• Biomolecules & Therapeutics
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• v.11 no.1
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• pp.51-57
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• 2003

General pharmacological properties of ADP, a new pharmaceutical composition, which contains a mixed water extract obtained from the mixture of Phellodendron cortex (Phellodendron amurense) and Anemarrhena rhizoma (Anemarrhena asphodeloides), as the active ingredients, were investigated in experimental animals administering orally and in vitro test system. ADP had no influences on general behavior, pentobarbital sleeping time, spontaneous motor activity, motor coordination of mice, normal body temperature, chemoshock produced by pentylenetetrazole and writhing syndromes induced by 0.8% acetic acid at the dose of 150 and 1500 mg/kg. Gastric secretion of rats and intestinal motility of mice were not also influenced by the administration of ADP at doses of 150 and 1500 mg/kg, with the exception of the significant decrease of free HCI concentration at a dose of 1500 mg/kg in rats. ADP (150 and 1500 mg/kg) did not alter mean arterial blood pressure and heart rate in conscious rats. ADP given to anesthetized rats showed no effect on respiratory rate at the same doses. In in vitro experiments, ADP at the concentration of 150 mg/L did not show direct effect and inhibitory or augmentative action on histamine- or acetylcholine-induced contractions in the isolated ileum of guinea-pig. Taken together, these results indicate that ADP does not induce any adverse effects in experimental animals.

• YAKHAK HOEJI
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• v.34 no.6
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• pp.439-446
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• 1990

The general pharmacological actions of recombinant human growth hormone (rHGH) were investigated. It had hypothermic action but neither sedative nor analgesic action. No pharmacological effects were observed in isolated guinea pig ileum and tracheal muscle and rat fundus and uterus. Slight hypotensive action with no effect on respiration was revealed at a dose of 20 IU/kg i.v. of rHGH in rabbits. 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 (80IU/kg), and produced a significant inhibitory effect on in vitro glycerol release in epinephrine-stimulated epididymal fat pad segments of rats.

• Biomolecules & Therapeutics
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• v.6 no.4
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• pp.406-411
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• 1998

The pre-mixed $_{13}C$-urea powder preparation in ${Helikit}_{TM}$ for test of Helicobacter pylori was evaluated for pharmacological properties. The oral doses of the preparation used in mice were 30-fold as compared to human doses. The results obtained in the present study demonstrate that spontaneous movement, hexobarbital-induced hypnosis, rotarod performance, body temperature, acetic acid-induced writhing syndrome, chemical and electroshock convulsion, pupil size and intestinal propulsion had not been affected at the oral doses of 230, 700 and 2100 mg/kg in mice. The blood pressure was slightly elevated as given intravenously in rats at a dose of 5 mg/kg of the preparation, but respiration was not influenced at the dose. In isolated guinea pig ileum and rat fundus preparation, the preparation at a concentration of $1{\times}10^{4}$ g/ml neither caused any direct effect nor inhibited the contraction produced by acetylcholine, histamine or 5-hydroxytryptamine. These results reported here provide evidence that pre-mixed $^{13}C$ 13/C-urea powder preparation is free of general pharmacological properties performed in oral administration.

• Biomolecules & Therapeutics
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• v.4 no.4
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• pp.385-390
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• 1996

General pharmacological properties of urinary trypsin inhibitor (UTI) following intravenous administration of 1,000,000 units/kg were examined in terms of effects on central nervous system, cardiovascular system, respiratory system, gastrointestinal system in mice, rats and rabbits. Administration of UTI (1,000,000 units/kg, iv) had no effect on central nervous system; no influences on pentobarbital sleeping time, spontaneous activity, normal body temperature, chemoshock produced by pentylenetetrazole solution, writhing syndromes induced by 0.6% acetic acid solution, and motor coordination of mice. The administration of UTI (1,000,000) units/kg, iv) in rats had no effect on systolic blood pressure and pulse rate. UTI (500,000 units/kg, iv) given to anesthetized rabbits showed no effect on respiratory rate. However, it showed significant elevation of respiratory rate at the concentration of 1,000,000 units/kg. Gastric secretion of rat and intestinal motility of mice were not influenced by the dose of 1,000,000 units/kg. In terms of autonomic nervous system, the material did not show direct effect and inhibitory or augmentative action of histamine- or acetylcholine-induced contraction at the concentration of 2,000 units/ml in the isolated ileum of guinea pig.

