Histamine H1-receptors in HL-60 monocytes are coupled to Gi-proteins and pertussis toxin-insensitive G-proteins and mediate activation of Ca2+ influx without concomitant Ca2+ mobilization from intracellular stores

URN zum Zitieren dieses Dokuments:

urn:nbn:de:bvb:355-epub-233016 Copy

DOI zum Zitieren dieses Dokuments:

10.5283/epub.23301 Copy

Seifert, Roland ; Grünbaum, L. ; Schultz, Günter

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Veröffentlichungsdatum dieses Volltextes: 26 Jan 2012 08:18

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Alternative Links zum Volltext:Pubmed

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Details

Dokumentenart:	Artikel
Titel eines Journals oder einer Zeitschrift:	Naunyn-Schmiedeberg's archives of pharmacology
Verlag:	Springer
Band:	349
Nummer des Zeitschriftenheftes oder des Kapitels:	4
Seitenbereich:	S. 355-361
Datum:	1994
Institutionen:	Chemie und Pharmazie > Institut für Pharmazie > Lehrstuhl Pharmakologie und Toxikologie (Prof. Schlossmann, ehemals Prof. Seifert)
Identifikationsnummer:	Wert Typ 8058107 PubMed-ID
Klassifikation:	Notation Art Adenosine Diphosphate Ribose/metabolism MESH Calcium/metabolism MESH Cell Line MESH GTP-Binding Proteins/metabolism MESH Histamine/pharmacology MESH Histamine Agonists/pharmacology MESH Humans MESH Imidazoles/pharmacology MESH Monocytes/metabolism MESH N-Formylmethionine Leucyl-Phenylalanine/pharmacology MESH Oxygen Consumption/drug effects MESH Pertussis Toxin MESH Platelet Aggregation Inhibitors/pharmacology MESH Receptors, Histamine H1/metabolism MESH Virulence Factors, Bordetella/pharmacology MESH
Dewey-Dezimal-Klassifikation:	600 Technik, Medizin, angewandte Wissenschaften > 610 Medizin 600 Technik, Medizin, angewandte Wissenschaften > 615 Pharmazie
Status:	Veröffentlicht
Begutachtet:	Ja, diese Version wurde begutachtet
An der Universität Regensburg entstanden:	Unbekannt / Keine Angabe
Dokumenten-ID:	23301

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Zusammenfassung

The results of binding studies suggest the presence of histamine H1-receptors in human monocytes, but it is not known whether these receptors are functionally active. This prompted us to study the effects of histamine (HA) on cytosolic Ca2+ concentration ([Ca2+]i) and superoxide anion (O2-) formation in HL-60 cells differentiated towards monocytes with 1 alpha,25-dihydroxycholecalciferol. In ...

Zusammenfassung

The results of binding studies suggest the presence of histamine H1-receptors in human monocytes, but it is not known whether these receptors are functionally active. This prompted us to study the effects of histamine (HA) on cytosolic Ca2+ concentration ([Ca2+]i) and superoxide anion (O2-) formation in HL-60 cells differentiated towards monocytes with 1 alpha,25-dihydroxycholecalciferol. In HL-60 monocytes, HA increased [Ca2+]i with a half-maximal effect at 8 microM and a maximum at 30-100 microM. Pertussis toxin (PTX) partially inhibited the stimulatory effects of HA on [Ca2+]i. Betahistine, a weak partial H1-receptor agonist, also increased [Ca2+]i, whereas H2- and H3-receptor agonists were ineffective. H1- but not H2- and H3-receptor antagonists inhibited HA-induced rises in [Ca2+]i. HA-induced rises in [Ca2+]i were desensitized in a homologous manner and were also inhibited by the activator of protein kinase C, 4 beta-phorbol 12-myristate 13-acetate. Various protein kinase C inhibitors did not interfere with homologous desensitization. The stimulatory effects of HA on [Ca2+]i were completely dependent on the presence of extracellular Ca2+ and were inhibited by the blocker of non-selective cation (NSC) channels, 1-(beta-[3-(4-methoxyphenyl)propoxyl]-4-methoxyphenethyl)-1 H-imidazole hydrochloride (SK & F 96365). HA was much less effective than the chemotactic peptide, N-formyl-L-methionyl-L-leucyl-L-phenylalanine (fMLP), to induce rises in [Ca2+]i. Unlike fMLP, HA did not activate O2- formation.(ABSTRACT TRUNCATED AT 250 WORDS)

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