• YAKHAK HOEJI
• /
• v.26 no.4
• /
• pp.189-196
• /
• 1982

Piperine was reported to have a potential central nervous system (CNS) depressant activity in mice. In order to search a more active and less toxic compound than piperine and to elucidate the active group of piperine, the aromatic amides (10 compeunds) and aromatic esters (10 cempounds) of 3, 4-methylenedioxycinnamic acid were synthesized and evaluated on CNS depressant activity in comparison with piperine. The pharmacological tests conducted are as follows; (1) Acute, toxicity, (2) Antagonism against strychnine induced conduced convulsion, (3) Antagonism against maximal electrobhock seizure, (4) Rotarod test, (5) Potentiation of hexobarbital sleeping time. It was observed that 3, 4-methylendioxycinanamic acid derivatives were less toxic than piperine, and showed no significant CNS depressant activities. These facts indicate that the piperoyl group might be concerned with the pharmacological activity of piperine.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.3
• /
• pp.1011-1016
• /
• 2011

A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data confirmed the structure of the synthesized compounds. The derivatives of these moieties were evaluated for anticonvulsant activity by MES model and neurotoxicity by rotarod method. The synthesized compounds showed good potential for anticonvulsant activity besides this, the compounds also showed neurotoxic effect. It was observed that compounds with $OCH_3$ at 3, 4 position of phenyl ring [5(a-l)] showed less protection against convulsions as compared to compounds having unsubstituted phenyl ring [4(a-l)].

• Bulletin of the Korean Chemical Society
• /
• v.30 no.7
• /
• pp.1445-1451
• /
• 2009

New benzotriazoles (5-8) or dibenzodiazepine derivatives (11-18) were synthesized starting from 3-[(2-amino- 4,5-disubstitutedphenyl)amino]-5,5-disubstitutedcyclohex-2-enones (1-4) through internal coupling of their diazonium salts or internal Mannich reaction in the presence of aromatic aldehydes. Pharmacological evaluation of benzotriazole and dibenzodiazepine derivatives for their clozapine-like properties revealed that dibenzodiazepine 11 bearing 4-bromophenyl group exhibited the same antipsychotic activity as the reference drug clozapine while the activity of benzotriazole 7 was 25% lesser than that of clozapine. Moreover, compounds 7 and 11 did not show significant CNS depressant activity as well as no or slight neurotoxicity on contrast to clozapine when tested in mice using forced swim, rotarod and horizontal screen tests.

• Journal of International Academy of Physical Therapy Research
• /
• v.7 no.2
• /
• pp.999-1005
• /
• 2016

The purpose of this study was to investigate the effects of low-intensity cardiac rehabilitation exercise on the cardiac function and the degree of fibrosis in an older white rat model. This study used male Sprague-Dawley white rats that were 50 weeks old. After the acute myocardial infarction induction, Twenty of the rats were randomly allocated into an experimental group and a control group, and each of the groups consisted of 8 rats. In the experimental group, the exercise was conducted for six weeks, 30 minutes a day, five days a week, using a Rotarod treadmill for animals. The degree of myocardial fibrosis was significantly repressed in the experimental group($13.69{\pm}1.90%$) and in the control group($15.67{\pm}1.54%$)(p<0.05). However, fractional shortening and ejection fraction did not show a significant difference. The results of this study suggest that cardiac rehabilitation with low intensity treadmill exercise repress the myocardial fibrosis.

• Biomolecules & Therapeutics
• /
• v.7 no.3
• /
• pp.285-291
• /
• 1999

DA-7101 is a new combined formulation of cefatrizine:clavulanic acid (2:1) under development as oral abtibiotics. The general pharmacological properties of DA-7101 on central nervous, cardiovascular, gas-trointestinal and other organ systems were studied by oral administration, in vivo and in vitro. DA-7101 had no marked effects all tests studied such as general behavior, hexobarbital-induced sleeping, spontaneous activity, anticonvulsion, body temperature, acetic acid-induced writhing, rotarod performance, heart rate and blood pressure in cats, isolated ileum movement, intestinal transition, gastric juice secretion and urine volume and electrolytes in rats. But exceptionally at the highest dose of 900 mg/kg, DA-7101 increased hexobarbital-induced sleeping time, caused a slight hypotension and decreased the secretion of gastric juice. These results suggest that at the estimated clinical dose DA-7101 would not bring about any serious acute adverse effects clinically.

• Korean Journal of Pharmacognosy
• /
• v.24 no.3
• /
• pp.231-234
• /
• 1993

Neuropharmacological profile of Humulus lupulus (hop) extract was studied in mice. At doses above 100 mg/kg(i.p.), it decreased spontaneous locomotor activity and raised the nociceptive threshold in the hot-plate test. At doses above 250 mg/kg (i.p.), it increased pentobarbital-induced sleeping time and produced muscle relaxant effect. At the dose of 500 mg/kg, anticonvulsive effect against pentylenetetrazole-induced convulsion and hypothermic effect was observed.

