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International Union of Pharmacology. XIII. Classification of histamine receptors.

Data up to Jan 2025

Published1997
Citations869
References375

Total Citations Per Year

Abstract

References (375)

SOME QUANTITATIVE USES OF DRUG ANTAGONISTS

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Histaminergic transmission in the mammalian brain

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Highly potent and selective ligands for histamine H3-receptors

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H1-Receptor Antagonists

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Distribution, properties, and functional characteristics of three classes of histamine receptor.

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Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists

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Cimetidine—A Non-Thiourea H2-Receptor Antagonist

1975 • 449 citations

Cultured endothelial cells synthesize both platelet-activating factor and prostacyclin in response to histamine, bradykinin, and adenosine triphosphate.

1985 • 430 citations

Histamine and noradrenaline decrease calcium-activated potassium conductance in hippocampal pyramidal cells

1983 • 413 citations

Molecular pharmacological aspects of histamine receptors

1995 • 353 citations

Histamine inhibits dopamine release in the mouse striatum via presynaptic H3 receptors

1993 • 337 citations

A human airway smooth muscle cell line that retains physiological responsiveness

1989 • 321 citations

Histamine H3 receptor-mediated inhibition of serotonin release in the rat brain cortex

1988 • 304 citations

Cyclic Nucleotides in the Nervous System

1977 • 297 citations

The distribution of histamine H1-receptors in the rat brain: An autoradiographic study

1981 • 290 citations

Modulation of neuronal firing mode in cat and guinea pig LGNd by histamine: possible cellular mechanisms of histaminergic control of arousal

1991 • 284 citations

A detailed autoradiographic mapping of histamine H3 receptors in rat brain areas

1993 • 270 citations

Autoinhibition of histamine synthesis mediated by presynaptic H3-receptors

1987 • 265 citations

Three histamine receptors (H1, H2 and H3) visualized in the brain of human and non-human primates

1990 • 262 citations

Brain histamine receptors as targets for antidepressant drugs

1978 • 258 citations

Histamine H3 receptors modulate the release of [3H]‐acetylcholine from slices of rat entorhinal cortex: evidence for the possible existence of H3 receptor subtypes

1992 • 256 citations

Role of the endothelium in the vasodilator response of rat thoracic aorta to histamine

1983 • 249 citations

Autoregulation of histamine release in brain by presynaptic H3-receptors

1985 • 245 citations

Inhibition of noradrenaline release in the rat brain cortex via presynaptic H3 receptors

1989 • 245 citations

Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors.

1996 • 235 citations

The effects of the H1 and H2 antihistamines on "allergic" histamine release and its inhibition by histamine.

1975 • 233 citations

A novel class (H3) of histamine receptors on perivascular nerve terminals

1987 • 232 citations

Tricyclic antidepressant drugs block histamine H2 receptor in brain

1977 • 231 citations

Expression cloning of a cDNA encoding the bovine histamine H1 receptor.

1991 • 230 citations

HETEROGENEITY OF HISTAMINE Hi‐RECEPTORS: SPECIES VARIATIONS IN [3H]MEPYRAMINE BINDING OF BRAIN MEMBRANES

1979 • 225 citations

Changes in cytosolic Ca2+ associated with von Willebrand factor release in human endothelial cells exposed to histamine. Study of microcarrier cell monolayers using the fluorescent probe indo-1.

1987 • 225 citations

Impromidine (SK&F 92676) is a very potent and specific agonist for histamine H2 receptors

1978 • 220 citations

Hemolytic Plaque Formation by Leukocytes in Vitro CONTROL BY VASOACTIVE HORMONES

1974 • 219 citations

Histamine-sensitive adenylate cyclase in mammalian brain

1976 • 218 citations

Histamine Augments Leukocyte Adenosine 3′,5′-Monophosphate and Blocks Antigenic Histamine Release

1971 • 188 citations

Molecular cloning of the human histamine H2 receptor

1991 • 183 citations

A detailed mapping of hist amine H1-receptors in guinea-pig central nervous system established by autoradiography with [125I]iodobolpyramine

1988 • 182 citations

Histamine potentiates N-methyl-d-aspartate responses in acutely isolated hippocampal neurons

1993 • 179 citations

The action of histamine and 5-hydroxytryptamine on isolated mammalian atria.

1960 • 177 citations

Histamine increases venular permeability via a phospholipase C-NO synthase-guanylate cyclase cascade

1993 • 174 citations

Enhancement by histamine of NMDA-mediated synaptic transmission in the hippocampus

1993 • 169 citations

Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex

1983 • 159 citations

S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist.

1992 • 158 citations

Actions of betahistine at histamine receptors in the brain

1985 • 157 citations

Isothiourea analogues of histamine as potent agonists or antagonists of the histamine H3-receptor

1992 • 148 citations

Sulphur-methylene isosterism in the developent of metiamide, a new histamine H2-receptor antagonist

1974 • 147 citations

Identification of two H3-histamine receptor subtypes.

1990 • 146 citations

H3‐Receptors Control Histamine Release in Human Brain

1988 • 145 citations

Molecular basis for the interaction of histamine with the histamine H2 receptor.

1992 • 144 citations

Regulation of P2y‐purinoceptor‐mediated prostacyclin release from human endothelial cells by cytoplasmic calcium concentration

1988 • 142 citations

Specific binding of 3H-mepyramine to histamine H1 receptors in intestinal smooth muscle

1977 • 141 citations

Histamine responsiveness of isolated gastric glands

1980 • 139 citations

Mechanisms of antihistamine-induced sedation in the human brain: H1 receptor activation reduces a background leakage potassium current

1994 • 138 citations

[3H]Mianserin: differential labeling of serotonin and histamine receptors in rat brain.

1981 • 137 citations

Molecular Cloning of the Human Histamine H1 Receptor Gene

1994 • 136 citations

Effects of histamine H3-receptor ligands on various biochemical indices of histaminergic neuron activity in rat brain

1989 • 135 citations

Reversible and irreversible labeling and autoradiographic localization of the cerebral histamine H2 receptor using [125I]iodinated probes.

