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Results for “Azulenes”

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At least 415 records · Page 23Linked to original sources
PubMed1989

Thromboxane A2 antagonistic action of a new anti-ulcer agent, azuletil sodium (KT1-32).

The TXA2/PGH2 receptor antagonistic activity of azuletil sodium (KT1-32), a new anti-ulcer agent, was examined. KT1-32 competitively antagonized the contraction of canine gastric arteries induced by U-46619, PGF2 alpha, and PGE2, whereas it had no effect on the PGF2 alpha-, PGE2- and LTD4-induced contraction of guinea-pig ileum, which was not affected by U-46619. In anesthetized dogs, KT1-32 significantly reduced the U-46619-induced decrease in gastric arterial blood flow. Gastric contraction induced by U-46619 in anesthetized rats was markedly inhibited by KT1-32. KT1-32 showed no influence on TXA2 synthetase and cyclooxygenase activities. These results indicate that KT1-32 is a competitive TXA2/PGH2 receptor antagonist, which may be important as to the effectiveness of KT1-32 against gastric ulcer.

15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5↗
PubMed2002

Stilbazulenyl nitrone, a novel azulenyl nitrone antioxidant: improved neurological deficit and reduced contusion size after traumatic brain injury in rats.

OBJECT: Stilbazulenyl nitrone (STAZN) is a second-generation azulenyl nitrone that has markedly enhanced antioxidant properties compared with those of conventional alpha-phenyl nitrones. In this study, the authors assessed the potential efficacy of STAZN in a rodent model of fluid-percussion brain injury, which results in a consistent cortical contusion. METHODS: After anesthesia had been induced in normothermic Sprague-Dawley rats (brain temperature 36-36.5 degrees C) by halothane-nitrous oxide, the animals were subjected to a right parietooccipital parasagittal fluid-percussion injury (1.5-2 atm). The agent (STAZN, 30 mg/kg: eight animals) or vehicle (dimethyl sulfoxide; eight animals) was administered intraperitoneally at 5 minutes and 4 hours after trauma. The neurological status of each rat was evaluated on Days 1, 2, and 7 postinjury (normal score 0, maximum injury 12). Seven days after trauma, the rat brains were perfusion fixed, coronal sections at various levels were digitized, and areas of contusion were measured. Treatment with STAZN significantly improved neurological scores on Days 2 and 7 postinjury compared with vehicle-treated rats. Administration of STAZN also significantly reduced the total contusion area by 63% (1.8 +/- 0.5 mm2 in STAZN-treated animals compared with 4.8 +/- 2.1 mm2 in vehicle-treated animals; p = 0.04) and the deep cortical contusion area by 60% (1.2 +/- 0.2 mm2 in STAZN-treated animals compared with 2.9 +/- 1.2 mm2 in vehicle-treated animals; p = 0.03). By contrast, hippocampal cell loss in the CA3 sector was unaffected by STAZN treatment. CONCLUSIONS: Therapy with STAZN, a novel potent antioxidant, administered following traumatic brain injury, markedly improves neurological and histological outcomes. Azulenyl nitrones appear to represent a promising class of neuroprotective agents for combating this devastating condition.

Animals↗
PubMed2000

Sex-related differences in urinary excretion of egualen sodium in rats.

Egualen sodium (sodium 3-ethyl-7-isopropyl-1-azulenesulfonate 1/3 hydrate) is a new antiulcer drug. There has been no difference observed in absorption between male and female rats, the relative amount of metabolites in male plasma has been higher than that in females, and the excretion ratios of metabolites in males have been significantly higher than those in females. However, the plasma concentration profile of total radioactivity in males has been higher than that in females. To clarify this discrepancy, the renal clearances and plasma concentrations of the unchanged drug and its metabolites were determined. The renal clearance of the unchanged drug in males was 21 times lower than that in females, and the urinary excretions in males and females were 2.1 and 39.5% of dose, respectively. This indicates that the major factor in the sex-related difference observed in the plasma concentration of total radioactivity is due to the difference in the renal clearance of the unchanged drug between the sexes. The results of treatments with probenecid in normal and gonadectomized rats revealed that egualen sodium was mainly excreted into urine by secretion through the renal tubule. Furthermore, the results of treatments with testosterone in rats revealed that the excretion of egualen sodium was highly affected by androgens. These facts indicated that the sex-related difference observed in the plasma concentration of total radioactivity can be attributed to the inhibition of renal tubular secretion of the unchanged drug by androgens. This is the first example of sex-related differences in both metabolism and excretion.

Administration, Oral↗
PubMed2002

[Constituents analysis on volatile oil of Pogostemon cablin from different collection time cultivated in Hainan].

The constituents of the volatile oil of Pogostemon cablin collected from Wanning city, Hainan province and the influence owing to different collection time were undertaken by GC/MS combination technology. The results showed that main compounds was patchouli alcohol in stem oil and leaf oil, its contents were respectively 36.06% and 37.74%; pogostone was poor, its contents in stem oil and leaf oil were respectively 17.08% and 0.85%; the contents of ten compounds were over 1%, which was respectively beta-patchoulene, beta-elemene, transcaryophyllene, delta-guaiene, seychellene, alpha-patchoulene, aciphyllene, alpha-guaiene, patchouli alcohol and pogostone; the contents of volatile oil from June to August were respectively 0.8%, 0.7% and 0.6%; patchouli alcohol, higher in July and June(42.62% and 40.84%), lower in August(31.40%).

Azulenes↗
PubMed2001

[Study of chemical constituents of essential oil from flowers of Mikania micrantha H.B.K].

The essential oil from flowers of Mikania micrantha H.B.K were extracted and its chemical constituents were analyzed by GC/MS. Forty-two compounds were identified and the main compounds with high contents were beta-cubebene (12.95%), allo-aromadendrene (11.67%), beta-caryophyllene (9.17%), 1H-inden-1-one, 5-(1, 1-dimethylethyl)-2, 3-(6.23%), beta-himaohalene (4.56%), trans-alpha-bergamotene (4.09%), limonene (3.68%), beta-ocimene (2.53%).

Azulenes↗