• The Korean Journal of Pharmacology
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• v.11 no.2
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• pp.19-27
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• 1975

Haloperidol, a butyrophenone, was synthetized by Janssen and introduced for the treatment of psychosis. Although structurally different from the phenothiazines, the butyrophenones share many of their pharmacological properties, such as inhibition of conditioned avoidance response, blocking effect of amphetamine reaction, producing catalepsy, antishock effect and protection against the lethal effects of catecholalmines. Chlorpromazine can lower the arterial blood pressure through its adrenergic blocking activity, its direct effect in relaxing vascular smooth muscle, its direct effect in depressing the myocardium and its action in a complex manner on the central nervous system. In the case of haloperidol, however, was not clarified the mechanism of lowering the blood pressure. The present paper describes the effects of haloperidol on cardiovascular system to investigate the mechanisms of its actions on the arterial blood pressure. The results are followings; 1. In anesthetized cats, intravenous administration of haloperidol and chlorpromazine in the dose of 0.1mg/kg produced a slight decrease in the blood pressure, which followed by complete recovery within $30{\sim}60$ minutes. In the dose of 3mg/kg, however, both produced an abrupt and marked decrease of the blood pressure, which followed by delayed recovery. 2. Haloperidol in the dose ranges of 0.1mg to 3.0mg/kg tended to produce the heart rate slowing in the cats, while chlorpromazine has no effect on the rate. 3. Following administration of haloperidol or chlorpromazine, epinephrine reversal in the arterial blood pressure was observed in the cat, however the responses of norepinephrine and acetylcholine were little affected. 4. In the isolated rabbit atrium the contractility was depressed by haloperidol in the doses over 0.5mg per 100ml, but the rate was not affected. In contrast, the epinephrine-induced contractility was not depressed after haloperidol treatment. However, the increased rate of atrium by epinephrine was partially blocked after haloperidol. 5. In the isolated rabbit aortic strip, epinephrine-induced contraction was blocked by haloperidol. With the above results, it may be concluded that the hypotensive effect of haloperidol was largely due to ${\alpha}$-adrenergic blocking properties and the direct effect in depressing the myocardium as well as its action on central nervous system.

• Microbiology and Biotechnology Letters
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• v.24 no.3
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• pp.321-326
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• 1996

In the course of screening for new bioactive compounds from oligotrophs in soil, a microorganism, designated as SA-246 and now identified as Micromonospora sp., has been shown to produce a strong antibacterial compound. The active compound was purified from broth filtrate by ethylacetate extraction, silica gel column chromatography, preparative TLC and HPLC, and was identified as crisamicin A based on mass and NMR spectral data. The compound SA- 246 exhibited not only strong antibacterial activity against Gram-positive bacteria but also cytotoxicity against cancer cell lines such as A549 (lung), SK-OV-3 (ovarian), SK-MEL-2 (melanoma), XF498 (central nervous system) and HCT15 (colon).

• Journal of Dairy Science and Biotechnology
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• v.27 no.1
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• pp.45-51
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• 2009

$\gamma$-aminobutyric acid (GABA) is a ubiquitous nonprotein amino acid that is produced primarily by $\alpha$-decarboxylation of L-glutamic acid (Glu) catalyzed by the enzyme glutamate decarboxylase (GAD). It is well known as a neurotransmitter that regulates inhibitory neurotransmission in the mammalian central nervous system. In addition, GABA has been proved to be effective for lowering blood pressure in mammals. This paper is intended to provide basic information about GABA, including the functional and biological activity of GABA, GABA production by lactic acid bacteria, and the utilization of GABA in the production of dairy products.

• The Journal of Korean Physical Therapy
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• v.24 no.4
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• pp.262-267
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• 2012

Purpose: This study was designed to analyze the differences in cerebral cortex activity of the elderly after extracting the movement related cortical potentials (MRCPs) from electroencephalogram (EEG) during a concentric and eccentric contraction of the elbow joint flexors, and entering them into the brain-mapping program to make the images. Methods: Right-dominant normal elderly people were divided into an eccentric contraction group and a concentric contraction group. Then, their MRCPs were measured using EEG and sEMG, during an eccentric and concentric contraction. Then, they were converted into images using the brain-mapping program. Results: Eccentric contraction group's $C_3$ and Cz showed statistically higher mean values of MRCP positive potential than the concentric contraction group. Conclusion: Researching a cerebral cortex activity, using MRCP, would provide basic data for clinical neuro-physiological researches on aging or neural plasticity of patients with a central nervous system injury.

