N-[3-[4'-(2",6"-Dimethylheptyl)phenyl]butanoyl]ethanolamine (E5050), a newly synthesized compound, was shown recently to induce uricosuria in humans via inhibition of the postsecretory reabsorption of urate. We examined the effects of this compound on urate excretion in rats loaded with oxonate and compared these effects with those of the uricosuric drugs trichlormethiazide and probenecid. When administered i.p., E5050 (0.3-15 mg/kg) increased the urinary excretion rate of urate and the ratio of urate clearance to inulin clearance in a dose-dependent manner, while the urine volume increased only slightly, and the glomerular filtration rate and plasma urate level were not changed. No paradoxical effect on urate excretion was observed. In contrast, trichlormethiazide and probenecid had a biphasic effect on urate excretion. In a pyrazinoic acid suppression test, the uricosuric effect of E5050 was completely inhibited by pretreatment with pyrazinoic acid. In a phenolsulfonphthalein (PSP) test, E5050 did not affect urinary PSP excretion, while probenecid strongly decreased such excretion. Thus, E5050 also appears to be uricosuric in rats.

01 Jan 1991·The Japanese Journal of Pharmacology

The Inhibitory Effect of a Novel Antiatheromatous Agent, E5050, on the Intimal Thickening of Aorta in Cholesterol-Fed Rabbit In Vivo.

Article

Author: Yasushi Saito ; Ryoichi Hashida ; Isao Yamatsu ; Hiroyuki Shiojiri ; Takao Saeki ; Nobuhiro Morisaki ; Issei Ohtsuka

The development of atheromatous lesions in the aortic arch of 0.5% cholesterol-fed rabbits was biochemically and morphologically examined. The animals were killed at week twelve (Cont-12W) or sixteen (Cont-16W). Both the micrographic and biochemical studies showed that the main atheromatous lesions in the Cont-12W group were fatty streaks, whereas those in the Cont-16W group were fibrous plaques. In these models, oral ingestion of 0.2% and 0.4% E5050, which has an antiproliferative effect on smooth muscle cells, had no effect on the surface involvement or the lipid content of the aortic arch at the sixteenth week, but reduced the degree of intimal thickening and the DNA content in the aortic arch in a dose-dependent manner. These results strongly suggest that E5050 suppresses the intimal thickening through its inhibitory effect on the proliferation of smooth muscle cells.

01 Jul 1990·European Journal of Pharmacology: Molecular PharmacologyQ3 · MEDICINE

Inhibitory effects of a novel antiatheromatous agent, E5050, an aortic smooth muscle cell proliferation, in vitro

Q3 · MEDICINE

Article

Author: Isao Yamatsu ; Nobuhiro Morisaki ; Takao Saeki ; Yasushi Saito ; Hiroyuki Shiojiri ; Hajime Tsunoda

The effect of a novel antiatheromatous agent, N-(3-[4'-(2'',6''-dimethylheptyl)phenyl]butanoyl)ethanolamin e (E5050), on the proliferation of porcine aortic smooth muscle cells was studied in vitro. E5050 dose-dependently inhibited DNA synthesis as well as proliferation of cells stimulated with 10% fetal calf serum with no cytotoxic effects. An inhibitory effect of E5050 on DNA synthesis was also confirmed in cells stimulated with human platelet extract and with a combination of platelet-derived growth factor and human plasma-derived serum. DNA synthesis in smooth muscle cells stimulated with other mitogens, such as fibroblast growth factor and insulin, was inhibited by E5050 and this inhibitory effect was positively correlated with the E5050 uptake into smooth muscle cells. These results indicate that E5050 inhibits smooth muscle cell proliferation stimulated by various mitogenic factors. It is suggested that E5050 prevents atherogenesis and inhibits the progression of fibromuscular lesions by interfering with the proliferation of arterial smooth muscle cells.

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Indication	Highest Phase	Country/Location	Organization	Date
Hypercholesterolemia	Phase 2	-	Eisai Co., Ltd.	-
Hyperlipidemias	Phase 2	JP	-	-

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