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At least 703 records · Page 39Linked to original sources
PubMed1984

Effect of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) on gastric ulcers and gastric secretion in experimental animals.

The effect of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) on various experimental gastric ulcers and gastric secretion in experimental animals was compared with that of cimetidine and cetraxate. MN-1695 significantly inhibited the formation of Shay, stress-induced, indomethacin-induced, and histamine-induced ulcers and significantly accelerated the healing of acetic acid-induced gastric ulcers. MN-1695 was much more effective in suppressing stress- and acetic acid-induced ulcers than indomethacin-induced, histamine-induced or Shay ulcers. Cimetidine was effective in preventing stress- and acetic acid-induced ulcers but had no significant effect on Shay, indomethacin-induced and histamine-induced ulcers. Cetraxate was effective in preventing only stress-induced ulcers and had almost no effect on other experimental ulcers. MN-1695 inhibited secretion of gastric juice, acid and pepsin in Shay rats, but had no influence on basal and secretagogue-stimulated acid secretion in the perfused stomach of urethanized rats. These findings suggest that MN-1695 is a new type of anti-ulcer agent.

Acetates↗
PubMed1984

Effect of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) on gastric mucosal blood flow in dogs.

The effect of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) on gastric mucosal blood flow ( GMBF ) and on the changes of GMBF induced by catecholamines, tetragastrin, histamine and indomethacin were investigated in anesthetized dogs. MN-1695 at doses up to 1 mumol/kg i.v. showed only a slight but prolonged increase of GMBF . MN-1695 tended to inhibit the decreases of GMBF induced by norepinephrine and the increase of GMBF induced by tetragastrin. The later phase of decreased GMBF induced by histamine was suppressed by MN-1695. However, MN-1695 had almost no effect on the increase of GMBF induced by epinephrine. MN-1695 produced a marked increase of antral mucosal blood flow which was reduced by pretreatment with indomethacin. Systemic blood pressure, respiration and the pressor responses induced by catecholamines and gastric secretagogues were not affected by MN-1695. These results suggest that MN-1695 may possess selective effects on the gastric mucosal microcirculation and that suppressive effects of MN-1695 on the GMBF decrease induced by ulcerogenic stimuli may be responsible for its anti-ulcer activities in various types of experimental gastric ulcers.

Animals↗
PubMed1984

Phase I study of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695), a new anti-ulcer agent.

A phase I study of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine (MN-1695), which is expected to have an anti-ulcer effect, was performed in 14 healthy male subjects. The safety and pharmacokinetics were examined in single-dose oral administration of 1, 2, 4, 8 and 16 mg/body and multiple-dose administration of 2 mg/body/day, once daily, for 28 consecutive days. As for the subjective symptoms, only light headache, general malaise and heart burn were observed in two out of 4 subjects in the 16-mg group. No abnormalities were found in blood pressure, pulse rate, respiratory rate, body temperature, body weight and ECG both in single- and multiple-dose studies. No abnormal changes attributed to this drug appeared in hematological and biochemical examinations and urinalysis. Times for reaching the maximum plasma concentration in the single-dose study were 3.5, 8 and 3.3 h in 4-, 8- and 16-mg groups, respectively. The elimination half-lives from the plasma were 152, 145 and 148 h for the 3 groups, respectively. The plasma concentration curves in the multiple-dose study were similar to those simulated with the pharmacokinetic parameters obtained in the single-dose study. The plasma concentration increased until the 14th day, as the administration continued, and reached steady state thereafter; there seemed to be no abnormal cumulation. The elimination patterns after multiple-dose administration were almost the same as those in the single-dose study; the half-life was about 170 h.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1978

Phase II study of triazinate and pyrazofurin in patients with advanced breast cancer previously exposed to cytotoxic chemotherapy.

The purpose of this phase II clinical trial was to evaluate the effectiveness of triazinate and pyrazofurin in the treatment of advanced breast cancer. Although an occasional patient experienced stability of disease, neither agent, as employed in this study, was able to produce an objective antitumor effect in this group of patients with previous chemotherapeutic exposure. At the dosages used in this study, neither agent can be recommended for further treatment of advanced breast cancer.

Adult↗
PubMed1984

Effect of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) on gastric mucosal damage induced by various necrotizing agents in rats.

