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At least 649 records · Page 36Linked to original sources
PubMed1984

Effects of trimebutine maleate (TM-906) on the smooth muscles of isolated guinea pig gallbladder.

Effects of trimebutine maleate (TM-906) on the smooth muscles of isolated guinea pig gallbladder were investigated. TM-906 inhibited the contractile responses to cholinergic nerve stimulation (5 Hz) and to acetylcholine (3 X 10(-8) g/ml) to the same extent, both of which produced much the same amplitude of contraction. TM-906 noncompetitively antagonized the contractile response to methacholine, and it caused a parallel shift of dose-response curves for the contractile response to CaCl2 to higher concentrations. Moreover, TM-906 inhibited the contractile response to 50 mM KCl in a dose-dependent manner. On the other hand, TM-906 itself evoked a slight contractile response in a dose-dependent manner. The contractile response induced by TM-906 was prevented by exposure to Ca++-free solution, but not by tetrodotoxin or atropine. From these results, it was suggested that TM-906 inhibited the contractile responses to cholinergic nerve stimulation, acetylcholine, methacholine and 50 mM KCl by reducing the influx of calcium ion across the cell membrane, while it was assumed that TM-906 itself evoked a slight contractile response by increasing in some way the concentration of the intracellular free calcium ion available for the contractile systems.

Acetylcholine↗
PubMed1986

Effects of trimebutine maleate (TM-906) on the spontaneous contraction of isolated duodenum and ileum in both guinea pigs and rabbits.

Effects of trimebutine maleate (TM-906) on the spontaneous contraction of isolated duodenum and ileum were studied in both guinea pigs and rabbits. In the duodenum and ileum of both guinea pigs and rabbits, TM-906 (10(-6) g/ml, 10(-5) g/ml) produced a potentiation of the spontaneous contraction in preparations with low contractile activity (low tone or small contraction), while it caused an inhibition of the spontaneous contraction in preparations with high contractile activity (high tone or large contraction). The potentiation of spontaneous contraction by TM-906 was more pronounced in the ileum than in the duodenum of both guinea pigs and rabbits. When the spontaneous contraction of duodenum and ileum was decreased by atropine, the potentiation of spontaneous contraction by TM-906 was further augmented and was more pronounced in the ileum than in the duodenum. When the spontaneous contraction was remarkably potentiated by physostigmine or acetylcholine, TM-906 markedly inhibited the potentiated spontaneous contraction, and the potentiation by TM-906 seen in preparations with low contractile activity disappeared. From these results, it is concluded that TM-906 produces, depending on the contractile activity of the preparations, a potentiation or an inhibition of the spontaneous contraction of duodenum and ileum in both guinea pigs and rabbits and that the potentiation by TM-906 is more pronounced in the ileum than in the duodenum. It is suggested that the endogenous acetylcholine partly modifies the effects of TM-906, but that it does not relate to the more pronounced potentiation by TM-906 in the ileum than in the duodenum.

Acetylcholine↗
PubMed1991

Changes in cyclic AMP content of rat gastric mucosa induced by ulcerogenic stimuli--in relation to the antiulcer activity of irsogladine maleate.

Changes in the cyclic AMP (cAMP) content of the gastric mucosa induced by ulcerogenic stimuli were investigated in rats. Ligation of the pylorus for 5 hr produced no glandular mucosal lesion, but increased the cAMP content in the fundus and antrum. Aspirin produced glandular mucosal lesions in the pylorus-ligated rats and caused an increase of the cAMP content in the fundus and a decrease in the antrum. Irsogladine maleate (IM), an antiulcer agent, inhibited both the changes in the cAMP content and the mucosal damage induced by aspirin. IM increased the cAMP content in both regions, especially the antrum, in normal rats. Dibutyryl cAMP (dbcAMP) given orally prevented the gastric mucosal lesions induced by aspirin without affecting gastric secretion. These results suggest that 1) the changes in the cAMP content of the fundus and antrum induced by aspirin may be associated with the formation of glandular mucosal damage, 2) the antiulcer activity of IM may be related to an increase of the cAMP content in mucous cells, and 3) dbcAMP given orally may penetrate into the surface mucous cells and activate defensive functions. Thus, cAMP in the mucous cells may protect the gastric mucosa.

Animals↗
PubMed1998

Irsogladine maleate may preserve gastric mucosal hydrophobicity against ethanol in phospholipids independent way in rats.

