Structure—Activity Relationships for alpha-1 Adrenergic Receptor Agonists and Antagonists

A STUDY OF THE ADRENOTROPIC RECEPTORS

1948 • 2,856 citations

Differentiation of Receptor Systems activated by Sympathomimetic Amines

1967 • 2,054 citations

Frontiers in Catecholamine Research

1973 • 1,252 citations

Presynaptic regulation of catecholamine release

1974 • 1,145 citations

A MODIFICATION OF RECEPTOR THEORY

1956 • 1,126 citations

The Classification of Adrenoceptors (Adrenergic Receptors). An Evaluation from the Standpoint of Receptor Theory

1972 • 812 citations

A functional basis for classification of α-adrenergic receptors

1977 • 802 citations

The classification of drugs and drug receptors in isolated tissues.

1984 • 474 citations

Relative pre- and postsynaptic potencies of ?-adrenoceptor agonists in the rabbit pulmonary artery

1975 • 455 citations

Frontiers in Catecholamine Research

1976 • 451 citations

Studies on the relationship between chemical constitution and physiological action

1933 • 437 citations

THE PHARMACOLOGICAL DIFFERENTIATION OF ADRENERGIC RECEPTORS*

1967 • 376 citations

Alpha sympathomimetic inhibition of adrenergic and cholinergic transmission in the rabbit heart

1972 • 293 citations

Pre- and postsynaptic effects of yohimbine stereoisomers on noradrenergic transmission in the pulmonary artery of the rabbit

1979 • 273 citations

IMPORTANT CONCEPTS OF RECEPTOR THEORY

1982 • 251 citations

Selectivity of some alpha adrenoceptor agonists for peripheral alpha-1 and alpha-2 adrenoceptors in the normotensive rat.

1981 • 197 citations

Identification of alpha-adrenergic receptors in uterine smooth muscle membranes by [3H]dihydroergocryptine binding.

1976 • 190 citations

Alpha and beta adrenergic effects of the stereoisomers of dobutamine.

1981 • 180 citations

Stereochemistry and biological activity of drugs

1983 • 178 citations

A comparison of pre- and postsynaptic effects of α-adrenolytic drugs in the pulmonary artery of the rabbit

1977 • 166 citations

Dissociation constants and relative efficacies of agonists acting on alpha adrenergic receptors in rabbit aorta.

1976 • 160 citations

Molecular geometry and adrenergic drug activity.

1974 • 146 citations

The pharmacological classification of adrenergic alpha 1 and alpha 2 receptors and their mechanisms of action.

1979 • 143 citations

Chemical Pharmacology of the Synapse

1977 • 121 citations

Adrenoceptors and catecholamine action

1981 • 111 citations

THE α‐ AND β‐ADRENOCEPTOR BLOCKING POTENCIES OF LABETALOL AND ITS INDIVIDUAL STEREOISOMERS IN ANAESTHETIZED DOGS AND IN ISOLATED TISSUES

1982 • 105 citations

Quantum mechanical study of the conformational properties of phenethylamines of biochemical and medicinal interest

1972 • 105 citations

A lipophilic, selective α1 -adrenoceptor agonist: 2-(2-chloro-5-trifluoromethylphenylimino) imidazolidine (St 587)

1981 • 104 citations

Molecular mechanics calculations on alkanes and non-conjugated alkenes

1977 • 98 citations

THE REGULATION OF TRANSMITTER RELEASE ELICITED BY NERVE STIMULATION THROUGH A PRESYNAPTIC FEED-BACK MECHANISM

1973 • 97 citations

Lack of cross-desensitization between structurally dissimilar α-adrenoceptor agonists

1977 • 97 citations

Receptor interactions of imidazolines. I. Affinity and efficacy for alpha adrenergic receptors in rat aorta.

1979 • 88 citations

Chemical pharmacology of the synapse

1976 • 84 citations

Studies on the relationship between chemical constitution and physiological action

1932 • 83 citations

Steric Aspects of Adrenergic Drugs

1970 • 79 citations

Pharmacological and biochemical properties of isomeric yohimbine alkaloids

1978 • 75 citations

Possible relationship between receptor reserve and the differential antagonism of alpha-1 and alpha-2 adrenoceptor-mediated pressor responses by calcium channel antagonists in the pithed rat.

1984 • 72 citations

An in vitro quantitative analysis of the alpha adrenoceptor partial agonist activity of dobutamine and its relevance to inotropic selectivity.

