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At least 163 records · Page 9Linked to original sources
PubMed1991

Influence of the trapidil derivative AR 12463 on serum and tissue lipids and development of aortic lesions during experimental atherosclerosis in rabbits.

Daily administration of the trapidil derivative AR 12463 (20 mg/kg body weight i.p.) to cholesterol-fed rabbits diminished statistically significantly the increase in serum total cholesterol. After 8 weeks of treatment all measured lipoprotein fractions were significantly lower in animals treated with AR 12463 (group 3) compared with the values of the untreated control (group 1) or vehicle-treated group (group 2). The reduction of serum levels was associated with statistically significantly reduced levels of cholesterol esters in kidney, liver and aorta. The levels of free cholesterol in the liver of group 3 animals were statistically significantly lower compared with the levels in the two other groups, whereas in kidney and aortas the levels of free cholesterol remained unchanged under the influence of AR 12463. The area of aorta covered with fatty streaks was significantly smaller in group 3 versus group 1. The results of this study indicate that treatment of rabbits with AR 12463 while feeding a cholesterol-rich diet prevents hypercholesterolemia as well as the cholesterol incorporation into tissues. The mode of action of AR 12463 on serum and tissue lipids as well as on the development of atherosclerosis is discussed.

Animals↗
PubMed1990

[Biotransformation of the trapidil (rocornal) derivative AR 12463 in the rat].

After p.o. administration of 5-piperidino-7-[N-pentyl-N-(beta- hydroxyethyl)]amino-s-triazolo[1,5-a]pyrimidine (1; AR 12463) more than 15 metabolites were isolated from urine and feces of male Wistar rats. Only small amounts of unchanged 1 were observed. The structure of 12 metabolites was elucidated or proposed on the basis of UV-, 13C NMR- and mass spectra. Main metabolites are 5-piperidin-4'-olyl-7-[N-pentyl-N-(beta- hydroxyethyl)]amino-s-triazolo[1,5-a]pyrimidine and 5-piperidin-4'-olyl-7-[N-pent-4-olyl-N-(beta-hydroxyet hyl)]amino-s- triazolo[1,5-a]pyrimidine. The other metabolites are mainly hydroxy- or ketopentyl derivatives and piperidinoles or piperidinones, respectively. Conjugates of most of the metabolites were identified, but the ratio phase-I/II metabolites was about 3:1. In contrast to trapidil, 5-methyl-7-diethylamino-s- triazolo[1,5-a]pyrimidine, no hydroxy derivatives of the bicyclic system were observed. The major part of unchanged 1 and metabolites is excreted via kidneys.

Adsorption↗
PubMed1987

[Effect of amrinone and trapidil on adherence, migration and phagocytic behavior of neutrophilic granulocytes of the human].

Amrinone and trapidile belong to a group of positive inotropic and simultaneously vasodilating substances, whose effects are based on an inhibition of phosphodiesterase (PDE), thus enriching intracellular c-AMP. In neutrophilic granulocytes these PDE-antogonists will produce an inhibition of adherence and phagocytosis, whereas the migration was not affected. The lower leukocyte effective concentration of 10 mmol/l can be achieved by a therapeutical application, so that a slight inhibition of the leukocyte function has to be accounted for as a side effect.

Amrinone↗
PubMed1988

Interaction of iloprost and indomethacin with the cardiac effects of isoprenaline, ouabain and trapidil.

Investigations in isolated heart preparations of guinea pigs showed, that iloprost enhanced the increase of cardiac performance by isoprenaline, but inhibit the positive inotropic effect of ouabain. On the other side pretreatment with indomethacin induced a significant rise of the cardiac effects of both isoprenaline and ouabain. The efficacy of trapidil and oxyfedrine remained uninfluenced. The results indicate, that prostanoids and cyclooxygenase inhibitors influence the effects of the investigated cardiac drugs. This is possibly be due to changes in the cellular membrane and the intracellular calcium content and should be considered in the therapeutic use of these substances.

Animals↗
PubMed1981

[HPLC of trapidil (Rocornal) and metabolites (author's transl)].

Trapidil (1; Rocornal) and 10 metabolites can be separated by a gradient technique on reversed phases (RP-8 instant columns) using the eluents methanol/water and acetonitrile/phosphate buffer (pH = 5.4); ultraviolet detection. Furthermore, HPLC techniques for purity testing and for determining 1 in serum are described.

Animals↗
PubMed1993

Effect of trapidil derivative AR 12456 on intracellular cholesterol homeostasis in human hepatoma cell line Hep G2.

The effect of trapidil derivative AR12456 on intracellular cholesterol metabolism was investigated in human hepatoma cell line HepG2. AR12456 enhanced the uptake and degradation of 125I-LDL in a dose-dependent manner. The drug inhibited cholesterol synthesis and esterification without affecting cellular cholesterol content and bile acid synthesis; cholesterol efflux was slightly increased. These results show that the inhibition of cholesterol synthesis together with the enhanced expression of LDL receptors may partially explain the hypocholesterolemic activity of compound AR12456.

Anticholesteremic Agents↗