Irsogladine maleate (IM) has been used as a mucosal protective agent, whose action is partially explained as enhancement of mucosal blood flow, increase of cellular cyclic AMP and facilitation of gap-junctional intercellular communication. Effect of IM on rat gastric mucosal hydrophobicity, one of the mucosal barrier properties, was investigated, in comparison with that of 16,16-dimethyl prostaglandin E2 (dmPGE2). IM alone had no effect on mucosal hydrophobicity and mucosal phospholipids content. dmPGE2 alone did not change mucosal hydrophobicity significantly, but remarkably increased mucosal surface-active phospholipids. Intragastric administration of absolute ethanol significantly decreased gastric mucosal hydrophobicity and mucosal phospholipids content. IM could prevent the decrease in mucosal hydrophobicity by ethanol, maintaining the surface mucus gel layer and mucosal surface phospholipids almost as non-damaged control levels, whereas dmPGE2 also prevented the decrease in mucosal hydrophobicity by ethanol, with the surface epithelium being partially exfoliated and mucosal surface-active phospholipids showing remarkable enhancement. These results suggest that IM may preserve gastric mucosal hydrophobicity against ethanol, not through enhancement of mucosal phospholipids content like prostaglandin, but possibly through its reported stabilization action to the epithelial cell lining, which may preserve the surface epithelium with the mucous gel layer containing surface-active phospholipids, a possible origin of mucosal hydrophobicity.

Animals↗
PubMed1999

Effect of zaldaride maleate, an antidiarrheal compound, on visceral pain reflex induced by small intestinal distention in anesthetized rats.

Using distention of the small intestine as a visceral pain model, we investigated the effect of zaldaride maleate (ZAL), a selective inhibitor of calmodulin, on the depressor response. In pentobarbital-anesthetized rats, small intestine distention was induced by rapid application of intraluminal pressures of 40 cmH2O causing a reflex fall in arterial blood pressure. The depressor response to intestinal distention was abolished by intraperitoneal administration of capsaicin (5 mg/rat), which depletes neuropeptides such as substance P from the sensory neurons, on the mesenteric stalk and by neonatal pretreatment with capsaicin (50 mg/kg, s.c.). Morphine (20 mg/kg, s.c.) reduced the depressor response following intestinal distention. At doses of 3 mg/kg (i.v.) and higher, ZAL significantly reduced depressor response. The effect of morphine was reversed by naloxone (5 mg/kg, i.v.); the effect of ZAL was not affected. These results suggest that ZAL helps reduce the visceral pain induced by noxious stimulus and that the antinociceptive effect of ZAL is not mediated by opioid receptors.

Adrenergic alpha-Antagonists↗
PubMed1999

Antidiarrheal effects of zaldaride maleate after oral, intravenous and subcutaneous administration to rats.

The antidiarrheal action of zaldaride maleate (ZAL) after oral, intravenous and subcutaneous administration was examined to determine whether ZAL acts systemically or locally in the intestine of rats. Oral administration of ZAL inhibited castor oil- and 16,16-dimethyl prostaglandin E2-induced diarrhea; however, intravenous or subcutaneous administration of ZAL was ineffective. When ZAL was orally administered, the area under the plasma concentration time curve of the compound was lower than that of ZAL following intravenous or subcutaneous administration at the maximum doses studied. The antidiarrheal effect of ZAL was not dependent on its plasma concentration level. These results suggest that ZAL acts locally in the intestinal tract in rats.

16,16-Dimethylprostaglandin E2↗
PubMed2000

Effects of zaldaride maleate, an antidiarrheal compound, on intracellular Ca2+-mediated short-circuit current response in the rat colonic mucosa.

The effect of zaldaride maleate (ZAL) on intracellular Ca2+-mediated short-circuit current (Isc) response in rat colonic mucosa was investigated. The Isc response to acetylcholine was partially reduced by the neuronal blocker tetrodotoxin. The tetrodotoxin-sensitive Isc response to acetylcholine was inhibited by ZAL. The tetrodotoxin-insensitive effect, which indicates direct stimulation of acetylcholine in colonic mucosa, was not affected by ZAL. The Isc response to the Ca2+ ionophore A23187 was reduced by ZAL in the presence of tetrodotoxin. These results suggest that ZAL reduces colonic ion secretion by inhibiting a tetrodotoxin-sensitive neuronal pathway and an intracellular Ca2+ pathway in epithelium.