1981 • 66 citations

Differences in the applicability of the Easson-Stedman hypothesis to the α1- and α2-adrenergic effects of phenethylamines and imidazolines

1983 • 64 citations

Synthesis and biological properties of 2-, 5-, and 6-fluoronorepinephrines

1979 • 64 citations

The chemistry and biology of ring‐fluorinated biogenic amines

1984 • 61 citations

Postsynaptic α2-adrenoceptors mediate pressor responses to 2-N,N-dimethylamino-5,6-dihydroxy-1,2,3,4-tetrahydronaphthalene (M-7)

1980 • 61 citations

Steric aspects of adrenergic drugs. II. Effects of DL isomers and desoxy derivatives on the reserpine-pretreated vas deferens.

1967 • 56 citations

Molecular mechanics and the camseq processor

1977 • 56 citations

Biophysical characterization of the purified alpha 1-adrenergic receptor and identification of the hormone binding subunit.

1982 • 50 citations

Atlas of the three-dimensional structure of drugs

1979 • 49 citations

Studies on YM-12617: A selective and potent antagonist of postsynaptic ?1-adrenoceptors

1985 • 48 citations

2-[[[2-(2,6-Dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzoxathian: a new antagonist with high potency and selectivity towards .alpha.1-adrenoreceptors

1984 • 48 citations

The preferred conformation of noradrenaline and a consideration of the α-adrenergic receptor

1969 • 47 citations

Steric aspects of adrenergic drugs. I. Comparative effects of DL isomers and desoxy derivatives.

1967 • 44 citations

Evidence for and against heterogeneity of alpha1-adrenoceptors

1986 • 43 citations

Molecular characteristics of biogenic monoamines and their analogs

1973 • 42 citations

Receptor interactions of imidazolines. IV. Structural requirements for alpha adrenergic receptor occupation and receptor activation by clonidine and a series of structural analogs in rat aorta.

1980 • 41 citations

Receptor Interactions of Imidazolines

1982 • 41 citations

Alpha 1-adrenergic receptor structure.

1984 • 40 citations

Quantitative relationships between .alpha.-adrenergic activity and binding affinity of .alpha.-adrenoceptor agonists and antagonists

1984 • 38 citations

A comparison of the contractile responses of the rabbit basilar and pulmonary arteries to sympathomimetic agonists: further evidence for variation in vascular adrenoceptor characteristics.

1981 • 37 citations

Cambridge Crystallographic Data Centre. II. Structural Data File

1973 • 33 citations

Absolute configuration of glycerol derivatives. 7. Enantiomers of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]ethyl]-1,4-benzodioxane (WB-4101), a potent competitive .alpha.-adrenergic antagonist

1979 • 31 citations

Photoaffinity labeling of the .alpha.1-adrenergic receptor using an 125I-labeled aryl azide analog of prazosin

1984 • 31 citations

Aromatic and benzylic hydroxyl substitution of imidazolines and phenethylamines: differences in activity at alpha-1 and alpha-2 adrenergic receptors.

1983 • 31 citations

Receptor interactrions of imidazolines. VI. Significance of carbon bridge separating phenyl and imidazoline rings of tolazoline-like alpha adrenergic imidazolines.

1980 • 31 citations

Steric aspects of adrenergic drugs. IX. Pharmacologic and histochemical studies on isomers of cobefrin (alpha-methylnorepinephrine).

1968 • 30 citations

Identification of the subunit-binding site of alpha 2-adrenergic receptors using [3H]phenoxybenzamine.

1984 • 29 citations

Stereochemical requirements of alpha-2 adrenergic receptors.

1982 • 29 citations

Conformational analogs of dopamine. Synthesis and pharmacological activity of (E)- and (Z)-2-(3,4-dihydroxyphenyl)cyclopropylamine hydrochlorides

1979 • 29 citations

Affinity chromatography of human platelet α ₂ -adrenergic receptors

1982 • 27 citations

Receptor interactions of imidazolines. II. Affinities and efficacies of hydroxy-substituted tolazoline derivatives in rat aorta.

1979 • 27 citations

Comparison of central and peripheral alpha1-adrenoceptors

1982 • 26 citations

Blockade of postjunctional vascular alpha 1- and alpha 2-adrenoceptors in pithed rat by the enantiomers of WB-4101

1983 • 25 citations

.alpha.-Adrenergic agents. 1. Direct-acting .alpha.1 agonists related to methoxamine

1981 • 25 citations

261. Molecular dissymmetry and physiological activity

1933 • 25 citations

Relative agonist potency as a means of differentiating α-adrenoceptors and α-adrenergic mechanisms

1985 • 24 citations

.alpha.-Adrenergic agents. 2. Synthesis and .alpha.1-agonist activity of 2-aminotetralins

1982 • 24 citations

The molecular conformation of clonidine hydrochloride, an ?-adrenergic agonist

1979 • 22 citations

Remarks on chemical specificity

1950 • 21 citations

Stereochemical requirements of α2-adrenergic receptors for α-methyl substituted phenethylamines

1982 • 20 citations

Crystal structure and absolute configuration of yohimbine hydrochloride, C21H27ClN2O3

1973 • 20 citations

l-1,2,3,4-Tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine: a potent and selective agonist at .alpha.1-adrenoceptors

1983 • 20 citations

ANTAGONISM OF PRE AND POSTSYNAPTIC α‐ADRENORECEPTORS BY BE 2254 (HEAT) AND PRAZOSIN

1981 • 19 citations

An evaluation of the ability of a series of full alpha-1 adrenoceptor agonists to release internal calcium in venous smooth muscle.

