and fluctuations of membrane currents that flow through drug-operated channels

1977 • 630 citations

A quantitative description of end‐plate currents

1972 • 625 citations

The binding of acetylcholine to receptors and its removal from the synaptic cleft

1973 • 576 citations

Lectures on Biostatistics.

1972 • 551 citations

CONDUCTANCE FLUCTUATIONS AND IONIC PORES IN MEMBRANES

1977 • 510 citations

Chemistry and Pharmacology of Polypeptide Toxins in Snake Venoms

1972 • 479 citations

Interaction at end-plate receptors between different choline derivatives

1957 • 477 citations

Acetylcholine Receptors in Muscle Fibres

1971 • 443 citations

The effect of voltage on the time course of end‐plate currents

1972 • 443 citations

Transmitter leakage from motor nerve endings

1977 • 443 citations

ON THE COOPERATIVITY OF BIOLOGICAL MEMBRANES

1967 • 439 citations

On the permeability of end‐plate membrane during the action of transmitter

1960 • 430 citations

On the application of “a plausible model” of allosteric proteins to the receptor for acetylcholine

1967 • 425 citations

Kinetics and steady‐state properties of the charged system controlling sodium conductance in the squid giant axon

1974 • 420 citations

Lectures on biostatistics

1971 • 419 citations

Kinetics of the allosteric interactions of phosphofructokinase from Escherichia coli

1968 • 416 citations

Ionic channels in nerve membranes

1970 • 416 citations

The margin of safety of neuromuscular transmission

1967 • 409 citations

Discreteness of Conductance Change in Bimolecular Lipid Membranes in the Presence of Certain Antibiotics

1970 • 405 citations

Ion‐concentration dependence of the reversal potential and the single channel conductance of ion channels at the frog neuromuscular junction.

1979 • 394 citations

Ionic pores, gates, and gating currents

1974 • 358 citations

Drug blockade of open end‐plate channels.

1976 • 352 citations

ACTIVE PHASE OF FROG'S END-PLATE POTENTIAL

1959 • 348 citations

The uptake of atropine and related drugs by intestinal smooth muscle of the guinea-pig in relation to acetylcholine receptors

1965 • 342 citations

The Rate of Action of Drugs on Cells

1937 • 319 citations

Binding of α-Bungarotoxin to Acetylcholine Receptors In Mammalian Muscle

1972 • 286 citations

The mode of action of nicotine and curari, determined by the form of the contraction curve and the method of temperature coefficients

1909 • 278 citations

Inferences about Membrane Properties from Electrical Noise Measurements

1972 • 274 citations

The pH-dependent rate of action of local anesthetics on the node of Ranvier.

1977 • 274 citations

Post‐synaptic potentiation: interaction between quanta of acetylcholine at the skeletal neuromuscular synapse.

1975 • 259 citations

In Vitro excitation of purified membrane fragments by cholinergic agonists

1971 • 250 citations

On the mechanism of desensitization at cholinergic receptors.

1970 • 247 citations

Enzymes: Physical principles

1973 • 245 citations

Purification and Properties of the Cholinergic Receptor Protein from Electrophorus electricus Electric Tissue

1974 • 238 citations

Potassium and sodium ion current noise in the membrane of the squid giant axon.

1975 • 235 citations

The antagonism between tubocurarine and substances which depolarize the motor end‐plate

1960 • 235 citations

On the Mode of Action of Local Anesthetics

1966 • 234 citations

Voltage jump analysis of procaine action at frog end‐plate

1977 • 230 citations

Noise analysis of drug induced voltage clamp currents in denervated frog muscle fibres.

1976 • 226 citations

Membrane Noise produced by Acetylcholine

1970 • 220 citations

The electromotive action of acetylcholine at the motor end‐plate

1950 • 212 citations

The binding of labelled tetrodotoxin to non‐myelinated nerve fibres

1972 • 206 citations

Photochromic Activators of the Acetylcholine Receptor

1971 • 205 citations

Purification and molecular properties of the acetylcholine receptor from Torpedo electroplax

1973 • 201 citations

Acetylcholine receptors in normal and denervated rat diaphragm muscle. II. Comparison of junctional and extrajunctional receptors

1975 • 198 citations

THE BINDING OF NICOTINAMIDE-ADENINE DINUCLEOTIDE TO YEAST D-GLYCERALDEHYDE-3-PHOSPHATE DEHYDROGENASE: TEMPERATURE-JUMP RELAXATION STUDIES ON THE MECHANISM OF AN ALLOSTERIC ENZYME

1966 • 196 citations

A new method for labelling saxitoxin and its binding to non-myelinated fibres of the rabbit vagus, lobster walking leg, and garfish olfactory nerves.

