title: In vitro study of histamine and histamine receptor ligands influence on the adhesion of purified human eosinophils to endothelium.
abstract: It is a well-known fact that histamine is involved in eosinophil-dependent inflammatory responses including cellular chemotaxis and migration. Nevertheless, the relative role of histamine receptors in the mechanisms of eosinophils adhesion to endothelial cells is not known. Therefore the aim of presented study was to examine the effect of selective histamine receptors ligands on eosinophils adhesion to endothelium. For that purpose the highly purified human eosinophils have been isolated from the peripheral blood. The viability and functional integrity of isolated eosinophils have been validated in several tests. Histamine as well as 4-methylhistamine (selective H4 agonist) in concentration-dependent manner significantly increased number of eosinophils that adhere to endothelium. Among the selective histamine receptors antagonist or H1 inverse agonist only JNJ7777120 (histamine H4 antagonist) and thioperamide (dual histamine H3/H4 antagonist) had direct effect on eosinophils adhesion to endothelial cells. Antagonists of H1 (diphenhydramine, mepyramine) H2 (ranitidine and famotidine) and H3 (pitolisant) histamine receptors were ineffective. To the best of our knowledge, this is the first study to demonstrate that histamine receptor H4 plays a dominant role in histamine-induced eosinophils adhesion to endothelium.
authors.affiliation: Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, 30-688 Krakow, Poland; Jagiellonian Center for Experimental Therapeutics (JCET), Bobrzyńskiego 14, 30-348, Krakow, Poland.
authors.forename: Marek
authors.initials: M
authors.lastname: Grosicki
authors.affiliation: Jagiellonian Center for Experimental Therapeutics (JCET), Bobrzyńskiego 14, 30-348, Krakow, Poland.
authors.forename: Tomasz
authors.initials: T
authors.lastname: Wójcik
authors.affiliation: Jagiellonian Center for Experimental Therapeutics (JCET), Bobrzyńskiego 14, 30-348, Krakow, Poland; Department of Experimental Pharmacology, Chair of Pharmacology, Jagiellonian University Medical College, Grzegórzecka 16, 31-531, Krakow, Poland.
authors.forename: Stefan
authors.initials: S
authors.lastname: Chlopicki
authors.affiliation: Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, 30-688 Krakow, Poland. Electronic address: mfkonono@cyf-kr.edu.pl.
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Kieć-Kononowicz
mesh_terms: D002448:Cell Adhesion / Q000187:drug effects*; D002450:Cell Communication / Q000187:drug effects; D002460:Cell Line; D002469:Cell Separation; D002470:Cell Survival / Q000187:drug effects; D054314:Drug Inverse Agonism; D004727:Endothelium / Q000166:cytology* / Q000187:drug effects*; D004804:Eosinophils / Q000166:cytology* / Q000187:drug effects*; D006632:Histamine / Q000378:metabolism*; D017442:Histamine Agonists / Q000494:pharmacology; D006634:Histamine H1 Antagonists / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000494:pharmacology; D008024:Ligands; D008761:Methylhistamines / Q000494:pharmacology; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000494:pharmacology; D010879:Piperazines / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D011968:Receptors, Histamine / Q000378:metabolism*
chemical_list: D017442:Histamine Agonists; D006634:Histamine H1 Antagonists; D007211:Indoles; D008024:Ligands; D008761:Methylhistamines; D010879:Piperazines; D010880:Piperidines; D011968:Receptors, Histamine; C484309:1-((5-chloro-1H-indol-2-yl)carbonyl)-4-methylpiperazine; C025566:4-methylhistamine; D009240:N-Formylmethionine Leucyl-Phenylalanine; D006632:Histamine; C052075:thioperamide
keywords: 4-Methylhistamine dihydrochloride (PubChem CID: 215819); Adhesion; Diphenhydramine hydrochloride (PubChem CID: 8980); Endothelium; Eosinophils; Famotidine (PubChem CID: 3325); Histamine; Histamine dihydrochloride (PubChem CID: 5818); Histamine receptors; JNJ7777120 (PubChem CID: 4908365); N-formyl-Met-leu-Phe (fMLP) (PubChem CID: 443295); Pitolisant (PubChem CID: 9948102); Pyrilamine maleate (PubChem CID: 5284451); Ranitidine hydrochloride (PubChem CID: 3033332); Thioperamide maleate (PubChem CID: 11211984)