1990 • 134 citations

Chemistry and Structure—Activity Relationships of Drugs Acting at Histamine Receptors

1982 • 133 citations

Genomic Cloning, Heterologous Expression and Pharmacological Characterization of a Human Histamine H1 Receptor

1993 • 131 citations

[125I]iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors.

1994 • 130 citations

Properties of calcium stores and transient outward currents in single smooth muscle cells of rabbit intestine.

1989 • 130 citations

Synthese des Imidazolyl‐äthylamins

1907 • 125 citations

Central actions of histamine: Microelectrophoretic studies

1977 • 125 citations

Endothelium‐dependent relaxation induced by angiotensin II and histamine in isolated arteries of dog

1984 • 122 citations

β ‐Adrenoceptor stimulation inhibits histamine‐stimulated inositol phospholipid hydrolysis in bovine tracheal smooth muscle

1988 • 121 citations

PHARMACOLOGY OF ANTIHISTAMINE COMPOUNDS

1947 • 120 citations

Involvement of histamine in growth of mouse and rat tumors: antitumoral properties of monofluoromethylhistidine, an enzyme-activated irreversible inhibitor of histidine decarboxylase.

1984 • 118 citations

Sedation and histamine H1‐receptor antagonism: studies in man with the enantiomers of chlorpheniramine and dimethindene

1991 • 118 citations

Inhibition of guinea pig ileum contractions mediated by a class of histamine receptor resembling the H3 subtype.

1987 • 117 citations

Histamine-induced calcium release and phorbol antagonism in cultured airway smooth muscle cells

1987 • 115 citations

Increased permeability of microcarrier-cultured endothelial monolayers in response to histamine and thrombin. A model for the in vitro study of increased vasopermeability.

1986 • 113 citations

Histamine H3‐receptors inhibit cholinergic neurotransmission in guinea‐pig airways

1989 • 110 citations

Guinea Pig Histamine H1 Receptor. II. Stable Expression in Chinese Hamster Ovary Cells Reveals the Interaction with Three Major Signal Transduction Pathways

1994 • 110 citations

Synthesis and in vitro pharmacology of arpromidine and related phenyl(pyridylalkyl)guanidines, a potential new class of positive inotropic drugs

1989 • 110 citations

Presynaptic inhibition produced by histamine at nicotinic synapses in enteric ganglia

1988 • 108 citations

Histamine is an Intracellular Messenger Mediating Platelet Aggregation

1989 • 108 citations

Histamine H1 receptor occupancy in human brains after single oral doses of histamine H1 antagonists measured by positron emission tomography

1995 • 108 citations

Site-Directed Mutagenesis of the Histamine H1 Receptor: Roles of Aspartic Acid107, Asparagine198 and Threonine194

1994 • 107 citations

Novel 1, 2, 4-oxadiazoles as potent and selective histamine H3 receptor antagonists

1996 • 105 citations

Histamine and cyclic AMP in isolated canine parietal cells.

1979 • 104 citations

Lipophilicity and hydrogen-bonding capacity of H1-antihistaminic agents in relation to their central sedative side-effects

1994 • 103 citations

Characteristics of histamine H1-receptors in peripheral tissues labeled with [3H]mepyramine.

1979 • 102 citations

Histamine H3-receptor signaling in the heart: possible involvement of Gi/Go proteins and N-type Ca++ channels.

1994 • 101 citations

Histamine H2-receptor agonists. Synthesis, in vitro pharmacology, and qualitative structure-activity relationships of substituted 4- and 5-(2-aminoethyl)thiazoles

1992 • 100 citations

HISTAMINE H1‐RECEPTORS IN THE BRAIN OF THE GUINEA‐PIG AND THE RAT: DIFFERENCES IN LIGAND BINDING PROPERTIES AND REGIONAL DISTRIBUTION

1980 • 100 citations

Effects of histamine on hippocampal pyramidal cells of the rat in vitro

1986 • 100 citations

THE RELEASE OF CATECHOL AMINES FROM THE ADRENAL MEDULLA BY HISTAMINE

1965 • 99 citations

Cloning and tissue expression of a rat histamine H2-receptor gene

1991 • 99 citations

A New Potent and Selective Histamine H3 Receptor Agonist, 4-(1H-imidazol-4-ylmethyl)piperidine

1994 • 98 citations

In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole.

1982 • 97 citations

Histamine-stimulated and GTP-binding proteins-mediated phospholipase A2 activation in rabbit platelets.

1990 • 97 citations

Inhibition of T suppressor cell expression by histamine type 2 (H2) receptor antagonists.

1984 • 96 citations

ICI 125,211: A new gastric antisecretory agent acting on histamine H2-receptors

1979 • 96 citations

Sensitivity of histamine H3 receptor agonist-stimulated [35S]GTPγ[S]binding to pertussis toxin

1996 • 95 citations

A third histamine receptor subtype: Characterisation, localisation and functions of the H3-receptor

1990 • 95 citations

Pharmacological characterization of histamine receptors mediating the stimulation of cyclic AMP accumulation in slices from guinea-pig hippocampus.

1978 • 94 citations

Pharmacological Characterization and Autoradiographic Localization of Histamine H2 Receptors in Human Brain Identified with [125I]Iodoaminopotentidine

1992 • 93 citations

Biogenesis and physiology of histamine.

1971 • 93 citations

Characterization and tissue distribution of H3 histamine receptors in guinea pigs by Nα-methylhistamine

1990 • 93 citations

MEMBRANE POTENTIAL CHANGES ASSOCIATED WITH TACHYPHYLAXIS AND POTENTIATION OF THE RESPONSE TO STIMULATING DRUGS IN SMOOTH MUSCLE

1960 • 93 citations

Intracellular Ca regulation during secretagogue stimulation of the parietal cell

1988 • 92 citations

Histamine H3 receptor binding sites in rat brain membranes: modulations by guanine nucleotides and divalent cations

1990 • 92 citations

Histaminergic modulation of synaptic plasticity in area CA1 of rat hippocampal slices

1995 • 90 citations

Functional Identification of Histamine H 3 -Receptors in the Human Heart

1995 • 90 citations

Antagonism of histamine-activated adenylate cyclase in brain by D-lysergic acid diethylamide.