• The Korean Journal of Pharmacology
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• v.30 no.2
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• pp.167-179
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• 1994

Recent evidence indicates that glial cells have a wide range of funtions which are critical for maintaining a balanced homeostatic environment in the central nervous system(CNS) peripheral nervous system(PNS). Morever, astrocytes are known to participate in the tissue repair and neuroimmunologic events within the CNS through many kinds of growth factors and cytokines. We investigated the effect of $TGF\;{\beta}_1$, on the growth and biochemical changes of rat glial cells in culture. The proliferative effect was determined by $^3H-thymidine$ uptake and the double immunostain with anti-cell-specific marker and anti-Bromodeoxyuridine(BrdU) antibody. To check the effect of biochemical changes we compared the amounts of glial fibrillar acidic protein(GFAP) and the activity of glutamine synthetase(GS) in astrocyte. And the amounts of myelin basic protein and the activity of 2',3'-cyclic nucleotide phosphohydrolase(CNPase) were measured in oligodendrocyte and the amounts of peripheral myelin in Schwann cell. When $TGF\;{\beta}_1$, was treated for 2 days with cultured glial cell, $TGF\;{\beta}_1$, decreased the $^3H-thymidine$ uptake and proliferation index of double immunostain of astrocytes, which indicates the inhibition of astroglial DNA synthesis, but stimulated the growth of Schwann cell. Also, $TGF\;{\beta}_1$, decrease the GS activity and increased the amounts of GFAP in astrocyte. In the case of Schwann cells the amounts of peripheral myelin was increased when treated with $TGF\;{\beta}_1$. However, $TGF\;{\beta}_1$, didn't show any effect on the proliferation and biochemical changes in oligodendrocyte. These results suggest that $TGF\;{\beta}_1$, might have a critical action in the regulation of proliferation and biochemical changes in glial cells, especially astrocyte.

• BMB Reports
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• v.40 no.6
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• pp.1077-1082
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• 2007

Human glutamate dehydrogenase exists in hGDH1 (housekeeping isozyme) and in hGDH2 (nerve-specific isozyme), which differ markedly in their allosteric regulation. In the nervous system, GDH is enriched in astrocytes and is important for recycling glutamate, a major excitatory neurotransmitter during neurotransmission. Chloroquine has been known to be a potent inhibitor of house-keeping GDH1 in permeabilized liver and kidneycortex of rabbit. However, the effects of chloroquine on nerve-specific GDH2 have not been reported yet. In the present study, we have investigated the effects of chloroquine on hGDH2 at various conditions and showed that chloroquine could inhibit the activity of hGDH2 at dose-dependent manner. Studies of the chloroquine inhibition on enzyme activity revealed that hGDH2 was relatively less sensitive to chloroquine inhibition than house-keeping hGDH1. Incubation of hGDH2 was uncompetitive with respect of NADH and non-competitive with respect of 2-oxoglutarate. The inhibitory effect of chloroquine on hGDH2 was abolished, although in part, by the presence of ADP and L-leucine, whereas GTP did not change the sensitivity to chloroquine inhibition. Our results show a possibility that chloroquine may be used in regulating GDH activity and subsequently glutamate concentration in the central nervous system.

