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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1-3
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pubmed:dateCreated |
2008-8-12
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pubmed:abstractText |
The recently cloned histamine H(4) receptor is expressed predominantly in haematopoietic cells and has been found to modulate the function of mast cells, eosinophils, dendritic cells and T lymphocytes. It represents an attractive target for pharmacological interventions against a number of inflammatory and autoimmune disorders. In the present work we used two-electrode voltage-clamp to demonstrate histamine H(4) receptor modulation of G protein-coupled inward rectifier potassium (GIRK) channels heterologously expressed in Xenopus oocytes. In accordance with earlier findings in other effector systems, full agonism by histamine and (R)-alpha-methylhistamine, partial agonism by clobenpropit and inverse agonism by thioperamide were observed. Furthermore, in oocytes injected with low amounts of receptor cRNA, clobenpropit apparently acted as a neutral antagonist. We also used the high temporal resolution afforded by this system to study the differential time courses of response deactivation upon ligand washout for clobenpropit and (R)-alpha-methylhistamine. GIRK channels represent a novel effector system for histamine H(4) receptor modulation, which may be of physiological relevance and prove useful in the development of compounds targeting this receptor.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/G Protein-Coupled...,
http://linkedlifedata.com/resource/pubmed/chemical/HRH4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Histamine Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Histamine Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Methylhistamines,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, G-Protein-Coupled,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Histamine,
http://linkedlifedata.com/resource/pubmed/chemical/Thiourea,
http://linkedlifedata.com/resource/pubmed/chemical/alpha-methylhistamine,
http://linkedlifedata.com/resource/pubmed/chemical/clobenpropit,
http://linkedlifedata.com/resource/pubmed/chemical/thioperamide
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0014-2999
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
4
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pubmed:volume |
591
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
52-8
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pubmed:meshHeading |
pubmed-meshheading:18582456-Animals,
pubmed-meshheading:18582456-Electrophysiology,
pubmed-meshheading:18582456-G Protein-Coupled Inwardly-Rectifying Potassium Channels,
pubmed-meshheading:18582456-Histamine Agonists,
pubmed-meshheading:18582456-Histamine Antagonists,
pubmed-meshheading:18582456-Humans,
pubmed-meshheading:18582456-Imidazoles,
pubmed-meshheading:18582456-Methylhistamines,
pubmed-meshheading:18582456-Oocytes,
pubmed-meshheading:18582456-Patch-Clamp Techniques,
pubmed-meshheading:18582456-Piperidines,
pubmed-meshheading:18582456-Receptors, G-Protein-Coupled,
pubmed-meshheading:18582456-Receptors, Histamine,
pubmed-meshheading:18582456-Thiourea,
pubmed-meshheading:18582456-Xenopus
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pubmed:year |
2008
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pubmed:articleTitle |
Electrophysiology-based analysis of human histamine H(4) receptor pharmacology using GIRK channel coupling in Xenopus oocytes.
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pubmed:affiliation |
Department of Neuroscience, Karolinska Institutet, SE-117 77 Stockholm, Sweden.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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