• YAKHAK HOEJI
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• v.29 no.1
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• pp.11-17
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• 1985

The behavioral effects of propranolol (60mg/kg) and metoprolol (100mg/kg) each alone and coadministered orally with cinnarizine (100mg/kg) were investigated and compared with each of betablockers alone treated group in rodents. Propranolol showed depressive effects through locomotor activity, conditioned avoidance response, rota-rod test, traction test, and analgesic effect in mice. When combined with cinnarizine and propranolol, the behavioral depressive effect of propranolol was reduced comparing with propranolol alone treated group. However, metoprolol alone or combined with cinnarizine didn't showed any behavioral depressive effect so much as propranolol.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.113-125
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• 1994

Many types of drugs affect functions of tile gastrointestinal tract. Investigators may be interested in discovery or pharmacological characterization of drugs as therapeutic agents intended for treatment of gastrointestinal disorders or in identification of gastrointestinal side effects of drugs intended for non-gastrointestinal indications. Examples of drug categories often associated with significant gastrointestinal side effects include cardiovascular drugs, antibiotics (erythromycin in particular), anti-inflammatory drugs, antiemetics, analgesics (especially opiates), antihistamines, antidepressants, and antipsychotics. Whether tile objective is development of gastrointestinal therapeutic agents or evaluation of gastrointestinal side effects, appropriate laboratory models for experimentation are essential.

• Journal of Oriental Neuropsychiatry
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• v.10 no.1
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• pp.53-78
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• 1999

As the average life span have been lengthened and the rate of senile population have been raised, chronic degenerative diseases incident to aging has been increased rapidly and become a social problem. With this social background, recently, the facts that oxygen radicals(OR) have toxic effects on Central Nervous System and Peripheral Nervous System and cause neuropathy such as Parkinson's Disease, Alzheimer Disease have been turned out, and accordingly lots of studies on the mechanism of the toxic effects of OR on nerves, the diseases caused by OR and the approaches to curing the diseases have been made. The purpose of this study is to examine the toxic effects caused by Glucose Oxidase(GO) and the effects of herbal extracts such as Chilbokyeum(CBY), Chilbokyeumga Acori Rhizoma(CAR), Acori Rhizoma(AR) on the treatment of the toxic effects. For this purpose, experiments with the cultured cell from the cerebrums of new born mice were done. The results of these experiments were as follows. 1. GO, a oxygen radical, decreased the survival rate of the cultured cells on NR assay, MTT assay and amount of neurofilaments and increased the amount of total protein, lipid peroxidation and the amount of LDH. 2. CBY have efficacy of increasing the amount of neurofilaments and total protein and decreasing lipid peroxidation and the amount of LDH. 3. CAR have efficacy of increasing the amount of neurofilaments and total protein and decreasing lipid peroxidation and the amount of LDH. 4. AR have efficacy of increasing the amount of neurofilaments and total protein. From the above results, It is concluded that Chilbokyeumgamibang has marked efficacy as a treatment for the damages caused in the GO-mediated oxidative process. And Chilbokyeumgamibang is thought to have certain pharmacological effects on controlling over aging and treating Dementia. Further clinical study of this pharmacological effects of Chilbokyeumgamibang should be complemented.

• Biomolecules & Therapeutics
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• v.22 no.4
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• pp.363-369
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• 2014

Synthetic cannabinoids (CBs) such as the JWH series have caused social problems concerning their abuse liability. Because the JWH series produces euphoric and hallucinogenic effects, they have been distributed illegally under street names such as "Spice" and "Smoke". Many countries including Korea have started to schedule some of the JWH series compounds as controlled substances, but there are a number of JWH series chemicals that remain uncontrolled by law. In this study, three synthetic CBs with different binding affinities to the $CB_1$ receptor (JWH-073, 081, and 210) and ${\Delta}^9$-tetrahydrocannabinol (${\Delta}^9$-THC) were evaluated for their potential for psychological dependence. The conditioned place preference test (unbiased method) and self-administration test (fixed ratio of 1) using rodents were conducted. $K_i$ values of the three synthetic cannabinoids were calculated as supplementary data using a receptor binding assay and overexpressed $CB_1$ protein membranes to compare dependence potential with $CB_1$ receptor binding affinity. All mice administered JWH-073, 081, or 210 showed significantly increased time spent at unpreferred space in a dose-dependence manner in the conditioned place preference test. In contrast, all tested substances except ${\Delta}^9$-THC showed aversion phenomenon at high doses in the conditioned place preference test. The order of affinity to the $CB_1$ receptor in the receptor binding assay was JWH-210 > JWH-081 >> JWH-073, which was in agreement with the results from the conditioned place preference test. However, no change in self-administration was observed. These findings suggest the possibility to predict dependence potential of synthetic CBs through a receptor binding assay at the screening level.

