title: Effect of derivatives of trapidil on the expression of LDL receptors.
abstract: The influence of trapidil and some of its derivatives (AR 12456, AR 12463, AR 12465) on the LDL receptor mediated uptake and degradation of 125 I-LDL by human skin fibroblasts (HSF) and human hepatic cells (HEP G2) was investigated. AR 12456 enhanced the uptake and degradation of 125 I-LDL in HEP G2, but inhibited this pathway in HSF. When this drug was preincubated with HEP G2 cells, and then the incubation medium was transferred to HSF, a stimulation of specific LDL pathway occurred also in this cell line. Trapidil, AR 12463 and AR 12465 were inactive under the same experimental conditions. These findings suggest that a metabolite of AR 12456 might be responsible for the enhanced expression of LDL receptors in human cells.
authors.affiliation: Institut für Pharmakologie und Toxikologie, Martin-Luther-Universität Halle-Wittenberg, GDR.
authors.forename: J
authors.initials: J
authors.lastname: Beitz
authors.forename: A
authors.initials: A
authors.lastname: Corsini
authors.forename: A
authors.initials: A
authors.lastname: Granata
authors.forename: R
authors.initials: R
authors.lastname: Fumagalli
authors.forename: H J
authors.initials: HJ
authors.lastname: Mest
authors.forename: R
authors.initials: R
authors.lastname: Paoletti
mesh_terms: D000959:Antihypertensive Agents / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular; D002460:Cell Line; D002478:Cells, Cultured; D006801:Humans; D007700:Kinetics; D008077:Lipoproteins, LDL / Q000378:metabolism; D008113:Liver Neoplasms; D011743:Pyrimidines / Q000494:pharmacology*; D011973:Receptors, LDL / Q000187:drug effects / Q000378:metabolism*; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D014192:Trapidil / Q000031:analogs & derivatives / Q000494:pharmacology*
chemical_list: D000959:Antihypertensive Agents; D008077:Lipoproteins, LDL; D011743:Pyrimidines; D011973:Receptors, LDL; C046930:AR 12456; C059531:AR 12465; D014192:Trapidil; C053729:AR 12463