The histamine H3 receptor and its ligands (Q34483311)

2 August 2017

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title

The histamine H3 receptor and its ligands (English)

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2 August 2017

Stark H

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2 August 2017

Arrang JM

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2 August 2017

Ligneau X

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2 August 2017

Garbarg M

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2 August 2017

Ganellin CR

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2 August 2017

Schwartz JC

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2 August 2017

Schunack W

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2 August 2017

publication date

1 January 2001

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Progress in medicinal chemistry

2 August 2017

published in

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2 August 2017

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2 August 2017

page(s)

279-308

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Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor

2 August 2017

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7 January 2021

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7 January 2021

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7 January 2021

Modulation of neurotransmitter release via histamine H3 heteroreceptors

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7 January 2021

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

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7 January 2021

Characterization of a digitonin-solubilized bovine brain H3 histamine receptor coupled to a guanine nucleotide-binding protein

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7 January 2021

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

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7 January 2021

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

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7 January 2021

Autoregulation of histamine release in brain by presynaptic H3-receptors

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7 January 2021

Histamine modulates high-voltage-activated calcium channels in neurons dissociated from the rat tuberomammillary nucleus

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7 January 2021

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

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7 January 2021

Prejunctional histamine H3-receptors inhibit electrically evoked endogenous noradrenaline overflow in the portal vein of freely moving rats

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7 January 2021

Histamine H3 receptor-mediated inhibition of noradrenaline release in the human brain

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7 January 2021

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

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7 January 2021

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

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7 January 2021

Histamine H3-receptor activation inhibits dopamine synthesis in rat striatum

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7 January 2021

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

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7 January 2021

Functional relationships between sensory nerve fibers and mast cells of dura mater in normal and inflammatory conditions

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7 January 2021

Effect of blockade of postsynaptic H1 or H2 receptors or activation of presynaptic H3 receptors on catecholamine-induced stimulation of ACTH and prolactin secretion

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Importance of histamine in the cytokine network in the lung through H2 and H3 receptors: stimulation of IL-10 production

1 reference

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7 January 2021

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

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

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

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7 January 2021

Characterization of Histamine Release from the Rat Hypothalamus as Measured by In Vivo Microdialysis

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7 January 2021

In vivo release of neuronal histamine in the hypothalamus of rats measured by microdialysis

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7 January 2021

Involvement of histaminergic neurons in arousal mechanisms demonstrated with H3-receptor ligands in the cat.

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7 January 2021

Effects of selective activation or blockade of the histamine H3 receptor on sleep and wakefulness

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Effects of thioperamide, a histamine H3 antagonist, on the step-through passive avoidance response and histidine decarboxylase activity in senescence-accelerated mice.

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Effects of thioperamide, a histamine H3-receptor antagonist, on a scopolamine-induced learning deficit using an elevated plus-maze test in mice

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Effects of clobenpropit (VUF-9153), a histamine H3-receptor antagonist, on learning and memory, and on cholinergic and monoaminergic systems in mice

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Improvement by FUB 181, a novel histamine H3-receptor antagonist, of learning and memory in the elevated plus-maze test in mice

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Endogenous histamine induces c-fos expression within paraventricular and supraoptic nuclei

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Responses of anterior pituitary hormones and hypothalamic histamine to blockade of histamine synthesis and to selective activation or inactivation of presynaptic histamine H3 receptors in stressed rats

1 reference

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7 January 2021

Role of Hypothalamic Histaminergic Neurons in Mediation of ACTH and Beta-Endorphin Responses to LPS Endotoxin in vivo

1 reference

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7 January 2021

Neuronal histamine in the hypothalamus suppresses food intake in rats

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7 January 2021

Hypothalamic neuronal histamine regulates feeding circadian rhythm in rats

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7 January 2021

Effects of intracerebroventricularly infused histamine and selective H1, H2 and H3 agonists on food and water intake and urine flow in Wistar rats

1 reference

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7 January 2021

Effect of thioperamide, a histamine H3 receptor antagonist, on electrically induced convulsions in mice

1 reference

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7 January 2021

Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Thioperamide, a selective histamine H3 receptor antagonist, protects against PTZ-induced seizures in mice

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7 January 2021

Medial vestibular nucleus in the guinea-pig: histaminergic receptors. II. An in vivo study