• The Korean Journal of Pharmacology
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• v.10 no.2
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• pp.43-54
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• 1974

The cactus family Cactaceae, numbering about 1,500 species, is a fleshy-stemmed perennial plant which is principally distributed in the south and north America. On the other hand, the cactus plant is presumed to be introduced into Korea in 1912-1945, thereafter it has been cultivated merely in favor of ornamentation with the exception of being occasionally used as medication among laymen. Opuntia elata which belongs to Opuntia genus, the Cactaceae family is one of the cacti being cultivated a great deal in Korea. Cho et. al. reported in 1974 that Opuntia dilenii manifested the cardiac inhibitory effect and oxytocic effect, and its mechanism might be partially due to the direct action. Besides this, there are few reports on the pharmacological research concerning Opuntia genus to be demonstrated in Korea. However, some other cacti have the remarkable pharmacological effects; the active ingredients, mescaline, anhalamine, anhalanine, etc. from Peyote cactus (Lophophora williamsii) belonging to Lophophora genus have the psychotomimetic and sympathomimetic effects, and the cardioactive glycosides from Cactus Grandifolius (Selenicereus grandiflorus) belonging to Cereus genus have the cardioactive and diuretic effects. The authors hereby inquired into this study to find out the propriety of the pharmacological properties of the ethanol extract of Opuntia elata (EX) on the heart, blood pressure, respiration, intestine and uterus in the experimental animals. The results of the experiment were as follows: 1. Administration of EX manifested the cardiac inhibitory effect caused by the negative inotropic action in the isolated heart of frog, and the pretreatment of atropine did not affect the inhibitory effect produced by EX. 2. Administration of EX manifested the transient hypotensive effect in the intact rabbit, and the pretreatment of atropine did not affect the hypotensive effect produced by EX. 3. Administration of the small dose of EX manifested no significant effect, but moderate dose or more the stimulating effect, and the large dose the asphyxia on the respiratory motility in the intact rabbit. 4. Administration of EX manifested the sustained augmentation of contractility in the excised duodenum of rabbit, and the pretreatment of atropine did not affect the stimulating effect produced by EX. 5. Administration of EX manifested the sustained augmentation of contractility in the excised pregnant uterus of rabbit, and the pretreatment of atropine and oxytocin did not affect the oxytocic effect produced by EX, but that of barium chloride more or less stimulated the oxytocic effect produced by EX.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.2
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• pp.380-388
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• 2002

The inhibitory effects of the traditional herbal medicine Hwao-tang on the progression of the atherosclerotic lesions were studied using the spontaneous familial hypercholesterolemia (FH) model, Kurosawa and Kusanagi-hypercholesterolemic (KHC) rabbits. Hwao-tang is activate blood circulation, vital energy and regulate menstruation, etc. Nowadays, Hwao-tang is mainly used for the treatment of inflammation, hyperlipemia and arteriosclerosis. However, pharmacological mechanisms of Hwao-tang on lipid metabolism and atherosclerosis formation are poorly understood. We have investigated the pharmacological effects of Hwao-tang on hypercholesterolemia and atherosclerosis using a spontaneous experimental model. In conclusion, the protection of extracts of HOT and its herbs on the ischemic infarction induced artificially might be related to their inhibitory effects on DIC, platelet coagulation and thrombic action. These suggest that Hwao-tang has inhibitory effects on the development of atheromatous plaque formation in spontaneous FH model rabbits. It is possible that the anti oxidative effects of Hwao-tang on LDL led to the beneficial effects observed in this study.

• 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.

