• YAKHAK HOEJI
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• v.51 no.2
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• pp.83-87
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• 2007

The effects of ethaverine on serotonin biosynthesis in murine mastocytoma P815 cells were investigated. Ethaverine at 2.5${\sim}$10 ${\mu}$M decreased serotonin content in a concentration-dependent manner. The IC$_{50}$ value of ethaverine was 6.1 ${\mu}$M. Ethaverine at concentrations up to 20 ${\mu}$M was not cytotoxic towards P815 cells. Under these conditions, tryptophan hydroxylase (EC 1.14.16.4; TPH), a rate-limiting enzyme in serotonin biosynthesis, was inhibited by ethaverine in P815 cells (15.3% inhibition at 7.5 ${\mu}$M), however, aromatic L-amino acid decarboxylase (EC 4.1.1.28) was not. These results indicate that ethaverine leads to a decrease in serotonin content by reducing TPH activity in P815 cells.

• The Korean Journal of Pharmacology
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• v.11 no.1 s.17
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• pp.33-38
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• 1975

The clinical efficacy of Ethaverine, a peripheral vasodilator, was studied according to a double-blind, non-cross over method in 29 diabetic patients with peripheral arterial diseases. The clinical improvement was assessed from the history of patients including the incidence and frequency of intermitten claudication. Ethaverine, after 4 weeks of therapy, was not effective in improving clinical symptoms compared to placebo. Ethaverine, however, was an efective vasodilator than placebo. The quality of vasodilation induced by Ethaverine, was similar to that of alcohol. A new clinical method of studying peripheral vasodilator was presented. The clinical symptoms of peripheral vascular arterial disease in the lower extrimities include reduced intensity of palpable pulses, coldness, and discoloration of the skin. Intermittent claudication may be present. Pathologic changes in vessel architecture precede the symptoms, and recognition of impending vascular insufficiency is a determining factor in selecting vasodilating therapy or surgical management. Also, post-operative patients who have chronic peripheral vascular arterial disease may be candidates for subsequent vasodilating therapy. Peripheral vasodilators, according to the series of reports, may be indicated in vasospastic peripheral vascular condition rather than an occlusive vascular disease and the vessel responds best when a relatively large vascular beds are involved rather than a small, capillary beds. Recently, the clinical efficacy of peripheral vasodilators have been challanged by many clinical investigators and clinicians. In this study, we have re-evaluated the efficacy of Ethaverine HCl as peripheral vasodilator in patients with vasospastic peripheral arterial disease. Ethaverine is claimed to be two to four times as potent a spasmolytic agent as papaverine in a variety of laboratory and clinical work.