1977 • 89 citations

Observations on Reactive Hyperaemia as Related to Histamine, on Drugs Antagonizing Vasodilatation Induced by Histamine and on Vasodilator Properties of Adenosinetri phosphate

1948 • 89 citations

Multiple signaling pathways of histamine H2 receptors

1989 • 88 citations

Pharmacologic effects of autacoids on subsets of T cells. Regulation of expression/function of histamine-2 receptors by a subset of suppressor cells.

1985 • 87 citations

Expression of a cloned rat histamine H2 receptor mediating inhibition of arachidonate release and activation of cAMP accumulation.

1992 • 86 citations

The isolated stomach preparation of the mouse: a physiological unit for pharmacological analysis

1985 • 85 citations

Inhibition of noradrenaline release from the sympathetic nerves of the human saphenous vein by presynaptic histamine H3 receptors

1992 • 85 citations

Histamine H1 receptors in human brain labelled with [3H]Doxepin

1984 • 84 citations

Evidence for endothelial cell-mediated regulation of macromolecular permeability by postcapillary venules.

1986 • 83 citations

Characterization of histamine H3 receptors regulating acetylcholine release in rat entorhinal cortex

1995 • 83 citations

Pharmacological characterization of the human histamine H2 receptor stably expressed in Chinese hamster ovary cells

1994 • 83 citations

Histamine H3-receptors modulate nonadrenergic noncholinergic neural bronchoconstriction in guinea-pig in vivo

1989 • 81 citations

Autacoids as modulators of the inflammatory and immune response

1981 • 80 citations

Norepinephrine and histamine potentiate the increases in cyclic adenosine 3':5'-monophosphate elicited by vasoactive intestinal polypeptide in mouse cerebral cortical slices: mediation by alpha 1- adrenergic and H1-histaminergic receptors

1985 • 80 citations

Histamine Receptors in Brain

1983 • 80 citations

Histamine as an intracellular messenger

1990 • 79 citations

Site-Directed Mutagenesis of the Histamine H1-Receptor Reveals a Selective Interaction of Asparagine207 with Subclasses of H1-Receptor Agonists

1994 • 78 citations

Role of histamine in tumor development

1985 • 78 citations

Histamine H2-receptor binding with 3H-cimetidine in brain

1978 • 78 citations

Histamine H 3 -Receptor–Mediated Inhibition of Calcitonin Gene-Related Peptide Release From Cardiac C Fibers

1996 • 76 citations

Endogenous histamine excites neurones in the guinea‐pig superior cervical ganglion in vitro.

1989 • 76 citations

Characterization of histamine H3‐receptors in guinea‐pig ileum with H3‐selective ligands

1990 • 75 citations

Increase in histidine decarboxylase activity in mouse skin after application of the tumor promoter tetradecanoylphorbol acetate

1981 • 75 citations

Differentiation of H10and H2-receptors mediating positive chronoand inotropic responses to histamine on atrial preparations of the guinea-pig

1974 • 75 citations

Histamine-induced phosphoinositide metabolism in cultured human umbilical vein endothelial cells. Association with thromboxane and prostacyclin release

1987 • 74 citations

Selective displacement of [3H]mepyramine from peripheral vs. central nervous system receptors by loratadine, a non-sedating antihistamine

1986 • 74 citations

On the mechanism of histamine induced enhancement of the cardiac Ca2+ current

1987 • 74 citations

Histamine H2-receptors on single central neurones

1975 • 74 citations

Ranitidine (AH 19065): a new potent, selective histamine H2-receptor antagonist [proceedings].

1979 • 73 citations

Structural and functional analysis of the canine histamine H2 receptor by site-directed mutagenesis: N-glycosylation is not vital for its action

1995 • 72 citations

SOME CHEMICAL AND PHYSICAL PROPERTIES ASSOCIATED WITH HISTAMINE ANTAGONISM

1955 • 72 citations

Role of phosphoinositide metabolism in functional antagonism of airway smooth muscle contraction by β-adrenoceptor agonists

1989 • 72 citations

Subunit-specific potentiation of recombinant N-methyl-D-aspartate receptors by histamine.

1994 • 72 citations

Unmasking of activated histamine H3-receptors in myocardial ischemia: their role as regulators of exocytotic norepinephrine release.

1994 • 71 citations

Effects of histamine H1‐, H2‐ and H3‐receptor selective drugs on the mechanical activity of guinea‐pig small and large intestine

1991 • 71 citations

Measurement of cytoplasmic free Ca2+ concentration in bovine tracheal smooth muscle using aequorin

1987 • 70 citations

Histamine H3-receptors inhibit neurogenic microvascular leakage in airways

1990 • 70 citations

Genomic Cloning of the Rat Histamine H1 Receptor

1993 • 69 citations

Characterization of histamine‐H3 receptors controlling non‐adrenergic non‐cholinergic contractions of the guinea‐pig isolated ileum

1992 • 69 citations

Histamine‐induced increases in cyclic AMP levels in bovine adrenal medullary cells

1991 • 69 citations

Naming of substituted histamines

1974 • 68 citations

UK-14,304, R(−)-α-methyl-histamine and SMS 201-995 block plasma protein leakage within dura mater by prejunctional mechanisms

1992 • 68 citations

Decreased H2 Histamine Response of Granulocytes of Asthmatic Patients

1977 • 68 citations

Cholecystokinin, carbachol, gastrin, histamine, and forskolin increase [Ca2+]i in gastric glands

1986 • 68 citations

H1- and H2-receptor mediated responses to histamine on contractility and cyclic AMP of atrial and papillary muscles from guinea-pig hearts

1977 • 67 citations

Guinea Pig Histamine H1 Receptor. I. Gene Cloning, Characterization, and Tissue Expression Revealed by In Situ Hybridization

1994 • 67 citations

Histamine-Induced Inhibition of Normal Human Basophil Chemotaxis to C5a

1977 • 66 citations

Are antihistamines sedative via a blockade of brain H1 receptors?

