title: Suppressive effects of the endothelin receptor (ETA) antagonist BQ-123 on ET-1-induced reduction of lipoprotein lipase activity in 3T3-L1 adipocytes.
abstract: Endothelin (ET)-1 reduced heparin-releasable lipoprotein lipase (LPL) activity in 3T3-L1 adipocytes in a concentration-dependent manner. However, a selective ETB receptor agonist, [Ala1,3,11,15]ET-1, did not act like ET-1. The ET-1-induced decrease in LPL activity was suppressed by a selective ETA receptor antagonist, BQ-123: the concentration-response curve for the ET-1 reduction of LPL activity was shifted to the right in the presence of BQ-123 in a concentration-dependent manner. This antagonistic effect of BQ-123 clarifies that the ETA receptor is responsible for the ET-1-induced reduction of LPL activity in 3T3-L1 adipocytes, which suggests that there is therapeutic potential for ETA antagonists in LPL-related lipoprotein disorders.
authors.affiliation: Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Japan.
authors.forename: F
authors.initials: F
authors.lastname: Ishida
authors.forename: K
authors.initials: K
authors.lastname: Saeki
authors.forename: T
authors.initials: T
authors.lastname: Saeki
authors.forename: K
authors.initials: K
authors.lastname: Ishikawa
authors.forename: M
authors.initials: M
authors.lastname: Ihara
authors.forename: T
authors.initials: T
authors.lastname: Kamei
authors.forename: M
authors.initials: M
authors.lastname: Yano
mesh_terms: D016475:3T3 Cells / Q000187:drug effects / Q000378:metabolism; D000818:Animals; D004305:Dose-Response Relationship, Drug; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D004789:Enzyme Activation / Q000187:drug effects; D008052:Lipid Metabolism, Inborn Errors / Q000188:drug therapy; D008071:Lipoprotein Lipase / Q000378:metabolism*; D051379:Mice; D010456:Peptides, Cyclic / Q000494:pharmacology*; D017466:Receptors, Endothelin / Q000187:drug effects*
chemical_list: D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D010456:Peptides, Cyclic; D017466:Receptors, Endothelin; D008071:Lipoprotein Lipase; C072247:cyclo(Trp-Asp-Pro-Val-Leu)