Acetylcholine↗
PubMed2000

Analysis of oxidation sensitivity of maleate cis-trans isomerase from Serratia marcescens.

The maleate cis-trans isomerase gene (maiA) from Serratia marcescens IFO3736 was cloned and sequenced. Serratia MaiA has 62.4% amino acid identity with Alcaligenes faecalis IFO13111 MaiA and 64.9% with Bacillus stearothermophilus MI-102 MaiA. All known ten amino acid sequences of MaiA had significant conserved regions containing cysteine residues, which were previously suggested to be involved in an active site of the enzyme. The maiA gene was expressed in Escherichia coli, and expressed products MaiA was purified and characterized. The purified enzyme of strain IFO3736 showed high activity at room temperature and high heat stability. It also showed higher activity in the presence of high concentration of aspartic acid than the enzyme of A. faecalis IFO13111, but it was also sensitive to chemical oxidation. By amino acid composition analysis, cysteine, methionine, and tyrosine residues were suggested to be oxidized to inactivate the enzyme by chemical oxidation. To investigate the mechanism of chemical oxidation of the enzyme, six methionine residues in the conserved regions of S. marcescens MaiA were replaced with cysteine residues by site-directed mutagenesis. The analysis of the constructed mutants suggested that the Met201 residue near the Cys198 residue is involved in the sensitivity of the enzyme to chemical oxidation.

Amino Acid Sequence↗
PubMed2006

The effects of a timolol maleate gel-forming solution on normotensive beagle dogs.

The effects of a timolol maleate gel-forming solution (TMGS) on intraocular pressure (IOP), blood pressure (BP), and pupil size (PS) were evaluated in normotensive dogs. TMGS was administered once daily to six normotensive beagle dogs. TMGS administration reduced IOP and PS. The hypotensive effect persisted for 24 hr after the administration. The mean reduction in IOP was 5.3 mm Hg (P<0.01). The changes in BP and PS were not significant. These results suggest that TMGS can potentially be used in the treatments of glaucoma and ocular hypertension in dogs.

Animals↗
PubMed1983

Update: midazolam maleate, a new water-soluble benzodiazepine.

It appears that midazolam maleate with its short half-life, water solubility, lack of venous irritation, lack of serious side effects, and benign cardiovascular, respiratory, and CNS effects, may become a useful drug in the dental profession, especially in the field of oral and maxillofacial surgery.

Anesthesia, Dental↗
PubMed1975

Effect of methylergobasine maleate on serum gonadotrophin and prolactin in humans.

Intramuscular injection of 0.2 mg methylergobasine maleate3) (Methergin, Sandoz) in women on day 3 post-partum, in regularly menstruating women and in adult men, is followed within 30 to 75 min by a 50% decrease in serum prolactin concentration: the levels remain low until 180 min and increase between 180 and 240 min. The amplitude of the decrease is the same when prolactin is measured in terms of the same serum prolactin standard by a homologous ovine assay and by a homologous human assay. However, in the case of regularly menstruating women and of men serum prolactin concentration is some three times higher when estimated by the ovine assay than when estimated by the human assay. This difference between assay results obtained by the two radioimmunoassay methods could be due to heterogeneity of serum prolactin. However, non-specific effects of serum are not excluded. In regularly menstruating women and in men, intramuscular injection of 0.2 mg methylergobasine maleate is followed within 45 to 75 min by a 50% decrease in immunoreactive serum LH concentration without concomtant change in immunoreactive FSH. The depression of LH secretion lasts for 1 to 2 h. The circulating levels of HCG in post-partum women are not modified after intramuscular injection of Methergin. In humans as in animals and in in vitro studies, inhibition of prolactin and LH release induced by ergot drugs are likely due to both an indirect effect via the hypothalamus and to a direct effect on the pituitary cells.

Adult↗
PubMed1984

[Effects of trimebutine maleate (TM-906) on the gastrointestinal motility in anesthetized dogs].

Effects of trimebutine maleate (TM-906) on the spontaneous motility of the gastrointestinal tracts were investigated in anesthetized dogs by means of force transducers. TM-906, administrated intravenously or intraduodenally, produced an inhibition followed by a potentiation of the spontaneous motility in the stomach, and caused a potentiation of the spontaneous motility in the duodenum, jejunum, ileum and colon. These effects of TM-906 were observed also in the vagotomized dogs as in the intact dogs. From these results, it is suggested that TM-906 modulates the spontaneous motility of the gastrointestinal tracts primarily through the peripheral mechanism.