1979 • 66 citations

Synthesis and Histamine H1 Receptor Agonist Activity of a Series of 2-Phenylhistamines, 2-Heteroarylhistamines, and Analogs

1995 • 66 citations

Immunoregulatory T cells in man. Histamine-induced suppressor T cells are derived from a Leu 2+ (T8+) subpopulation distinct from that which gives rise to cytotoxic T cells.

1985 • 65 citations

A highly potent and selective H3 agonist relaxes rabbit middle cerebral artery, in vitro

1988 • 65 citations

Histamine and Immune Responses

1982 • 65 citations

Purification of a histamine H3 receptor negatively coupled to phosphoinositide turnover in the human gastric cell line HGT1.

1992 • 65 citations

Multiple regulation of proenkephalin gene expression by protein kinase C.

1988 • 65 citations

Nordimaprit, homodimaprit, clobenpropit and imetit: affinities for H3 binding sites and potencies in a functional H3 receptor model

1993 • 65 citations

Effects of opioid peptides and morphine on histamine‐induced catecholamine secretion from cultured, bovine adrenal chromaffin cells

1986 • 65 citations

Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5‐HT3 receptor revealed

1995 • 65 citations

Zolantidine (SK&F 95282) is a potent selective brain‐penetrating histamine H2‐receptor antagonist

1988 • 64 citations

Characterization of H2 histamine receptor: linkage to both adenylate cyclase and [Ca2+]i signaling systems

1992 • 64 citations

Separate receptors mediating the positive inotropic and chronotropic effect of histamine in guinea-pig atria

1975 • 63 citations

Characterization of the binding of the first selective radiolabeled histamine H3‐receptor antagonist, [125I]‐iodophenpropit, to rat brain

1994 • 63 citations

Patterns of mast cell alterations and in vivo mediator release in human allergic skin reactions

1980 • 62 citations

The Guinea Pig Histamine H2 Receptor: Gene Cloning, Tissue Expression and Chromosomal Localization of Its Human Counterpart

1995 • 62 citations

Histamine: action on supraoptic and other hypothalamic neurones of the cat

1975 • 61 citations

Histamine‐induced inositol phospholipid breakdown in the longitudinal smooth muscle of guinea‐pig ileum

1985 • 61 citations

Dimaprit, [S-[3-(N,N-dimethylamino)propyl]isothiourea]. A highly specific histamine H2-receptor agonist. Part 2. Structure-activity considerations

1994 • 61 citations

Pharmacological studies with SK&F 93944 (temelastine), a novel histamine H1‐receptor antagonist with negligible ability to penetrate the central nervous system

1986 • 61 citations

H1-histaminergic activation of catecholamine release by chromaffin cells

1988 • 61 citations

Histamine increases cytosolic Ca2+ in HL-60 promyelocytes predominantly via H2 receptors with an unique agonist/antagonist profile and induces functional differentiation.

1992 • 60 citations

Novel Carbamates as Potent Histamine H3 Receptor Antagonists with High in Vitro and Oral in Vivo Activity,

1996 • 60 citations

Endothelium‐dependent relaxation of rabbit middle cerebral artery to a histamine H3‐agonist is reduced by inhibitors of nitric oxide and prostacyclin synthesis

1992 • 60 citations

Stereoselectivity of the histamine H3-presynaptic autoreceptor

1985 • 60 citations

Synergism between histamine H1- and H2-receptors in the cAMP response in guinea pig brain slices: effects of phorbol esters and calcium.

1988 • 59 citations

[125I]Iodoproxyfan and Related Compounds: A Reversible Radioligand and Novel Classes of Antagonists with High Affinity and Selectivity for the Histamine H3 Receptor

1996 • 59 citations

A study of the histamine H2‐receptor mediating relaxation of the parenchymal lung strip preparation of the guinea‐pig

1985 • 58 citations

INTRODUCTION TO ANTIHISTAMINE AGENTS AND ANTERGAN DERIVATIVES

1950 • 57 citations

Basal and stimulated formation and release of L-arginine-derived nitrogen oxides from cultured endothelial cells.

1990 • 57 citations

Synergy between the inositol phosphate responses to transfected human adenosine A1‐receptors and constitutive P2‐purinoceptors in CHO‐K1 cells

1995 • 56 citations

The role of calcium in the regulation of cyclic nucleotide levels in brain slices of rat and guinea pig

1978 • 56 citations

Histamine Receptors and Cyclic Nucleotides

1982 • 56 citations

[3H]Doxepin interactions with histamine H1-receptors and other sites in guinea pig and rat brain homogenates

1981 • 56 citations

Pharmacological specificity of brain histamine H2-receptors differs in intact cells and cell-free preparations

1980 • 55 citations

Regulation of the human histamine H1 receptor stably expressed in Chinese hamster ovary cells

1996 • 55 citations

(Imidazolylphenyl)formamidines. A structurally novel class of potent histamine H2 receptor antagonists

1984 • 55 citations

Restoration by histamine of the calcium-dependent electrical and mechanical response in the guinea-pig papillary muscle partially depolarized by potassium

1976 • 55 citations

Mutual interaction of histamine H3-receptors and ?2-adrenoceptors on noradrenergic terminals in mouse and rat rain cortex

1992 • 55 citations

Stable Expression of Human H1‐histamine‐receptor cDNA in Chinese Hamster Ovary Cells

1994 • 53 citations

Iodoaminopotentidine and related compounds: a new class of ligands with high affinity and selectivity for the histamine H2 receptor

1992 • 53 citations

The histamine H3 receptor: a general presynaptic histaminergic regulatory system?