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7 January 2021

Actions of betahistine at histamine receptors in the brain

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7 January 2021

Betahistine dihydrochloride in the treatment of vertigo of peripheral vestibular origin A double-blind placebo-controlled study

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7 January 2021

Betahistine increases vestibular blood flow

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7 January 2021

H3-receptors control histamine release in human brain

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7 January 2021

HA autoreceptor assay with superfused slices of rat brain cortex and electrical stimulation

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7 January 2021

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

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7 January 2021

Novel partial agonists for the histamine H(3) receptor with high in vitro and in vivo activity

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7 January 2021

(Partial) agonist/antagonist properties of novel diarylalkyl carbamates on histamine H3 receptors.

1 reference

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7 January 2021

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

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7 January 2021

Effects of selected histamine H3 receptor antagonists on tele-methylhistamine levels in rat cerebral cortex

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7 January 2021

In vivo occupancy of histamine H3 receptors by thioperamide and (R)-alpha-methylhistamine measured using histamine turnover and an ex vivo labeling technique

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7 January 2021

Stereoselectivity of the histamine H3-presynaptic autoreceptor

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7 January 2021

The histamine H3 receptor agonist N alpha-methylhistamine produced by Helicobacter pylori does not alter somatostatin release from cultured rabbit fundic D-cells

1 reference

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7 January 2021

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

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7 January 2021

Synthesis, X-ray crystallography, and pharmacokinetics of novel azomethine prodrugs of (R)-alpha-methylhistamine: highly potent and selective histamine H3 receptor agonists

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7 January 2021

New potent azomethine prodrugs of the histamine H3-receptor agonist (R)-alpha-methylhistamine containing a heteroarylphenyl partial structure.

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7 January 2021

A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist

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7 January 2021

Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo

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7 January 2021

A new potent and selective histamine H3 receptor agonist, 4-(1H-imidazol-4-ylmethyl)piperidine

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7 January 2021

Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H-imidazole

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7 January 2021

Computer-Assisted Analysis of Histamine H2â and H3-Receptor Agonists

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7 January 2021

Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine

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7 January 2021

From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists

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7 January 2021

Novel histamine H3 receptor antagonists: synthesis and evaluation of formamidine and S-methylisothiourea derivatives

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7 January 2021

Heteroarylaminoethyl and heteroarylthioethyl imidazoles. Synthesis and H3-receptor affinity

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7 January 2021

Design of Potent Non-Thiourea H3-Receptor Histamine Antagonists

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7 January 2021

4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists

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7 January 2021

Novel H3 receptor antagonists. Sulfonamide homologs of histamine

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7 January 2021

Novel carbonic anhydrase isozymes I, II and IV activators incorporating sulfonyl-histamino moieties

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7 January 2021

Carbonic anhydrase activators - part 21. Novel activators of isozymes I, II and IV incorporating carboxamido and ureido histamine moieties

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7 January 2021

New analogs of burimamide as potent and selective histamine H3 receptor antagonists: the effect of chain length variation of the alkyl spacer and modifications of the N-thiourea substituent

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7 January 2021

Azines and Diazines as Potential Histamine H3‐Receptor Antagonists

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7 January 2021

Pyrazoles as potential histamine H3-receptor antagonists

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7 January 2021

4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: novel antagonists of the histamine H3 receptor

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7 January 2021

Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity

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7 January 2021

Development of chiral N-alkylcarbamates as new leads for potent and selective H3-receptor antagonists: synthesis, capillary electrophoresis, and in vitro and oral in vivo activity.

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7 January 2021

H3-receptor antagonists: synthesis and structure-activity relationships of para- and meta-substituted 4(5)-phenyl-2-[[2-[4(5)-imidazolyl]ethyl]thio]imidazoles

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7 January 2021

Synthesis and biological assays of new H3-antagonists with imidazole and imidazoline polar groups

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7 January 2021

4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity

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7 January 2021

A novel series of (phenoxyalkyl)imidazoles as potent H3-receptor histamine antagonists

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7 January 2021

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

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7 January 2021

Development of FUB 181, a selective histamine H3-receptor antagonist of high oral in vivo potency with 4-(omega-(arylalkyloxy)alkyl)-1H-imidazole structure

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Ciproxifan and chemically related compounds are highly potent and selective histamine H3-receptor antagonists

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Design, synthesis, and structure-activity relationships of acetylene-based histamine H3 receptor antagonists

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

General construction pattern of histamine H3-receptor antagonists: change of a paradigm

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Synthesis and histamine H3 receptor activity of 4-(n-alkyl)-1H-imidazoles and 4-(omega-phenylalkyl)-1H-imidazoles

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

The effect of haloperidol on the histaminergic neuron system in the rat brain.