• YAKHAK HOEJI
• /
• v.39 no.5
• /
• pp.471-479
• /
• 1995

The recombinant human epidermal growth factor(DWP 401) was investigated on the pharrnacological actions. DWP 401 had no effects on the hexobarbital-induced sleeping time, locomotor activity, rotarod test, body temperature, analgesic action and anticonvulsant action in mice. It also had no influences on the isolated tracheal muscle and ileum of guinea-pig, isolated uterus and fundus strip of rats. Slight hypotensive action with effect on respiration was revealed at a dose of 8 g/kg i.v. of DWP 401 in rabbits. DWP 401 exhibited a weak inhibitory action of glucose tolerance in normal rats, significantly lowered the blood glucose contents in adrenalectomized rats at .a concentration of 160 g,/kg, and produced a significant inhibitory effect on leucocyte migration in CMC-pouch of rats at a concentration of 32 g/rat. Furthermore, DWP 401 showed a significant decrease on gastric juice volume and acidity. However. DWP 401 had no intestinal propulsion rate and influence on urine excretion.

• Journal of Preventive Medicine and Public Health
• /
• v.26 no.2 s.42
• /
• pp.222-230
• /
• 1993

Industrial glues, known as 'Bonds' in Korea, contain many kinds of organic solvents, and glue sniffing of youths became one of the social problems in Korea. Mixed exposures to solvents by glue sniffing may induce chronic toxicities different from those by exposures to solvents of single component. To test effects of the glue sniffing on weight gain or central nervous system, two groups of 20 male Sprague-Dawley rats were exposed to air(control group) or vapors of the glues to narcotic status(exposed group), and weight check, tail flick test, hot plate test, rotarod treadmill test were done on the 14th,24th, 36th, 45th, 53rd, 86th, 102nd, 117th, 134th and 151st days after the first exposure. On the 188th day, their brains were excised and examined by a pathologist. Weight gain, controlled against time change, showed significant difference between the groups, but response times in tail flick test, hot plate tests, and rotarod treadmill test didn't. In pathological examination with blind method, no macroscopic or microscopic differences were found between the two groups. These results suggests that organic lesion in central nervous system may not ensue glue sniffing, but, before firm conclusion, more studies in various exposure conditions should be followed.

• Toxicological Research
• /
• v.20 no.3
• /
• pp.251-261
• /
• 2004

A large number of chemical pollutants including phthalates, alkylphenolic compounds and organochlorine pesticides have the ability to disrupt endocrine function in animals, and alter cog-nitive function. Because hormone mediated events play an important role in central nervous system development and function, the changes in cognitive function seem to be mediated by the endocrine-like action of these chemicals. The present study therefore was designed to investigate effect of bisphenol A (BPA), an endocrine disrupting chemical on neuro-behavial patterns, and expression of estrogen receptors and tyrosine hydroxylase, a limiting enzyme of dopamine synthesis pathway. BPA was treated orally for 3 weeks into 3 week old mice, and then the neuro-behavial patterns (stereo-type behaviors such as jumping rearing and forepaw tremor, climbing behavior, tail flick, rotarod and locomotor activity), and the expression of estrogen receptors and tyrosine hydroxylase were deter-mined every 3 week for 9 weeks. During the treatment of BPA, the food uptake and body weight increase were not significantly changed. BPA resulted in the increased stereotype behaviors (jump-ing, rearing and forepaw tremor) 6 or 9 weeks after treatment. The time response to tail flick and locomotor activity were decreased by the treatment of BPA, whereas the time for rotarod was increased by the treatment of BPA. The expression of estrogen receptor alpha and beta was increased in the brain and pituitary gland. Maximum expression was found in the brain after 9 week of 100 mg/kg BPA treatment and in the pituitary gland after 6 week of 100 mg/kg BPA treatment. Tyrosine hydroxylase was increased in dose and time dependent manners in the brain but no change was found in the pituitary gland. The present data show that exposure of BPA in the young mice could alter expression of estrogen receptors and dopamine synthesis pathway, thereby modulate neuro-behavial patterns (increase of stereotype behaviors but decrease locomotor activity).

• Biomolecules & Therapeutics
• /
• v.14 no.4
• /
• pp.253-258
• /
• 2006

LDD175(4-choloro-7-trifluoromethyl-10H-benzo[4,5]furo[3,2-b]indole-l-carboxylic acid) is one of benzofuroindole derivatives that act as a potent $BK_{Ca}$ channel openers. In the process of testing LDD175 as a new drug candidate, an acute toxicity study was carried out in mice. The mice were administered LDD175 intraperitoneally at dose of 0.2, 1, 10, 50, 100, 200, 400, 800mg/kg and orally at dose of 10, 100, 400, 800mg/kg body weight. After administering LDD175, the vital organs such as the liver, kidney and spleen were carefully observed for any significant pathological features or differences from the norm over a l4-day period. LDD175 did not induce any short-term toxicity at doses less than 100mg/kg. A $LD_{50}$ of LDD175 was 2493mg/kg in male mice and 4908mg/kg in female mice. Weight reduction was observed at a dose of 800mg/kg in male, and 400 and 800mg/kg in female. The kidney weight decreased in females after an intraperitoneal injection of LDD175 high dose(>400mg/kg, i.p.), and the spleen weight increased in the male(800mg/kg, i.p.) and female(400mg/kg, i.p.) mice. Inspite of the change in organ weights, there were neither histopathological changes nor any gross morphological abnormalities detected in any organ. LDD175 did not produce significant changes in the general behavior at doses of <200mg/kg, but decreased locomotor activity was observed at an intraperitoneal dose of 400mg/kg. Its effects on the locomotor activity and activity on the rotarod were tested and compared with the effects of diazepam 5mg/kg. The decrement in the locomotor activity and the activity on the rotarod induced by LDD175 was less serious than it by diazepam.