title: The novel compound NO-1886 activates lipoprotein lipase in primary cultured adipose and skeletal muscle cells.
abstract: As previously reported, we have discovered that a novel compound, NO-1886 (diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl] benzylphosphonate) has a powerful lipoprotein lipase (LPL) stimulating activity. Oral administration of NO-1886 increased LPL activity in postheparin plasma of experimental animals, resulting in the reduction of plasma triglyceride with concomitant elevation of high density lipoprotein cholesterol. However, the mechanism of NO-1886 on LPL activity is not clearly understood. To address this problem, we examined the effect of NO-1886 on LPL activity in primary rat cell culture isolated from adipose and skeletal muscle tissue. NO-1886 increased total LPL activity 18% and 23% in adipocytes at a dose of 3 and 10 micrograms/ml, respectively, and 43% at a dose of 10 micrograms/ml in skeletal muscle cells. These results indicate that NO-1886 may act directly on LPL-producing cells such as adipose and skeletal muscle.
authors.affiliation: Pharmacology Section, Otsuka Pharmaceutical Factory, Inc., Tokushima, Japan.
authors.forename: A
authors.initials: A
authors.lastname: Hagi
authors.forename: I
authors.initials: I
authors.lastname: Hirai
authors.forename: H
authors.initials: H
authors.lastname: Kohri
authors.forename: K
authors.initials: K
authors.lastname: Tsutsumi
mesh_terms: D000273:Adipose Tissue / Q000166:cytology / Q000187:drug effects* / Q000201:enzymology; D000818:Animals; D001549:Benzamides / Q000494:pharmacology*; D002478:Cells, Cultured; D004789:Enzyme Activation; D008071:Lipoprotein Lipase / Q000378:metabolism*; D008297:Male; D018482:Muscle, Skeletal / Q000166:cytology / Q000187:drug effects* / Q000201:enzymology; D009943:Organophosphorus Compounds / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D001549:Benzamides; D009943:Organophosphorus Compounds; C082137:4-diethoxyphosphorylmethyl-N-(4-bromo-2-cyanophenyl)benzamide; D008071:Lipoprotein Lipase