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Intermediate affinity and potency of clozapine and low affinity of other neuroleptics and of antidepressants at H3 receptors

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Interaction of clozapine with the histamine H3 receptor in rat brain

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

The moderate affinity of clozapine at H3 receptors is not shared by its two major metabolites and by structurally related and unrelated atypical neuroleptics

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Synthesis of 1,2-benzisothiazole derivatives and investigation of their putative histaminergic activity

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Non-imidazole histamine H3 ligands. Part I. Synthesis of 2-(1-piperazinyl)- and 2-(hexahydro-1H-1,4-diazepin-1-yl)benzothiazole derivatives as H3-antagonists with H1 blocking activities

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Non-imidazole histamine H3 ligands, Part 2: New 2-substituted benzothiazoles as histamine H3 antagonists

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Synthesis of potent non-imidazole histamine H3-receptor antagonists

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

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

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

[125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Agonist and antagonist effects of histamine H3 receptor ligands on 5-HT3 receptor-mediated ion currents in NG108-15 cells

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Radiosynthesis and biodistribution of 123I-labeled antagonists of the histamine H3 receptor as potential SPECT ligands

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7 January 2021

Synthesis,in vitro pharmacology and radiosynthesis ofN-(cis-4-fluoromethylcycloyhexyl)-4-(1(H)-imidazol-4-yl)piperidine-11-thiocarbonamide (VUF 5000), a potential PET ligand for the histamine H3 receptor

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7 January 2021

Evaluation of [ 18 F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H 3 receptor

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7 January 2021

Therapeutic potential of histamine H3 receptor agonists and antagonists.

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7 January 2021

[The roles of histamine H3 receptors in the behavioral disorders and neuropsychopharmacological aspects of its ligands in the brain]

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7 January 2021

Functional relationship between mast cells and C-sensitive nerve fibres evidenced by histamine H3-receptor modulation in rat lung and spleen

1 reference

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7 January 2021

Histamine H3-receptor-mediated inhibition of calcitonin gene-related peptide release from cardiac C fibers. A regulatory negative-feedback loop

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7 January 2021

Histamine as a therapeutic alternative in migraine prophylaxis: a randomized, placebo-controlled, double-blind study

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https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

An update on histamine H3 receptors and gastrointestinal functions

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Effects of (R)-<alpha>-methylhistamine and its prodrug BP 2.94 on gastric mucosal lesions in cold/restraint stressed rats

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Gastric mucosal injury by nonsteroidal anti-inflammatory drugs is reduced by (R)-<alpha>-methylhistamine and its pro-drugs in the rat.

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

New aspects of the role of histamine in cardiovascular function: identification, characterization, and potential pathophysiological importance of H3receptors

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Neuronal histamine deficit in Alzheimer's disease

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Effects of histamine H3 receptor agonists and antagonists on cognitive performance and scopolamine-induced amnesia.

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Histamine neurons in human hypothalamus: Anatomy in normal and alzheimer diseased brains

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Inhibition of histamine versus acetylcholine metabolism as a mechanism of tacrine activity

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Thioperamide, a histamine H3 receptor antagonist, powerfully suppresses peptide YY-induced food intake in rats

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Pharmacological evaluation of an in vivo model of vestibular dysfunction in the rat.

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Effect of clobenpropit, a centrally acting histamine H3-receptor antagonist, on electroshock- and pentylenetetrazol-induced seizures in mice

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

The effects of histamine H3-receptor antagonists on amygdaloid kindled seizures in rats

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Histamine metabolites in cerebrospinal fluid of patients with chronic schizophrenia: their relationships to levels of other aminergic transmitters and ratings of symptoms

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

Effects of histamine H3 receptor ligands in experimental models of anxiety and depression

1 reference

https://api.crossref.org/works/10.1016%2FS0079-6468%2808%2970096-1

7 January 2021

10.1016/S0079-6468(08)70096-1

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