Anesthesia↗
PubMed2006

Effectiveness of house dust mite acaricide tri-n-butyl tin maleate on carpets, fabrics and mattress foam: a standardization of methodology.

The aim of this study was to determine the effectiveness of the acaricide tri-n-butyl tin maleate, industrially applied to samples of carpets, mattress foam, and fabrics used for furniture upholstery, soft toys and shoe uppers. Approximately 100 adult house dust mites of the species Dermatophagoides pteronyssinus were inoculated into a Petri dish containing the sample (a piece of carpet, mattress foam, or fabric), treated with the acaricide, randomly collected. Mite-maintenance culture medium was added on top of each sample. After one, two, three, seven and 30 days of incubation at 25 degrees C and 75% relative humidity, each dish was examined using a 40X stereoscopic microscope (40X). One hundred percent acaricide effectiveness was obtained in treated materials by the end of the 30th-day postinoculation period, under optimal conditions for mite maintenance.

Animals↗
PubMed1984

Successful treatment of the crisis of scleroderma with enalapril maleate (MK-421).

A 74-year-old man has been known to have scleroderma for 5 years. Two months before the hospitalization, his blood pressure was rapidly elevated, and progressive renal impairment and ulcerations of the fingers manifested. Then he was diagnosed to have a crisis of scleroderma. The treatment with a new long-acting angiotensin I converting enzyme inhibitor, enalapril maleate (MK-421), normalized the blood pressure and protected the progress of renal impairment without side effects.

Aged↗
PubMed2002

Changes of endothelin in streptozotocin-induced diabetic rats: effects of an angiotensin converting enzyme inhibitor, enalapril maleate.

Endothelin-1 (ET-1) concentrations are increased in patients with diabetes mellitus, particularly those with diabetic retinopathy, or essential hypertension. We hypothesized that ET-1 might participate in the development and progression of diabetic microangiopathy. In this study, the effects of the angiotensin converting enzyme (ACE) inhibitor, enalapril maleate, on diabetic angiopathy were examined in streptozotocin (STZ)-induced diabetic (STZ-DM) rats by monitoring variations in renal function and ET-1 concentrations in blood and organ tissues. Significant increases in kidney weight and in concentrations of urinary albumin, N-acetyl-fl-d-glucosamidase (NAG) and serum ET-1 were observed in the STZ-DM rats as compared with the non-diabetic rats, and the concentration of ET-1 in the kidneys tended to be increased. Microscopic and electron microscopic analyses showed increased mesangial cell proliferation, matrix expansion and enlarged mesangial area in the kidney of the diabetic rats. After administration of the ACE inhibitor, increased concentrations of urinary albumin and NAG in the STZ-DM rats were reduced to the control values with a slight improvement in the electron microscopic changes. These data suggest that ET-1 may be involved in the development and progression of diabetic nephropathy and may explain, in part, why diabetes is liable to complicate hypertension. ACE inhibitor may help to restore diabetic nephropathy in the STZ-induced diabetic rats.

Acetylglucosaminidase↗
PubMed1987

[Chronic oral toxicity study of proglumetacin maleate in beagle dogs].

A chronic oral toxicity test of proglumetacin maleate (PGM), an anti-inflammatory agent, was studied at dose-levels of 0, 0.6, 2.5 and 10.0 mg/kg/day using male and female beagle dogs. They were treated for 12 months, followed by 1 month recovery period. Excretion soft and mucous feces was observed in females of 2.5 mg/kg/day group. In addition, excretion of diarrheal and blood-tinged feces was also found in females of 10.0 mg/kg/day group. One female animal given 10.0 mg/kg/day of PGM was found dead on day 178 of administration. For about a month before death, diarrheal and blood-tinged feces, decreases in body weight and food consumption, and anemia had been noticed. At the autopsy, brown-cloudy ascitic fluid, adhesion of visceral organs, hyperemia or hemorrhage in the mucosa and serosa of the digestive tract, and an ulcer in the duodenum were found. No significant influences of PGM were noted on the changes of body weights, food and water consumptions, excluding the dead animal. A fecal occult blood test showed an increase in no. of animals with blood-positive reaction in 2.5 and 10.0 mg/kg/day groups of both sexes, especially marked in females of 10.0 mg/kg/day group. In urinary tests, no significant changes were found in any of the PGM-treated groups of both sexes; the dead one, however, showed decreases in urine volume and electrolyte excretion on month 6 of administration. No significant hematological changes associated with the administration of PGM were found in any of the animals excluding the dead one, in which anemia and inflammation-related findings were found on month 6 of administration. Serum-biochemical tests showed no significant changes in any of the PGM-treated groups of both sexes. No significant influences of PGM were found on ICG and PSP clearances, ocular fundus and ECG. At the autopsy performed at the end of administration, no significant changes were found in any of the PGM-treated groups of both sexes. Histopathologically, a duodenal ulcer and peritonitis-related findings were observed in the female dead animal of 10.0 mg/kg/day group. No influences of PGM were found in any of the tests performed at the end of the recovery phase. From these results, the non-effective dose of PGM was estimated to be 0.6 mg/kg/day, and the toxic doses of PGM to be more than 10.0 mg/kg/day for males and 10.0 mg/kg/day for females, respectively, in beagle dogs treated orally with PGM for 12 months.

