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The effect of moxisylyte hydrochloride on isolated human penile corpus cavernosum tissue was investigated and compared with other a-adrenergic antagonists. Moxisylyte produced a concentration-dependent relaxation of a norepinephrine-induced (1 x 10(-5) M) contraction of the corpus cavernosum tissue. Pretreatment with 1 x 10(-6) M doses of moxisylyte reduced competitively the norepinephrine-induced contraction. The competitive effect of prazosin was strongest among four tested agents, followed by phentolamine, moxisylyte, and then yohimbine. The activity ratio for each antagonist is 2.4 for moxisylyte, as compared with 28.2 for prazosin, 6.7 for phentolamine, and 1.6 for yohimbine respectively. Moxisylyte hydrochloride is an agent with potential clinical and research uses capable of producing erection when injected intra-cavernously. 相似文献
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Y Watanabe T Ito M Shiomi Y Tsujita M Kuroda M Arai M Fukami A Tamura 《Biochimica et biophysica acta》1988,960(3):294-302
In this paper, we examined whether the development of atherosclerosis in the Watanabe heritable hyperlipidemic (WHHL) rabbit, an animal model of familial hypercholesterolemia in man, could be prevented by the reduction of serum cholesterol levels. Pravastatin sodium (the generic name of CS-514), a potent inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, was used as a cholesterol-lowering drug. The drug was administered orally to 12 WHHL rabbits (2-3 months old) at a dose of 50 mg/kg per day for 24 weeks, and 13 animals were given water as control. In the treated group, serum cholesterol, phospholipid and triacylglycerol levels were significantly reduced by 28%, 32% and 16%, respectively, as compared with those of the control group. Although the prevention of development of the aortic atherosclerosis was not significant, the progression of coronary atherosclerosis was significantly prevented. The incidence of atherosclerosis in four main coronary arteries was reduced from 42% (control group) to 19% (treated group, P less than 0.01), and the development of lesion of coronary arteries evaluated by area of lesion was reduced from 19.7% (control group) to 9.1% (treated group, P less than 0.05). Histopathological findings supported the above observations. In addition, development of xanthoma in digital joints was also reduced from 90.4% (control group) to 58.3% (treated group, P less than 0.005). These results suggest that the development of coronary atherosclerosis and xanthoma in WHHL rabbit was reduced by continuous reduction of serum cholesterol levels treated with pravastatin sodium. 相似文献
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Inositol deficiency of Schizosaccharomyces pombe did not induce significant change of contents of various cellular components except for phospholipids and inositol. The most remarkable decrease in inositol content by the deficiency occurred in the mitochondrial fraction. Electronmicroscopic observation of the inositol-deficient cells of Sch. pombe showed no remarkable thickening of cell wall as occurred in the inositol-exacting mutant of Saccharomyces cerevisiae Strain A–21–20.Marked loss of fermentative activity under the aerobic condition was caused from inositol deficiency without significant change of activities of respiration and anaerobic fermentation. This seemed to indicate elevated regulatory control of the fermentative activity by oxygen in the inositol-deficient Sch. pombe.Phosphorylative activities of intact cells and the isolated mitochondria coupled with oxidation was also remarkably suppressed by inositol deficiency. 相似文献
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