1989 • 53 citations

Histamine depolarizes rat medial vestibular nucleus neurons recorded intracellularly in vitro

1990 • 52 citations

Binding of [3H]cimetidine to rat brain tissue

1980 • 52 citations

Biochemical characterization of histamine-sensitive adenylate cyclase in mammalian brain

1977 • 51 citations

Affinities of Histamine H1‐Antagonists in Guinea Pig Brain: Similarity of Values Determined from [3H]Mepyramine Binding and from Inhibition of a Functional Response

1981 • 51 citations

Synthesis, X-ray Crystallography, and Pharmacokinetics of Novel Azomethine Prodrugs of (R)-.alpha.-Methylhistamine: Highly Potent and Selective Histamine H3 Receptor Agonists

1995 • 50 citations

Histamine homologues discriminating between two functional H3 receptor assays. Evidence for H3 receptor heterogeneity?.

1996 • 50 citations

Histamine activates H1-receptors to induce cytosolic free calcium transients in cultured vascular smooth muscle cells from rat aorta

1986 • 49 citations

Characterization of histamine H-1 receptors on human peripheral lung

1985 • 49 citations

Lysine200 Located in the Fifth Transmembrane Domain of the Histamine H1 Receptor Interacts with Histamine but Not with All H1 Agonists

1995 • 49 citations

The first radiolabeled histamine H3 receptor antagonist, [125I]iodophenpropit: Saturable and reversible binding to rat cortex membranes

1992 • 48 citations

Inhibition of electrically evoked contractions of guinea-pig ileum preparations mediated by the histamine H3 receptor

1990 • 48 citations

Effects of Antihistamine Compounds on the Adrenaline Liberation from the Suprarenals

1949 • 47 citations

The in vivo pharmacological profile of histamine (H1) antagonists in the rat

1982 • 47 citations

Hypersensitivity to histamine in the guinea-pig brain: Microiontophoretic and biochemical studies

1978 • 46 citations

Histamine excites pedunculopontine neurones in guinea pig brainstem slices

1990 • 46 citations

Potencies of antagonists chemically related to iodoproxyfan at histamine H3 receptors in mouse brain cortex and guinea-pig ileum: evidence for H3 receptor heterogeneity?

1996 • 46 citations

Pharmacological and Functional Characterisation of the Wild—Type and Site—Directed Mutants of the Human H1Histamine Receptor Stably Expressed in CHO Cells

1995 • 46 citations

Pharmacological properties of histamine-sensitive adenylate cyclase from mammalian brain.

1979 • 45 citations

High-affinity binding of [3H]doxepin to histamine H1-receptors in rat brain: Possible identification of a subclass of histamine H1-receptors

1982 • 45 citations

Evidence that histamine and carbachol may open the same ion channels in longitudinal smooth muscle of guinea‐pig ileum

1981 • 45 citations

A Novel Series of (Phenoxyalkyl)imidazoles as Potent H3-Receptor Histamine Antagonists

1996 • 45 citations

The H1 receptor agonist 2-(3-chlorophenyl)histamine activates Gi proteins in HL-60 cells through a mechanism that is independent of known histamine receptor subtypes.

1994 • 44 citations

Histamine and its lymphocyte-selective derivatives as immune modulators

1987 • 44 citations

Is there a difference in the affinity of histamine H1 receptor antagonists for CNS and peripheral receptors? An in vitro study

1993 • 44 citations

Membrane properties, response to amines and to tetanic stimulation of hippocampal neurons in the genetically epileptic mutant mouse tottering

1988 • 44 citations

Absence of an effect of terfenadine on guinea pig brain histamine H1-receptors in vivo determined by receptor binding techniques.

1982 • 43 citations

Solubilization and Characterization of Histamine H1 receptors in brain.

1982 • 43 citations

Differential effect of sodium ions and guanine nucleotides on the binding of thioperamide and clobenpropit to histamine H3‐receptors in rat cerebral cortical membranes

1995 • 43 citations

Regulation of [Ca2+]i by secretagogue stimulation of canine gastric parietal cells

1992 • 43 citations

[3H]‐thioperamide as a radioligand for the histamine H3 receptor in rat cerebral cortex

1996 • 43 citations

Molecular Cloning of the Guinea-Pig Histamine H1 Receptor Gene

1993 • 42 citations

Effects of histamine on dentate granule cells in vitro

1990 • 42 citations

Tricyclic antidepressants: Potent blockade of histamine H1 receptors of guinea pig ileum

1979 • 42 citations

Histamine H3 receptors regulate acetylcholine release from the guinea pig ileum myenteric plexus

1991 • 42 citations

Cerebral Circulation and Histamine: 1. Participation of Vascular H1- and H2-Receptors in Vasodilatatory Responses to Carotid Arterial Infusion

1981 • 42 citations

Receptor autoradiography with 11C and [3H]-labelled ligands visualized by imaging plates

1992 • 42 citations

Characterization of histamine H3 receptors inhibiting 5-HT release from porcine enterochromaffin cells: Further evidence for H3 receptor heterogeneity

1994 • 42 citations

Histamine hyperpolarizes hippocampal neurones in vitro

1981 • 42 citations

Characteristics of the Mouse Genomic Histamine H1 Receptor Gene

1996 • 41 citations

A comparison of some of the pharmacological properties of etintidine, a new histamine H2-receptor antagonist, with those of cimetidine, ranitidine and tiotidine.

1983 • 41 citations

GABA, benzodiazepine and histamine-H1 receptors in the guinea pig cerebellum: effects of kainic acid injections studied by autoradiographic methods

1981 • 41 citations

Cloning, RNA Expression, and Chromosomal Location of a Mouse Histamine H2 Receptor Gene

1996 • 41 citations

Histamine H1-receptor-mediated cyclic GMP production in guinea-pig lung tissue is an l-arginine-dependent process

1991 • 40 citations

The acute effects of acrivastine (BW825C), a new antihistamine, compared with triprolidine on measures of central nervous system performance and subjective effects

1985 • 40 citations

Histamine-induced negative inotropism: mediation by H1-receptors.

