title: Differential uptake of grepafloxacin by human circulating blood neutrophils and those exudated into tissues.
abstract: The uptake of the antimicrobial quinolone agent, grepafloxacin, both by human circulating blood neutrophils and by those exudated into tissues, was evaluated in vitro by comparing the intracellular drug concentrations. In circulating blood neutrophils, the uptake of grepafloxacin was rapid and saturable at 37 degrees C. The uptake of grepafloxacin into circulating blood neutrophils was reduced by lowering the environmental temperature or by the presence of metabolic inhibitors, suggesting the involvement of an active transport mechanism. Furthermore, the uptake of grepafloxacin by tissue (salivary) neutrophils was also partially temperature-dependent and was significantly greater than that by circulating blood neutrophils, i.e. exudation of neutrophils into tissue results in a markedly enhanced transport mechanism for grepafloxacin. This phenomenon may be related to the higher defense activity against infection seen in exudated tissue neutrophils.
authors.affiliation: Department of Pharmacology, Gifu University School of Medicine, Gifu City, Japan. mniwa@cc.gifu-u.ac.jp
authors.forename: M
authors.initials: M
authors.lastname: Niwa
authors.forename: K
authors.initials: K
authors.lastname: Hotta
authors.forename: Y
authors.initials: Y
authors.lastname: Kanamori
authors.forename: H
authors.initials: H
authors.lastname: Matsuno
authors.forename: O
authors.initials: O
authors.lastname: Kozawa
authors.forename: M
authors.initials: M
authors.lastname: Hirota
authors.forename: T
authors.initials: T
authors.lastname: Uematsu
mesh_terms: D000890:Anti-Infective Agents / Q000097:blood*; D000963:Antimetabolites / Q000494:pharmacology; D002118:Calcium / Q000494:pharmacology; D005110:Extracellular Space / Q000187:drug effects / Q000378:metabolism; D024841:Fluoroquinolones; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism*; D010879:Piperazines / Q000097:blood*; D012463:Saliva / Q000166:cytology; D013696:Temperature
chemical_list: D000890:Anti-Infective Agents; D000963:Antimetabolites; D024841:Fluoroquinolones; D010879:Piperazines; C075375:grepafloxacin; D002118:Calcium