• Biomolecules & Therapeutics
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• v.20 no.2
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• pp.133-143
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• 2012

Matrix metalloproteinases (MMPs) are a subfamily of zinc-dependent proteases that are re-sponsible for degradation and remodeling of extracellular matrix proteins. The activity of MMPs is tightly regulated at several levels including cleavage of prodomain, allosteric activation, com-partmentalization and complex formation with tissue inhibitor of metalloproteinases (TIMPs). In the central nervous system (CNS), MMPs play a wide variety of roles ranging from brain devel-opment, synaptic plasticity and repair after injury to the pathogenesis of various brain disorders. Following general discussion on the domain structure and the regulation of activity of MMPs, we emphasize their implication in various brain disorder conditions such as Alzheimer's disease, multiple sclerosis, ischemia/reperfusion and Parkinson's disease. We further highlight accumu-lating evidence that MMPs might be the culprit in Parkinson's disease (PD). Among them, MMP-3 appears to be involved in a range of pathogenesis processes in PD including neuroinflamma-tion, apoptosis and degradation of ${\alpha}$-synuclein and DJ-1. MMP inhibitors could represent poten-tial novel therapeutic strategies for treatments of neurodegenerative diseases.

• International Journal of Contents
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• v.16 no.1
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• pp.57-64
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• 2020

We sought to compare upper extremity muscle activity between handwriting on paper and touchscreen with dominant and non-dominant hands in younger adults (age 23.90±1.12) and the elderly (age 75.55±5.76). Muscle activity (percent of maximum voluntary contraction) in the biceps brachii muscle, triceps brachii muscle, flexor carpi ulnaris muscle, and extensor carpi ulnaris muscle was measured using an electromyography device. As a result, our data indicate that muscle activity is lower in younger adults than the elderly. Besides, muscle activity is lower in the dominant versus non-dominant hand, and lower when writing using a touchscreen than on paper. These results can be used to support recommending touchscreens in the elderly. Also, they can be used as baseline data for comparing the performance of non-paretic side and paretic side in patients relative to the central nervous system.

• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.211-219
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• 1993

The general and some pharmacological actions of DWP 302 were investigated in animals and the following results were obtained. In central nervous system, DWP 302 had no effects on the pentobarbital induced anaesthesia, locomotor activity, rotarod test, traction test, analgesic action in the mice and body temperature in the rat. DWP 302 showed no depressive action on the convulsion induced by strychnine and electronic shock. From these results, DWP 302 was considered to have no or little pharmacological effect on the central nervous system. Furthermore, DWP 302 had no influences on the normal blood pressure and heart rate. In the isolated ileum of guinea pig, DWP 302 showed neither contractive nor relaxing effects against the acetylcholine ($10^{-6}g/mι$), histamine ($10^{-6}g/mι$) and $BaCl_2$ ($10^{-4}g/mι$) at a concentration of $1.9{\times}10^{-4}g/mι$ in bath. But it caused a slight increase in basal tone at a concentration of $6.3{\times}10^{-4}g/mι$ and this effect was inhibited by atropine $10^{-7}g/mι.$ In the isolated trachea and vas deference, DWP 302 showed no effect on the contractions produced by histamine and norepinephrine, respectively. And DWP 302 showed no effect on the contractions produced by acetylcholine and oxytocin in the isolated nonpregnant rat uterus. DWP 302 had no effect on bile excretion, urine volume, pH and gastrointestinal motility, But, DWP 302 showed a significant inhibitory effect on gastric secretion in the rat.

• Korean Journal of Clinical Pharmacy
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• v.20 no.2
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• pp.128-137
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• 2010

This review summarizes gender differences in pharmacokinetics, pharmacodynamics, and adverse drug reactions. Gender differences in pharmacokinetics are categorized by four major factors: absorption/bioavailability, distribution, metabolism, and elimination. There are sex-based differences in gastric emptying time, gastric alcohol dehydrogenase activity, apparent volume of distribution, ${\alpha}1$-acid glycoprotein level, phase I (CYP) and phase II metabolizing enzymes, glomerular filtration rate, and drug transporters. This review also reports gender differences in pharmacokinetics and pharmacodynamics of cardiovascular agents, central nervous system acting agents and antiviral agents. In addition, it has been reported that females experience more adverse reactions such as coughing, tachycardia, nausea, vomiting, rash, hypersensitivity, hepatotoxicity, and metabolic disorder after taking cardiovascular, central nervous system acting and antiviral agents. Therefore, in order to provide optimal drug dosage regimens both in male and female, gender differences in pharmacokinetics, pharmacodynamics, and adverse drug reactions must be considered.