1978 • 40 citations

Histamine receptors in brain as targets for tricyclic antidepressants

1981 • 40 citations

Homologs of Histamine as Histamine H3 Receptor Antagonists: A New Potent and Selective H3 Antagonist, 4(5)-(5-Aminopentyl)-1H-imidazole

1995 • 40 citations

Induction of prostacyclin biosynthesis is closely associated with increased guanosine 3',5'-cyclic monophosphate accumulation in cultured human endothelium.

1986 • 40 citations

Design of Potent Non-Thiourea H3-Receptor Histamine Antagonists

1995 • 39 citations

Chromosomal localization of the human histamine H1-receptor gene

1994 • 39 citations

Properties of 3H-cimetidine binding in rat brain membrane fractions

1980 • 39 citations

Differential effects of extracellular calcium removal and nonspecific effects of Ca2+ antagonists on acid secretory activity in isolated gastric glands

1985 • 39 citations

Effect of a new potent H2-blocker, 3-[[[2-(diaminomethylene)amino]-4-thiazolyl]methyl]thio]-N2-sulfamoyl propionamidine (YM-11170), on gastric secretion, ulcer formation and weight of male accessory sex organs in rats.

1982 • 39 citations

Characterization of histamine receptors mediating the stimulation of cyclic AMP accumulation in rabbit cerebral cortical slices

1985 • 38 citations

The binding of [3H]‐tiotidine to homogenates of guinea‐pig lung parenchyma

1985 • 38 citations

Characterization of [3H]mepyramine binding to the longitudinal muscle of guinea pig small intestine.

1981 • 38 citations

A Novel Pyrrolidine Analog of Histamine as a Potent, Highly Selective Histamine H3 Receptor Agonist

1995 • 38 citations

Two Distinct Pathways for Histamine H2 Receptor Down-regulation

1996 • 37 citations

The binding of doxepin to histamine H1‐preceptors in guinea‐pig and rat brain

1985 • 37 citations

Characterization of histamine receptors in cat cerebral arteries in vitro and in situ.

1983 • 37 citations

Histamine modulates calcium current in guinea pig ventricular myocytes.

1988 • 36 citations

The binding of conformationally restricted antihistamines to histamine receptors

1973 • 36 citations

Tyrosine Hydroxylase Phosphorylation in Bovine Adrenal Chromaffin Cells: The Role of Intracellular Ca2+ in the Histamine H1 Receptor‐Stimulated Phosphorylation of Ser8, Ser19, Ser31, and Ser40

1995 • 36 citations

Synthesis, absolute configuration, stereoselectivity, and receptor selectivity of (.alpha.R,.beta.S)-.alpha.,.beta.-dimethylhistamine. A novel highly potent histamine H3 receptor agonist

1992 • 35 citations

Thapsigargin potentiates histamine-stimulated HCl secretion in gastric parietal cells but does not mimic cholinergic responses.

1991 • 35 citations

[125I]iodobolpyramine, a highly sensitive probe for histamine H1-receptors in guinea-pig brain

1986 • 35 citations

Inotropic Effects of Histamine in Human Myocardium

1984 • 35 citations

Modulation of acetylcholine, capsaicin and substance P effects by histamine H3 receptors in isolated perfused rabbit lungs

1995 • 35 citations

Histamine-induced hydrolysis of polyphosphoinositides in guinea-pig ileum and brain

1986 • 35 citations

Two novel, potent and selective histamine H3 receptor agonists

1992 • 34 citations

Imaging histamine H1 receptors in the living human brain with carbon-11-pyrilamine.

1991 • 34 citations

Adenosine promotes histamine H1-mediated negative chronotropic and inotropic effects on human atrial myocardium.

1988 • 33 citations

Histamine H3 receptor-mediated inhibition of gastric acid secretion in conscious dogs

1993 • 33 citations

Pharmacological characterization of histamine receptors in the human temporal artery.

1989 • 33 citations

Antidepressants are weak competitive antagonists of histamine H2 receptors in dissociated brain tissue

1983 • 33 citations

Autoregulation of histamine synthesis through H3 receptors in isolated fundic mucosal cells

1993 • 32 citations

Characterization of histamine H1-receptor binding peptides in guinea pig brain using [125I]iodoazidophenpyramine, an irreversible specific photoaffinity probe.

1988 • 32 citations

Cloning and structure-function of the H2 histamine receptor

1991 • 32 citations

Binding Characteristics of a Histamine H3-Receptor Antagonist, (3H)S-Methylthioperamide: Comparison with (3H)(R).ALPHA.-Methylhistamine Binding to Rat Tissues.

1994 • 32 citations

Maximum entropy calculation of the island-size distribution for a simple diffraction profile

1990 • 32 citations

The effects of derivatives of histamine on natural suppressor cells.

1986 • 32 citations

3H-cimetidine and the H2-receptor

1983 • 31 citations

Histamine analogues. 33rd communication: 2-phenylhistamines with high histamine H1-agonistic activity

1990 • 31 citations

Histamine Affects Release and Biosynthesis of Opioid Peptides Primarily via H1‐Receptors in Bovine Chromaffin Cells

1987 • 31 citations

pH-dependent modulation of N-methyl-d-aspartate receptor-mediated synaptic currents by histamine in rat hippocampus in vitro

1995 • 31 citations

Gastric H+ secretion: histamine (cAMP-mediated) activation of protein phosphorylation

1988 • 30 citations

Intracellular histamine and liver regeneration: High affinity binding of histamine to chromatin, low affinity binding to matrix, and depletion of a nuclear storage pool following partial hepatectomy

1992 • 30 citations

Contractile elements in endothelial cells as potential targets for drug action

1986 • 30 citations

pH‐dependent Facilitation of Synaptic Transmission by Histamine in the CA1 Region of Mouse Hippocampus

1995 • 30 citations

Drugs from emasculated hormones: The principle of syntopic antagonism

1989 • 30 citations

Cyclic nucleotides and contraction/relaxation in airway muscle: H1 and H2 agonists and antagonists.