The effect of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695) on the gastric mucosal damage induced in rats by various necrotizing agents was compared with those of cimetidine, cetraxate and prostaglandin (PG) E2. MN-1695 at doses of 0.37 mg (1 mumol) to 3.72 mg (10 mumol)/kg, significantly decreased in a dose-dependent manner the damage indices after the application of ethanol, HCl, NaOH, 25% NaCl or boiling water. Cimetidine in doses of 12.6 mg (50 mumol) to 126 mg (500 mumol)/kg was effective only against HCl-induced damage. Cetraxate in doses of 34.2 mg (100 mumol) to 342 mg (1 mmol)/kg was effective against damage due to ethanol, HCl, 25% NaCl or boiling water. However, cetraxate increased the damage index of NaOH-induced injury. PGE2 in a dose of 25 micrograms (70 nmol)/kg was effective against ethanol and 25% NaCl. The histological changes of gastric mucosal cells produced by ethanol were significantly decreased by MN-1695 and PGE2. These results suggest that MN-1695 has a cytoprotective action like that of PGE2 and that this cytoprotection inhibits the development of various kinds of experimental gastric ulcers.

Animals↗
PubMedDate not supplied

Phase II study of vinblastine-CCNU, triazinate, and dactinomycin in advanced renal cell cancer.

A total of 133 patients with advanced or metastatic adenocarcinoma of the kidney were stratified according to performance status and time from initial diagnosis to recurrence and were then randomized to one of three different drug treatment arms or the crossover secondary treatment. The study drugs (combination vinblastine-CCNU and single-agent triazinate or dactinomycin) failed to provide any meaningful antitumor activity for these patients with advanced renal cell cancer.

Adenocarcinoma↗
PubMed1982

[Gas chromatographic determination of sym-triazine herbicides in drugs from vegetable sources (author's transl)].

Several separation phases were tested for effectiveness in the gas chromatographic determination of residues of sym-triazine herbicides in officinal drugs. Carbowax 20 M, OV 225 and OV 330 are well suited for separating this group of active agents. A NP-FID was used as a gas chromatographic detector. Sample preparation was optimized. Chloroform (as an extracting agent) and the shaking method were best suited for extracting. The samples were purified by column chromatography, DMSO/petroleum ether partition and purification by extraction from a hydrochloric solution being performed subsequently if necessary. The recovery rates and the reproducibility observed for various drugs and different extraction methods were compared. The limit of detection of the method laid at 0.02 mg/kg.

Chromatography, Gas↗
PubMed1980

Antifungal properties of a novel 1,2,4-triazine derivative I 319.

The antifungal activity of the sodium salts, of 3-thiolo-5-phenyl-1,2,4-triazine (I 319) was determined in vitro and in vivo. The minimal inhibitory concentration (MIC) of I 319 for 33 pathogenic and saprophytic fungal strains ranged from 3.1 to 25 microgram/ml. In vivo, experiments were performed on a model of subacute candidiasis in Balb/c mice infected intraperitoneally with Candida albicans. The antifungal activity was estimated on the basis of the extension of the mice life span and on the number of living yeast cells present in the kidneys, liver and spleen of treated and control mice. A single i.p. dose of I 319 (25 mg/kg) prolonged the survival time of treated animals up to 200%. Five subsequent doses of the compound diminished the number of C. albicans cells in the tissues of these mice. The DL50 of I 319 for mice (i.p.) was about 250 mg/kg.

Animals↗
PubMed1981

Bronchodilator and antiallergic properties of LA 2851 (2-4-diamino-7-methyl-pyrazolo (1,5-a) 1,3,5-triazine).

LA 2851, 2-4-diamino-7-methyl-pyrazolo (1,5a) 1, 3, 5 triazine has been found to possess potent bronchodilator and inhibitor properties on experimental active and passive anaphylaxis. In vitro evaluation on guinea-pig trachea indicated that LA 2851 had relaxant properties on unstimulated and stimulated (histamine or pilocarpine) strips. Resistance and compliance measurement in anaesthetized dogs and guinea-pigs showed that the drug reversed or prevented in vivo bronchoconstriction due to histamine. The relaxant effect was not linked to beta stimulating property. LA 2851 was as active as theophylline in all tests used. LA 2851 and theophylline prevented anaphylactic shock in mice. DSCG was poorly active. IgE mediated passive cutaneous anaphylaxis in rat was dose-dependently inhibited by LA 2851 (DSCG greater than LA 2851 greater than theophylline). According to these results the compound decreased histamine release from rat mast cells induced by different secretagogues (LA 2851 greater than DSCG greater than theophylline). No tachyphylaxis (PCA) nor time preincubation dependency (mast cells) was found with LA 2851 as it has been reported for DSCG. LA 2851 by its pharmacological properties associated with a very low toxicity (2.5 to 5 times less than theophylline) provides a new potential agent for respiratory diseases.