1976 • 195 citations

The Relation between Classical and Cooperative Models for Drug Action

1973 • 194 citations

Enzymes: physical principles

1972 • 191 citations

Voltage dependence of agonist effectiveness at the frog neuromuscular junction: resolution of a paradox.

1975 • 190 citations

The action of tubocurarine and atropine on the normal and denervated rat diaphragm

1967 • 180 citations

A study of curare action with an electrical micro-method

1957 • 180 citations

Generation of end-plate potentials

1976 • 176 citations

Effects of membrane potential, temperature and neostigmine on the conductance change caused by a quantum or acetylcholine at the toad neuromuscular junction.

1975 • 172 citations

The characteristics of ‘end‐plate noise’ produced by different depolarizing drugs

1973 • 171 citations

Regulation of binding properties of the nicotinic receptor protein by cholinergic ligands in membrane fragments from Torpedo marmorata.

1975 • 169 citations

A quantitative analysis of local anaesthetic alteration of miniature end‐plate currents and end‐plate current fluctuations.

1977 • 169 citations

Decamethonium both opens and blocks endplate channels.

1978 • 168 citations

An upper limit to the number of sodium channels in nerve membrane?

1967 • 163 citations

An analysis of the dose‐response relationship at voltage‐clamped frog neuromuscular junctions.

1978 • 162 citations

On the excitability and cooperativity of the electroplax membrane.

1968 • 159 citations

Measurement of the conductance of the sodium channel from current fluctuations at the node of Ranvier.

1976 • 158 citations

Voltage-dependence of drug-induced conductance in frog neuromuscular junction.

1975 • 156 citations

Half-Site Reactivit

1974 • 153 citations

Acetylcholine receptors

1974 • 149 citations

Binding of Naja nigricollis (3H)alpha-toxin to membrane fragments from Electrophorus and Torpedo electric organs. II. Effect of cholinergic agonists and antagonists on the binding of the tritiated alpha-neurotoxin.

1974 • 148 citations

Determination of dose‐response curves by quantitative ionophoresis at the frog neuromuscular junction.

1978 • 147 citations

Rates and equilibria at the acetylcholine receptor of Electrophorus electroplaques: a study of neurally evoked postsynaptic currents and of voltage-jump relaxations.

1977 • 145 citations

Alteration by Xylocaine (Lidocaine) and Its Derivatives of the Time Course of the End Plate Potential

1968 • 143 citations

An analysis of the action of a false transmitter at the neuromuscular junction.

1977 • 142 citations

Factors affecting the time course of decay of end‐plate currents: a possible cooperative action of acetylcholine on receptors at the frog neuromuscular junction.

1975 • 135 citations

Acetylcholine Receptor and Ion Conductance Modulator Sites at the Murine Neuromuscular Junction: Evidence from Specific Toxin Reactions

1973 • 133 citations

A morphological study of the cholinergic receptor protein from Torpedo marmorata in its membrane environment and in its detergent-extracted purified form

1978 • 130 citations

Effects of some aliphatic alcohols on the conductance change caused by a quantum of acetylcholine at the toad end‐plate.

1975 • 130 citations

The mode of action of antagonists of the excitatory response to acetylcholine in Aplysia neurones.

1978 • 128 citations

The binding of labelled saxitoxin to the sodium channels in nerve membranes

1973 • 128 citations

The regulation of enzyme activity and allosteric transition

1970 • 127 citations

Drug Receptors and their Function

1971 • 125 citations

The effect of membrane polarization on the time course of the end‐plate current in frog sartorius muscle

1969 • 123 citations

The kinetics of action of acetylcholine antagonists in smooth muscle

1966 • 122 citations

Conductance of channels opened by acetylcholine-like drugs in muscle end-plate

1975 • 121 citations

Effects of inhibitors of the binding of iodinated alpha-bungarotoxin to acetylcholine receptors in rat muscle.