1980 • 30 citations

Characterization of functional histamine H1 receptors on a cultured smooth muscle cell line

1988 • 29 citations

Histamine H1‐Receptor in Heart: Unique Electrophoretic Mobility and Autoradiographic Localization

1990 • 29 citations

Differential effects of histamine mediated by histamine H1- and H2-receptors on contractility, spontaneous rate and cyclic nucleotides in the rabbit heart

1988 • 28 citations

Increased Permeability Associated with Dilatation of Endothelial Cell Junctions Caused by Histamine in Intimal Explants from Bovine Pulmonary Artery

1984 • 28 citations

Cloning of the H1 histamine receptor

1992 • 28 citations

Inotropic, electrophysiological and biochemical responses to histamine in rabbit papillary muscles: evidence for coexistence of H1- and H2-receptors.

1990 • 27 citations

Histamine interaction on surface recognition sites of H2‐type in parietal and non‐parietal cells isolated from the guinea pig stomach

1982 • 25 citations

Characterisation of the Binding of the Histamine H3 Receptor Agonist [3H](R)-Alpha Methyl Histamine to Homogenates of Rat and Guinea-Pig Cortex

1991 • 25 citations

Studies on the mechanism of histamine-induced release of noradrenaline and 5-hydroxytryptamine from slices of rat cerebral cortex

1988 • 25 citations

Studies on histamine H2 receptors coupled to cardiac adenylate cyclase. Blockade by H2 and H1 receptor antagonists.

1979 • 25 citations

ATP-sensitive K+ channels mediate regulation of substance P release via the prejunctional histamine H3 receptor

1995 • 24 citations

Histamine receptor-dependent and/or -independent activation of guanine nucleotide-binding proteins by histamine and 2-substituted histamine derivatives in human leukemia (HL-60) and human erythroleukemia (HEL) cells

1995 • 24 citations

High affinity histamine H3 receptors regulate ACTH release by AtT-20 cells

1992 • 24 citations

Histamine H2-binding on guinea pig cerebral cortex

1986 • 23 citations

2 Histamine Receptors in the Mammalian Central Nervous System: Biochemical Studies

1987 • 23 citations

Characteristics of histamine H1 receptors on HeLa cells

1993 • 23 citations

Photoaffinity Labeling and Electrophoretic Identification of the H1‐Receptor: Comparison of Several Brain Regions and Animal Species

1989 • 23 citations

Histamine-stimulated phosphoinositide hydrolysis in developing rat brain.

1987 • 23 citations

Histamine H1‐receptor‐mediated inositol phospholipid hydrolysis in DDT1MF‐2 cells: agonist and antagonist properties

1993 • 22 citations

Kinetic studies on the mechanism by which histamine H1 receptors potentiate cyclic AMP accumulation in guinea pig cerebral cortical slices.

1988 • 22 citations

THE ACTION OF HISTAMINE ON HYDROCHLORIC ACID AND PEPSIN SECRETION IN MAN

1949 • 22 citations

The role of calcium in the cyclic AMP response to histamine in rabbit cerebral cortical slices

1987 • 22 citations

Interaction of histamine with gastric mucosal cells. Effect of histamine H2 antagonists on binding and biological response.

1982 • 21 citations

Histamine-operated calcium channels in intestinal smooth muscle of the guinea-pig

1987 • 21 citations

Histamine H2-binding studies in the guinea-pig brain

1984 • 21 citations

Studies on histamine H2 receptors coupled to cardiac adenylate cyclase Effects of guanylnucleotides and structural requirements for agonist activity

1979 • 21 citations

Characterization of a Digitonin‐Solubilized Bovine Brain H3 Histamine Receptor Coupled to a Guanine Nucleotide‐Binding Protein

1992 • 21 citations

Developments in histamine H1-receptor agonists

1995 • 20 citations

Hypothermia-induced potentiation of histamine H2-receptor-mediated relaxation and cyclic AMP increase in the isolated mesenteric artery of the rabbit

1979 • 20 citations

Enhancement of Histamine H1‐Receptor Agonist Activity by 1,4‐Dithiothreitol in Guinea‐Pig Cerebellum and Cerebral Cortex

1986 • 20 citations

Action of neuroleptic agents on histamine-sensitive adenylate cyclase in rabbit cerebral cortex

1976 • 20 citations

Histamine activates proenkephalin A mRNA but not phenylethanolamine N-methyltransferase mRNA expression in cultured bovine adrenal chromaffin cells

1989 • 19 citations

Adenosine selectively attenuates H2- and beta-mediated cardiac responses to histamine and norepinephrine: an unmasking of H1- and alpha-mediated responses.

1984 • 19 citations

Characterisation of the specific binding of the histamine H3 receptor antagonist radioligand [3H]GR168320

1996 • 19 citations

Temperature‐dependence of the kinetics of the binding of [3H]‐(+)‐N‐methyl‐4‐methyldiphenhydramine to the histamine H1‐receptor: comparison with the kinetics of [3H]‐mepyramine

1988 • 19 citations

Characterization of histamine H1 binding sites on human T lymphocytes by means of 125I-iodobolpyramine. Preferential expression of H1 receptors on CD8 T lymphocytes.

1990 • 18 citations

Histamine receptors in adipose tissue: involvement of cyclic adenosine monophosphate and the H2-receptor in the lipolytic response to histamine in isolated canine fat cells.

1975 • 18 citations

Cerebellar histamine-H1 receptor distribution: An autoradiographic study of purkinje cell degeneration, staggerer, weaver and reeler mutant mouse strains

1986 • 18 citations

Biochemical characterization of histamine H1 receptors in bovine adrenal medulla

1991 • 18 citations

Pharmacological and immunological characterization of N-methyl-D-aspartate receptors in human NT2-N neurons.

