Suppressive effects of the endothelin receptor (ETA) antagonist BQ-123 on ET-1-induced reduction of lipoprotein lipase activity in 3T3-L1 adipocytes.
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.
Ishida
F
F
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Japan.
Saeki
K
K
Saeki
T
T
Ishikawa
K
K
Ihara
M
M
Kamei
T
T
Yano
M
M
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*
D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D010456:Peptides, Cyclic; D017466:Receptors, Endothelin; D008071:Lipoprotein Lipase; C072247:cyclo(Trp-Asp-Pro-Val-Leu)