1976 • 115 citations

Studies on the electrogenic action of acetylcholine with Torpedo marmorata electric organ

1976 • 113 citations

Displacement currents in the node of Ranvier

1975 • 111 citations

How many conductance states do potassium channels have?

1975 • 108 citations

A study of desensitization using voltage clamp

1975 • 108 citations

Co-operative binding of nicotinamide-adenine dinucleotide to yeast glyceraldehyde-3-phosphate dehydrogenase

1971 • 106 citations

Dynamic properties of isolated acetylcholine receptor proteins: release of calcium ions caused by acetylcholine binding.

1976 • 103 citations

The M. omohyoideus of the mouse as a convenient mammalian muscle preparation

1976 • 102 citations

The effect of procaine on the action of acetylcholine at the neuromuscular junction.

1975 • 101 citations

Junctional and extrajunctional acetylcholine receptors in normal and denervated frog muscle fibres

1976 • 100 citations

On the analysis of pharmacological experiments in terms of an allosteric receptor model.

1973 • 99 citations

Conductance increases produced by bath application of cholinergic agonists to Electrophorus electroplaques.

1975 • 96 citations

Acetylcholine receptor distribution on myotubes in culture correlated to acetylcholine sensitivity.

1977 • 96 citations

A Kinetic Model for the Action of Xylocaine on Receptors for Acetylcholine

1968 • 96 citations

The binding of tetrodotoxin to nerve membranes

1971 • 95 citations

Tetrodotoxin binding to normal depolarized frog muscle and the conductance of a single sodium channel.

1975 • 95 citations

Handbuch der experimentellen Pharmakologie.

1967 • 95 citations

Calcium Binding and Tension Development in Detergent-Treated Muscle Fibers

1974 • 90 citations

Voltage-dependent effect of curare at the frog neuromuscular junction

1977 • 90 citations

Interconversion between Different States of Affinity for Acetylcholine of the Cholinergic Receptor Protein from Torpedo marmorata

1975 • 87 citations

Partial Characterization of a Tetrodotoxin-Binding Component from Nerve Membrane

1972 • 86 citations

THE AFFINITY AND EFFICACY OF ONIUM SALTS ON THE FROG RECTUS ABDOMINIS

1967 • 85 citations

Relaxation measurements on the acetylcholine receptor.

1975 • 85 citations

On the measurement of the affinity of partial agonists for receptors.

1969 • 82 citations

Sodium transport by the acetylcholine receptor of cultured muscle cells.

1975 • 81 citations

An analysis of the dose-response curve at voltage-clamped frog-endplates

1975 • 79 citations

Electrical changes in the membrane in junctional transmission

1973 • 77 citations

The binding of tetrodotoxin and α‐bungarotoxin to normal and denervated mammalian muscle

1974 • 74 citations

In vitro excitation of purified membrane fragments by cholinergic agonists

1971 • 74 citations

An attempt at an analysis of the factors determining the time course of the end‐plate current

1972 • 72 citations

Studies on the electrogenic action of acetylcholine with Torpedo marmorata electric organ

1976 • 68 citations

Kinetics of agonist conductance changes during hyperpolarization at frog endplates

1997 • 67 citations

Acetylcholine Binding to Torpedo Electroplax: Relationship to Acetylcholine Receptors

1971 • 67 citations

Mechanisms of Drug Action at the Voluntary Muscle Endplate

1975 • 66 citations

Inhibition of Lysosomal Plasminogen Activator Activity in Experimental Shock

1973 • 66 citations

The rate of action of atropine.

1968 • 64 citations

Characterization of drug iontophoresis with a fast microassay technique

1976 • 64 citations

Transmission of Impulses from Nerve to Muscle

1976 • 63 citations

Analysis of Cooperativity of Drug-Receptor Interaction by Quantitative Iontophoresis at Frog Motor End Plates

1976 • 61 citations

A quantitative description of end‐plate currents in the presence of two lidocaine derivatives.

1976 • 60 citations

Postsynaptic membranes in the electric tissue of Narcine: IV. Isolation and characterization of the nicotinic receptor protein

1977 • 60 citations

Density and dose-response curve of acetylcholine receptors in frog neuromuscular junction

1975 • 59 citations

Relaxation experiments using bath‐applied suberyldicholine.