1996 • 17 citations

Patch clamp study of histamine activated potassium currents on rabbit olfactory bulb neurons

1995 • 17 citations

Endogenous expression of histamine H1 receptors functionally coupled to phosphoinositide hydrolysis in C6 glioma cells: regulation by cyclic AMP

1994 • 17 citations

Phencyclidine blocks histamine H3-receptors in rat brain

1988 • 17 citations

Selective enhancement of histamine H1‐receptor responses in guinea‐pig ileal smooth muscle by 1,4‐dithiothreitol

1986 • 17 citations

Structural and functional analysis of the canine histamine H2 receptor by site-directed mutagenesis: N-glycosylation is not vital for its action

1995 • 16 citations

Effects of histamine on mechanical performance and biochemical and electrical activity in the heart of monkeys (Macaca fuscata)

1983 • 16 citations

Pharmacological properties of histamine-sensitive adenylate cyclase from guinea pig cardiac ventricular muscle.

1979 • 16 citations

A Study on the Induction of Histidine Decarboxylase in Tumor-bearing Rat

1970 • 16 citations

Drugs from Emasculated Hormones: The Principle of Syntopic Antagonism (Nobel Lecture)

1989 • 16 citations

Evidence for low brain penetration by the H1-receptor antagonist temelastine (SK & F 93944)

1987 • 15 citations

Serotonin and histamine receptor-mediated inhibition of serotonin and noradrenaline release in rat brain cortex under nimodipine treatment

1991 • 15 citations

Effects of Ca2+ channel antagonists and ryanodine on H1-receptor mediated electromechanical response to histamine in guinea-pig left atria

1988 • 15 citations

Response of the histamine h2-receptor in brain to antidepressant drugs.

1982 • 14 citations

Re-examination of [3H]mepyramine binding assay for histamine H1 receptor using quinine

1992 • 14 citations

Regulation of [Ca2+]i rise activated by doxepin-sensitive H1-histamine receptors in jurkat cells, cloned human T lymphocytes

1996 • 13 citations

Temporal changes in the calcium‐dependence of the histamine H1‐receptor‐stimulation of cyclic AMP accumulation in guinea‐pig cerebral cortex

1989 • 13 citations

EXCITATION OF BRAIN STEM NEURONS BY NORADRENALINE AND HISTAMINE

1990 • 13 citations

Purification of [3H]mepyramine receptor from rat liver and its amino acid sequence homology with debrisoquine 4-hydroxylase cytochrome P-450

1990 • 12 citations

Immunohistochemical localization of histamine-stimulated increases in cyclic GMP in guinea pig lung.

1987 • 12 citations

The nature of the binding of [3H]mepyramine to homogenates of guinea-pig cerebral cortex at different [3H]ligand concentrations

1983 • 12 citations

Structure-Activity Relationships of Histamine H2-Agonists, a New Class of Positive Inotropic Drugs

1991 • 11 citations

Actions of nizatidine on the rat uterus, dog stomach and experimentally induced gastric lesions.

1986 • 11 citations

High, Stable Expression of the Bovine Histamine H1-Receptor Coupled to [Ca2+]i Mobilization in CHO-K1 Cells

1993 • 10 citations

Differential effects of histamine on the N-methyl-d-aspartate channel in hippocampal slices and cultures

1996 • 10 citations

Effect of the tachykinin antagonist, [abetd-Pro4, abetd-Trp7,9,10] substance P-(4?11), on tachykinin- and histamine-induced inositol phosphate generation in intestinal smooth muscle

1987 • 10 citations

Histamine analogues. 32nd communication: synthesis and pharmacology of sopromidine, a potent and stereoselective isomer of the achiral H2-agonist impromidine

1989 • 10 citations

Interaction of mianserin, amitriptyline and haloperidol with guinea pig cerebral histamine H2 receptors studied with [125I]iodoaminopotentidine

1991 • 10 citations

Effects of iodoproxyfan, a potent and selective histamine H3 receptor antagonist, onα 2 and 5-HT3 receptors

1995 • 8 citations

Histamine-sensitive adenylate cyclase in monkey brain

1982 • 8 citations

Histamine H[3]-receptors inhibit neurogenic microvascular leakage in airways

1990 • 8 citations

Characteristics of [3H]mepyramine binding in DDT1MF-2 cells: Evidence for high affinity binding to a functional histamine H1 receptor

1994 • 7 citations

N G-Nitro-<scp>l</scp>-arginine methyl ester inhibits the effect of an H3-histaminergic receptor agonist on NANC contraction in guinea-pig perfused bronchioles

1994 • 7 citations

Correlation between histamine-induced neuronal excitability and activation of adenylate cyclase in the guinea pig hippocampus

1984 • 7 citations

Chemistry of Anti-H1 Histamine Antagonists

1978 • 7 citations

Digitonin-solubilized histamine H1-receptors bind to polyethylenimine-treated glass-fibre filters

1988 • 5 citations

Lack of haemodynamic effects of nitric oxide on post‐capillary pulmonary hypertension induced by acute sino‐aortic denervation

1997 • 5 citations

Mechanical responses of cultured pre- and neonatal myocytes

1979 • 5 citations

Construction of a Novel Bifunctional Biogenic Amine Receptor by Two Point Mutations of the H2-Histamine Receptor

1995 • 4 citations

Site-directed mutagenesis of the histamine H[1] receptor : roles of aspartic acid[107], asparagine[198] and threonine[194]

1995 • 2 citations

Synthesis and histamine H2-receptor activity of heterocyclic impromidine analogues.

1992 • 2 citations

Histamine H(1)-Receptor-Mediated Calcium Influx in Ddt(1)Mf-2 Cells

1992 • 1 citations

The Effect of Lipophilic Substituents on the H2‐Histaminergic Activity of Some Close Analogues of Impromidine

1992 • 1 citations

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International Union of Pharmacology. XIII. Classification of histamine receptors. (1997) – PubMed | Metascience Observatory Explorer