Administration, Oral↗
PubMed1993

Pharmacokinetics of fluvoxamine maleate in patients with liver cirrhosis after single-dose oral administration.

The pharmacokinetics of fluvoxamine maleate were investigated in 13 patients with biopsy-proven liver cirrhosis. They received a single oral 100mg dose as an enteric-coated tablet, and plasma samples were collected up to 168h after administration. Geometric mean values for peak plasma concentrations and area under the plasma concentration-time curves (AUC) were 39 micrograms/L and 1338 micrograms.h/L, respectively. Mean (+/- SD) elimination half-life (t1/2) was 25 +/- 11h, and increased with higher plasma bilirubin levels, although no relationship between bilirubin and AUC was observed. AUC was about 50% higher in patients than in healthy volunteers from another similar study. This was mainly because of a longer t1/2. Although there is a great overlap between AUC values of fluvoxamine in patients and healthy volunteers, it is nevertheless concluded that in patients with signs of active liver disease, e.g. raised bilirubin, it is wise to lower the initial daily dose and to carefully monitor the patient during subsequent upward dose adjustments.

Administration, Oral↗
PubMedDate not supplied

Brompheniramine maleate: a double-blind, placebo-controlled comparison with terfenadine for symptoms of allergic rhinitis.

This was a double-blind, randomized, placebo-controlled, multicenter, parallel study comparing the effectiveness, at recommended doses, of an extended-release formulation of brompheniramine maleate and terfenadine in the treatment of allergic rhinitis. Subjects with symptoms of seasonal and/or perennial allergic rhinitis received brompheniramine 12 mg (n = 106), 8 mg (n = 105), terfenadine 60 mg (n = 106), or placebo (n = 53) twice daily for 14 days. On treatment days 3, 7, and 14, symptom severity ratings (i.e., rhinorrhea, sneezing, nasal congestion, itchy nose, eyes or throat, excessive tearing, postnasal drip) were completed by the physician; subjects and physicians each completed a global efficacy evaluation. Brompheniramine 12 mg and 8 mg and terfenadine were more effective than placebo (p < or = 0.05) on the physicians' global: brompheniramine 12 mg was more effective than terfenadine (p < or = 0.05) on days 7 and 14 and brompheniramine 8 mg on day 3. On the subjects' global evaluation, brompheniramine 12 mg and 8 mg and terfenadine were more effective than placebo (p < or = 0.05); brompheniramine 12 mg was more effective than terfenadine (p < or = 0.05) on days 7 and 14 and brompheniramine 8 mg on day 3. In general, brompheniramine 8 mg was comparable to terfenadine. On days 3 and 7, the total symptom and total nasal symptom severity scores for subjects receiving brompheniramine 12 mg were significantly more improved than for placebo (p < 0.05); terfenadine was not different from placebo; brompheniramine 12 mg was significantly better than terfenadine on day 7 (p < 0.05) for reducing total symptom severity and on days 3, 7, and 14 for reducing total nasal symptom severity. Adverse experiences were reported by 155 (41.9%) of the 370 subjects enrolled in the study. The overall rate of adverse experiences in the brompheniramine 12 mg treatment group (57.5%) was significantly greater (p < 0.05) than for brompheniramine 8 mg (38.1%), terfenadine (31.1%), and placebo (39.6%). In conclusion, an extended-release formulation of brompheniramine 12 mg or 8 mg bid alleviates allergic rhinitis symptoms and brompheniramine 12 mg provides significantly better relief of these symptoms than terfenadine 60 mg bid.

Administration, Oral↗