Anaphylaxis↗
PubMed1995

Synthesis and pharmacological evaluation of 1,2,4-triazine and its congeners.

3-[Mercapto]-n-propanoxy/methyl-ethanoxy branched chain in 5,6-Diphenyl- 1,2,4-triazine were condensed with O-phenylene diamine or O- aminophenol or o-aminothiophenol. The carboxylic groups of the synthesized compounds were cyclised to yield imidazoles, oxazoles and thiazoles. They were screened for their anti-inflammatory response in albino rats against carrageenin induced paw oedema. The active compounds were also evaluated for their ED50 value in albino rats and analgesic activity in albino mice. The compounds exhibited significant anti-inflammatory activity also showed marked protection against aconitine induced writhing response. The potent compounds showed high LD50 values.

Animals↗
PubMed1995

[Iminodimethylation, a method for pharmacomodulation in pyrimido-[3,4-a]-s-triazine series].

Primary amines react with two formaldehydes and compounds presenting two mobile hydrogen atoms, this reaction can be called iminodimethylation. This reaction can be used in order to perform a pharmacomodulation in the pyrimido [3,4-a]-s-triazine series. Against Epidermophyton floccosum, the activity is better when nitrogen 7 is not substituted, when the heroatom in position 2 is 0 instead of S and when an aromatic nucleus is directly linked to the nitrogen atom in position 3.

Antifungal Agents↗
PubMedDate not supplied

Multiresidue method for the chromatographic determination of triazine herbicides and their metabolites in raw agricultural products.

A method is described for the determination of 19 triazine herbicides and 4 metabolites in 6 agricultural products that represent diverse matrixes. In addition, a modification of this method to determine the more water-soluble metabolite, desethyldesisopropylatrazine, is described. In both these procedures, residues are extracted with methanol, and the product coextractives are removed using solvent partition and cation-exchange solid-phase extraction chromatography. A nitrogen phosphorus detector and DB-17 megabore column are used for the temperature-programmed chromatographic determination of samples fortified at 0.02-1.0 ppm levels. Average recoveries ranged from 81.1 to 106.2% for the parent herbicides and from 59.6 to 87.5% for the metabolites on all crops. An average recovery of 101.1% was obtained for desethyldesisopropylatrazine.

Animals↗
PubMed1994

Synthesis of some new heterobicyclic compounds containing spiro-1,2,4-triazine moiety as potential anti-HIV and anticancer agents.

A number of heterobicyclic compounds such as 1,3,5-thiazine, thiazolidinone, pyrimidine, pyrimidinedione, imidazole, quinazolinone and 1,2,4-triazinone derivatives have been sythesized by reaction of 1,6-dihydro-3(2H)-thioxo-6-spiro-(9'- fluorene)-1,2,4-triazin-5(4H)-one (1) with sulphur/nitrogen compounds in neutral or alkaline media. Structure elucidation of the new compounds have been carried out with the help of elemental analysis and spectral data. Some of these compounds were tested for in vitro anti HIV and anticancer activities.

Antineoplastic Agents↗
PubMed1994

Synthesis of some new heterobicyclic compounds containing spiro-1,2,4-triazine moiety as potential anti HIV and anticancer agents.

A number of heterobicyclic compounds such as 1,3,5-thiazine, thiazolidinone, pyrimidine, pyrimidinedione, imidazole, quinazolinone and 1,2,4-triazinone derivatives have been synthesized by interaction of 1,6-dihydro-3 (2H)-thioxo-6-spiro-(9'-fluorene)-1,2,4-triazin-5(4H)-one (1) with sulphur/nitrogen compounds in neutral or alkaline medium. Structure elucidation of the new compounds has been carried out with the help of elemental analysis and spectral data. Some of these compounds were tested for in vitro anti HIV and anticancer activities.

Antineoplastic Agents↗
PubMedDate not supplied

[The stacking interaction of antibiotics of the pyrimido[5,4-e]-1,2,4-triazine series with purines].

The changes in the PMR spectra of purine bases added to aqueous solutions (D2O) of antibiotics of the pyrimido[5,4-e]-1,2,4-triazine type, reumycin and xanthotricin as well as the changes in the PMR indicate formation of heteroassociates with batch structure as a result of stacking interaction. Chemotherapeutic effect of the antibiotics is explained by their intercalation into the batches of the nucleic acids bases, which violates their functioning.

Antibiotics, Antineoplastic↗