1977 • 56 citations

KINETICS OF AGONIST CONDUCTANCE CHANGES DURING HYPERPOLARIZATION AT FROG ENDPLATES

1975 • 56 citations

Mechanism of blockade of neuromuscular transmission by pentobarbital.

1975 • 56 citations

The effect of atropine on acetylcholine action at the neuromuscular junction

1973 • 55 citations

A discontinuous relationship between the acetylcholine-activated channel conductance and temperature

1976 • 55 citations

A voltage‐clamp study of the permeability change induced by quanta of transmitter at the mouse end‐plate.

1978 • 55 citations

SOME IONIC FACTORS THAT INFLUENCE THE ACTION OF ACETYLCHOLINE AT THE MUSCLE END‐PLATE MEMBRANE*

1959 • 54 citations

EFFECTS OF SEVERAL INHALATION ANAESTHETICS ON THE KINETICS OF POSTSYNAPTIC CONDUCTANCE CHANGES IN MOUSE DIAPHRAGM

1976 • 54 citations

Current-voltage relation and reversal potential at junctional and extrajunctional ACh-receptors of the frog neuromuscular junction

1976 • 54 citations

Response of acetylcholine receptors to rapid photochemically produced increases in agonist concentration

1977 • 53 citations

Dynamic properties of isolated acetylcholine receptor protein: kinetics of the binding of acetylcholine and Ca ions.

1976 • 52 citations

A comparison of current‐voltage relations for full and partial agonists.

1978 • 51 citations

The active form of pentobarbital in squid giant axons.

1971 • 49 citations

Binding of d-tubocurarine and α-bungarotoxin in normal and denervated mouse muscles

1974 • 49 citations

Comparison between the affinities for reversible cholinergic ligands of a purified and membrane bound state of the acetylcholine‐receptor protein from Electrophorus electricus

1973 • 49 citations

The binding of labelled saxitoxin to the sodium channels in normal and denervated mammalian muscle, and in amphibian muscle.

1977 • 45 citations

Influence of chloride ions on changes in membrane potential during prolonged application of carbachol to frog skeletal muscle

1973 • 43 citations

On the role of junctional cholinesterase in determining the time course of the end‐plate current.

1977 • 43 citations

The study of allosteric proteins

1973 • 43 citations

Relaxation spectra of aspartate transcarbamylase. I. Interaction of 5-bromocytidine triphosphate with native enzyme and regulatory subunit

1970 • 42 citations

Noise and relaxation studies of acetylcholine induced currents in the presence of procaine.

1978 • 42 citations

End-plate noise.

1968 • 41 citations

Decamethonium in depolarized muscle and the effects of tubocurarine

1970 • 41 citations

On the latency and form of the membrane responses of smooth muscle to the iontophoretic application of acetylcholine or carbachol

1976 • 40 citations

Binding of perhydro-histrionicotoxin to the postsynaptic membrane of skeletal muscle in relation to its blockage of acetylcholine-induced depolarization.

1977 • 39 citations

The kinetics of the interaction between tetrodotoxin and mammalian nonmyelinated nerve fibers.

1972 • 38 citations

EFFECTS OF METHYL-AND ETHYL-DERIVATIVESOF NH4+ ON THE NEUROMUSCULAR JUNCTION

1959 • 38 citations

Cooperativities in the binding of acetylcholine to its receptor

1973 • 36 citations

Endplate currents are shortened by octanol: Possible role of membrane lipid

1974 • 36 citations

The rate of action of competitive neuromuscular blocking agents.

1967 • 35 citations

Relation Between Structure and Action of Quaternary Ammonium Neuromuscular Blocking Agents

1965 • 34 citations

INFLUENCE OF SKF‐525A CONGENERS, STROPHANTHIDIN AND TISSUE‐CULTURE MEDIA ON DESENSITIZATION IN FROG SKELETAL MUSCLE

1974 • 33 citations

Desensitization at the Motor Endplate

1973 • 32 citations

Restoration of neuromuscular transmission in sodium‐free hydrazinium solution

1959 • 32 citations

Evidence for separate initiation and inhibitory sites in the regulation of membrane potential of electroplax I. Kinetic studies with α-bungarotoxin

1973 • 32 citations

The Cholinergic Receptor Protein from Fish Electric Organ

1975 • 31 citations

Ligand interactions with the acetylcholine receptor from Torpedo californica. Extensions of the allosteric model for cooperativity to half-of-site activity

1976 • 31 citations

Voltage dependence of agonist responses at voltage-clamped frog endplates

1976 • 31 citations

Saxitoxin and procaine act independently on separate sites of the sodium channel

1976 • 30 citations

An allosteric mechanism for the acetylcholine receptor

1972 • 30 citations

Vulnerability of desensitized or curare-treated acetylcholine receptors to irreversible blockade by cobra toxin.