• YAKHAK HOEJI
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• v.36 no.1
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• pp.17-25
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• 1992

The general and some other pharmacological actions of growth hormone without N-terminal methionine(rhGH) were investigated in animals. The hormone had no influences on the central nervous system and on body temperature at a high oral dose of 40 IU/kg in animals. It had neither analgesic nor antiepileptic actions at the high doses. In the isolated ileum and trachea of guinea-pig and isolated stomach fundus and uterus of rat, it showed neither contractive nor relaxing effects at a concentration of $1{\times}10^{-3}\;IU/ml$ in bath, and no inhibitory action at a dose of $1{\times}10^{-3}\;IU/ml$ against the contractions produced by histamine ($5{\times}10^{-5}\;g/ml$), serotonin($1{\times}10^{-5}\;g/ml$), acetylcholine($1{\times}10^{-5}\;g/ml$) and oxytocin($5{\times}10^{-3}\;IU/ml$). Furthermore, the intravenous injection of 20 IU/kg rhGH had no influences on the normal blood pressure and respiration in rabbits. These negative results in pharmacological profile are thought that the hormone may not elicit serious side effects. On the other hand, the rhGH exhibited a weak inhibitory action of glucose tolerance in normal rats, significantly lowered the blood glucose contents in adrenalectomized rats 20 min after i.v. administration of 80 IU/kg, and showed a significant inhibitory effect on in vitro glycerol release in epinephrine-stimulated epididymal fat pad segments of rats.

• Journal of mucopolysaccharidosis and rare diseases
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• v.2 no.2
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• pp.43-45
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• 2016

Whole body energy balance is achieved through the coordinated regulation of energy intake and energy expenditure in various tissues including liver, muscle and adipose tissues. A positive energy imbalance by excessive energy intake or insufficient energy expenditure results in obesity and related metabolic diseases. Although there have been many obesity treatment trials aimed at the reduction of energy intake, these strategies have achieved only limited success because of their associated adverse effects. Serotonin is among those traditional pharmacological targets for anti-obesity treatment because central 5-HT functions as an anorexigenic neurotransmitter in the brain. Thus, there have been many trials aimed at increasing the activity of 5-HT in the central nervous system, and some of the developed methods are already used in the clinical setting as anti-obesity drugs. However, recent studies suggest the new functions of peripheral serotonin in energy homeostasis ranging from the endocrine regulation by gut-derived serotonin to the autocrine/paracrine regulation by adipocyte-derived serotonin. Pharmacological inhibition of 5-HT synthesis leads to inhibition of lipogenesis in epididymal white adipose tissue (WAT), induction of browning in inguinal WAT and activation of adaptive thermogenesis in brown adipose tissue (BAT). Fat specific Tph1 knock-out (Tph1 FKO) mice exhibit similar phenotypes as mice with pharmacological inhibition of 5-HT synthesis, suggesting the localized effects of 5-HT in adipose tissues. In addition, Htr3a KO mice exhibit increased energy expenditure in BAT and Htr2a KO mice exhibit the decreased lipid accumulation in WAT. These data suggest the clinical significance of the peripheral serotonergic system as a new therapeutic target for anti-obesity treatment.

• Mass Spectrometry Letters
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• v.10 no.1
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• pp.18-26
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• 2019

We developed a bioanalytical method for simultaneous determination of nine NBOMe derivatives (25H-NBOMe, 25B-NBOMe, 25E-NBOMe, 25N-NBOMe, 25C-NBOH, 25I-NBOH, 25B-NBF, 25C-NBF, and 25I-NBF) in human plasma using liquid chromatography tandem mass spectrometry (LC-MS/MS). Human plasma samples were pre-treated using solid-phase extraction. Separation was achieved on a C18 column under gradient elution using a mobile phase containing 0.1% formic acid in acetonitrile and 0.1% formic acid in water at a flow rate of 0.3 mL/min. Mass detection was performed in the positive ion mode using multiple reaction monitoring. The calibration range was 1-100 ng/mL for all quantitative analytes, with a correlation coefficient greater than 0.99. The intra- and inter-day precision and accuracy varied from 0.85 to 6.92% and from 90.19 to 108.69%, respectively. The recovery ranged from 86.36 to 118.52%, and the matrix effects ranged from 27.09 to 99.72%. The stability was acceptable in various conditions. The LC-MS/MS method was validated for linearity, accuracy, precision, matrix effects, recovery and stability in accordance with the FDA guidance. The proposed method is suitable for reliable and robust routine screening and analysis of nine NBOMe derivatives in forensic field.