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Evaluation of Histamine H1-, H2-, and H3-Receptor Ligands at the Human Histamine H4 Receptor: Identification of 4-Methylhistamine as the First Potent and Selective H4 Receptor Agonist
The histamine H4 receptor (H4R) is involved in the chemotaxis of leukocytes and mast cells to sites of inflammation and is suggested to be a potential drug target for asthma and allergy. So far,Expand
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Qualitative determination of false-positive effects in the acetylcholinesterase assay using thin layer chromatography.
A method has been developed to determine the false-positive effects on acetylcholinesterase inhibition in the TLC assay based on Ellman's method. Various aldehydes and amines have been tested inExpand
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Dual Efficacy of Delta Opioid Receptor-Selective Ligands for Ethanol Drinking and Anxiety
Alcoholism and anxiety disorders have a huge impact on society and afflict 17.6 million and 40 million people in the United States, respectively. A strong comorbidity exists between alcoholism andExpand
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The δ<ce:inf loc=post>1</ce:inf> Opioid Receptor Is a Heterodimer That Opposes the Actions of the δ<ce:inf loc=post>2</ce:inf> Receptor on Alcohol Intake
BACKGROUND Opioid receptors are clinically important targets for both pain and alcohol abuse. Three opioid receptors have been cloned: mu, delta, and kappa, all of which effect alcohol consumption inExpand
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Opioid-receptor-heteromer-specific trafficking and pharmacology.
Homomerization and heteromerization of 7 transmembrane spanning (7TM)/G-protein-coupled receptors (GPCRs) have been an important field of study. Whereas initial studies were performed in artificialExpand
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Cloning and characterization of dominant negative splice variants of the human histamine H4 receptor.
The H(4)R (histamine H(4) receptor) is the latest identified member of the histamine receptor subfamily of GPCRs (G-protein-coupled receptors) with potential functional implications in inflammatoryExpand
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Novel Screening Assay for the Selective Detection of G-Protein-Coupled Receptor Heteromer Signaling
Drugs targeting G-protein-coupled receptors (GPCRs) make up more than 25% of all prescribed medicines. The ability of GPCRs to form heteromers with unique signaling properties suggests an entirelyExpand
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Distinctive modulation of ethanol place preference by delta opioid receptor-selective agonists.
BACKGROUND Naltrexone is one of the few drugs approved by the Federal Drug Administration for the treatment of alcoholism. However, naltrexone is only effective in a subpopulation ofExpand
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Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
We describe the structure-activity relationships for a series of ligands structurally related to the recently identified (5-chloro-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone (1) as histamineExpand
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Oligomerization of Recombinant and Endogenously Expressed Human Histamine H4 Receptors
In this study, we report the homo- and hetero-oligomerization of the human histamine H4R by both biochemical (Western blot and immobilized metal affinity chromatography) and biophysicalExpand
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