1972 • 29 citations

Response of acetylcholine receptors to photoisomerizations of bound agonist molecules

1978 • 28 citations

Conversion of high affinity acetylcholine receptor from Torpedo californica electroplax to an altered form

1975 • 26 citations

ON THE SIMULTANEOUS ACTION OF TWO COMPETITIVE ANTAGONISTS

1974 • 25 citations

Functional Properties of Postjunctional Membrane

1976 • 24 citations

The influence of curare on the uptake and release of a neuromuscular blocking agent labeled with radioactive iodine.

1963 • 24 citations

An anti‐curare effect of hexamethonium at the mammalian neuromuscular junction

1973 • 24 citations

Entry of decamethonium in rat muscle studied by autoradiography

1970 • 23 citations

Half-of-the-site reactivity of the membrane-bound Electrophorus electricus acetylcholine receptor

1974 • 23 citations

The turnover and distribution of labelled corticosterone during post-natal development of the duckling (Anas platyrhynchos)

1976 • 22 citations

INTERACTION OF COMPETITIVE ANTAGONISTS: THE ANTI‐CURARE ACTION OF HEXAMETHONIUM AND OTHER ANTAGONISTS AT THE SKELETAL NEUROMUSCULAR JUNCTION

1975 • 22 citations

Potentiation by an Antagonist

1969 • 21 citations

Drug interactions at the motor endplate

1975 • 20 citations

Affinity of cholinergic ligands for the partially purified acetylcholine receptor from mammalian skeletal muscle

1974 • 18 citations

DEPOLARIZATION OF END-PLATES BY ACETYLCHOLINE EXTERNALLY APPLIED

1956 • 17 citations

Labeled decamethonium in denervated skeletal muscle.

1971 • 16 citations

THE KINETICS OF COMPETITIVE ANTAGONISTS ON GUINEA-PIG ILEUM

1976 • 16 citations

Rate of offset of action of slow-acting muscarinic antagonists is fast

1977 • 16 citations

A Linear Dose-Response Curve at the Motor Endplate

1973 • 16 citations

Binding of ?-bungarotoxin and cholinergic ligands to acetylcholine receptors in the membrane of skeletal muscle

1977 • 16 citations

Comparison of the action of different barbiturates on squid axon membranes

1975 • 15 citations

Structure-Function Relationships in Excitable Membranes

1975 • 13 citations

Purification of Neurophysins by Affinity Chromatography

1974 • 13 citations

Adsorption and diffusion of gamma‐globulin during passive sensitization of chopped guinea‐pig lung.

1965 • 12 citations

Two mechanisms for spontaneous recovery from depolarising drugs in rat muscle

1976 • 11 citations

Die Dissoziationskonstante zwischen Curare und dem Acetylcholin-Receptor

1971 • 9 citations

The action of tubocurarine at the neuromuscular junction [proceedings].

1978 • 8 citations

Further studies on the binding properties of cobra neurotoxin to cholinergic receptors in mouse skeletal muscle

1975 • 8 citations

Ganglionic transmission in the autonomic nervous system.

1968 • 7 citations

A COMPARISON OF THE TIME COURSE OF EXCITATION AND INHIBITION BY IONTOPHORETIC DECAMETHONIUM IN FROG ENDPLATE

1976 • 6 citations

Co-operativity in the cyclic model for drug-receptor interaction

1976 • 4 citations

LABELLED DECAMETHONIUM IN CAT MUSCLE

1976 • 4 citations

How long does a molecule stay on the receptor? Explanation of a paradox.

1970 • 4 citations

THE USE OF DIFFERENT AGONISTS IN ANTAGONIST AFFINITY CONSTANT ESTIMATIONS

1976 • 2 citations

生体膜―刺激受容過程の分子的機作

1975 • 2 citations