1985 • 19 citations

Stereochemical studies of adrenergic drugs. Optically active derivatives of imidazolines

1976 • 18 citations

Optically active derivatives of imidazolines. .alpha.-Adrenergic blocking properties

1980 • 17 citations

α1-adrenoceptor-mediated vasoconstriction in vivo to enantiomers of SK&F 89748-A

1984 • 17 citations

Synthesis and pharmacological properties of a series of 2-substituted aminomethyl-1,4-benzodioxanes

1969 • 17 citations

Receptor interactions of imidazolines. III. Structure-activity relationships governing alpha adrenergic receptor occupation and receptor activation for mono- and dimethoxy-substituted tolazoline derivatives in rat aorta.

1979 • 16 citations

Ultraviolet photoelectron spectroscopy of cyclic amidines. 2. Electronic structure of clonidine and some related 2-(phenylimino)imidazolidines with .alpha.-adrenergic activity

1980 • 16 citations

Alpha adrenoreceptors of rabbit aorta and stomach fundus.

1981 • 16 citations

Optically active catecholimidazolines: a study of steric interactions at .alpha.-adrenoreceptors

1983 • 15 citations

Photoaffinity label for the alpha 1-adrenergic receptor: synthesis and effects on membrane and affinity-purified receptors.

1983 • 13 citations

Discrimination between peripheral and central α-adrenergic effects using meta-substituted imidazolidines

1981 • 13 citations

Photoaffinity cross-linking of a radioiodinated probe, 125I-A55453, into alpha 1-adrenergic receptors.

1984 • 13 citations

A conformational study of .beta.-phenethanolamine receptor sites. I. The syntheses of the 3-amino-2-phenyl-trans-2-decalols

1968 • 13 citations

Conformational requirements of alpha 2-adrenergic receptors.

1982 • 13 citations

Calcium Influx-Dependent and -Independent α1-Adrenoceptor-Mediated Processes of Vasoconstriction In Vivo Do Not Operate via Different α1-Adrenoceptor Subtypes

1984 • 11 citations

In vitro studies on 6-fluoronoradrenaline at several peripheral sympathetic neuroeffector junctions

1981 • 11 citations

Quantitative aspects of alpha adrenergic effects induced by clonidine-like imidazolidines. I. Central hypotensive and peripheral hypertensive activities.

1982 • 10 citations

Calcium influx-dependent and -independent alpha 1-adrenoceptor-mediated processes of vasoconstriction in vivo do not operate via different alpha 1-adrenoceptor subtypes.

1984 • 10 citations

Kinetics of Alpha-Adrenoreceptor Blockade by Phentolamine in the Normal and Denervated Rabbit Aorta and Rat Vas Deferens

1979 • 10 citations

Evidence in favour of a selective ?1-adrenoceptor blocking action of WB 4101 in vivo

1982 • 9 citations

Adrenergic Blocking Properties of some New Benzodioxanes

1965 • 9 citations

INTERACTIONS OF DIMETHOXY‐SUBSTITUTED TOLAZOLINE DERIVATIVES WITH α₁‐ AND α₂‐ADRENORECEPTORS IN VITRO

1985 • 9 citations

N-[2-hydroxy-5-[2-(methylamino)ethyl]phenyl]methanesulfonamide. A potent agonist which releases intracellular calcium by activation of .alpha.1-adrenoceptors

1985 • 8 citations

Selectivity of Benzodioxane α-Adrenoceptor Antagonists for α<sub>1</sub>-and α<sub>2</sub>-Adrenoceptors Determined by Binding Affinity

1983 • 8 citations

Evaluation of the alpha-1 and alpha-2 adrenoceptor-mediated effects of a series of dimethoxy-substituted tolazoline derivatives in the cardiovascular system of the pithed rat.

1985 • 7 citations

Arylazide photoaffinity probe for α2-adrenoceptors

1985 • 6 citations

Preferential Blockade of α1-Adrenoceptors in the Rabbit Pulmonary Artery by Derivatives of β-Phenylethylamine Chemically Related to BE 2254 (HEAT)

1983 • 5 citations

The irreversible alpha-blocker benextramine interacts with two different thiol groups.

1983 • 1 citations

Deleted Work

1955 • 0 citations