• YAKHAK HOEJI
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• v.36 no.2
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• pp.115-119
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• 1992

The possibility as an anti-inflammatory drug of Prunus davidiana which have been used in Korean folk medicine for treatment of neuritis and rheumatism was investigated on carrageenin-induced paw edema in rats. The MeOH extract exhibited potent inhibitory effect on carrageenin-edema rats when topically applicated. On the other hand, it did not show any effect when orally tested. It also had no influences on isolated ileum of guinea pig and anti-platelet aggregating activities. Thus, it appears from the present findings that the MeOH extract of P. davidiana may be utilizable only for the external treatment of inflammed sites. This study was also conducted to further isolation of flavonoids from the EtOAc soluble fraction and characterized as persiconin and isosakuranin by spectrometric analysis.

• Biomolecules & Therapeutics
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• v.6 no.2
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• pp.159-164
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• 1998

General pharmacological properties of recombinant human parathyroid hormone (hPTH) were examined. The administration of hPTH (7, 35 and 175 lU/kg sc) in mice had no effects in general behavior and central nervous system, and no influences on normal body temperature, writhing syndromes induced by 0.7% acetic acid solution and chemoshock produced by strychnine and pentetrazol solution. hPTH (9 and 44 lU/kg, sc) given to anesthetized rabbits showed no effect on blood pressure of carotid artery and respiration, and it did not influence the responses produced by injection of acetylcholine or epinephrine. It showed no direct effect at 4.4$\times$10$_{-2}$IU/ml in isolated stomach fundus and uterus of rats and ileum of guinea-pig, and it also showed no inhibition of contraction produced by acetylcholine, oxytocin, serotonin and histamine in the above-mentioned preparations. It did not influence intestinal propulsion at the doses of 7,35 and 175 lU/kg sc in mice. This drug exhibited no effect on urinary excretion at the doses of 7 and 35 lU/kg sc in rats. However, at a dose of 175 lU/kg sc, it showed a decreased urination along with decreased excretion of potassium, sodium and chloride ion. These results indicate that hPTH does not exert any of serious pharmacological effects except the inhibition of urination at a highest dose used.

• Biomolecules & Therapeutics
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• v.7 no.1
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• pp.89-96
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• 1999

CJ-50002 is an oral vaccine against V.vulnificus infection composed of whole cell lysate of V. vulnificus. The general pharmacological properties of CJ-50002 were evaluated in various animals and in vitro system. CJ-50002 at oral doses of 0.2, 2 and 20 mg/kg had no effect on general behavior in mice, chromo- and electro-convulsions in mice, writhing syndrome induced by acetic acid in mice, body temperature in rats, charcoal meal propulsion in mice and urine and electrolytes excretion in rats. However, oral administration of CJ-50002 at dose of 20 mg/kg prolonged the hexobarbital-inuced sleeping inducing time in mice. In anesthetized dogs, CJ-50002 showed no effect on blood pressure, heart rate and ECG but decreased the respiratory rate and femoral blood flow at dose of 20 mg/kg. p.o. CJ-50002 had no effect on the contractile response of the isolated guinea pig ileum to various spasmogen at concentrations of 0.2, 2 and 20 $\mu\textrm{g}$/ml, respectively. Since these pharmacological effects of CJ-500o2 were observed at dose much greater than those in clinical use (approximately 0.16 mg/kg, p.o.), it is likely that this vaccine may be relatively free of undesirable effects in clinical practice.

• Biomolecules & Therapeutics
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• v.4 no.2
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• pp.154-161
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• 1996

General pharmacological properties of LB-00014, an erythropoietin which was produced by recombinant DNA technique in Biotech Research Institute, LG Chemical Ltd. were examined. The administration of LB-00014 (60, 600, 6000 IU/kg, iv) in mice had no effect in general behavior and central nervous system, and no influences on normal body temperature, writhing syndromes induced by 0.7% acetic acid solution and chemoshock produced by strychnine and pentetrazole solution. LB-00014 (60, 600, 6000 IU/kg, iv) given to anesthetized rabbits showed no effect on blood pressure of carotid artery and respiration rates, and it did not influence the responses produced by injection of acetylcholine or epinephme. The administration of LB-00014 (601, 600, 6000 IU/kg, iv) in rats had no effect on the plasma prothrombin time, activated partial thromboplastin time and hemolytic action. The platelet aggregation induced by collagen in human plasma was not influenced by LB-00014 (10, 100, 1000 lU/kg, iv). It showed no direct effect at 100 and 1000IU/m1 in isolated stomach fundus and uterus of rats and ileum of guinea-pig, and it also had no inhibition of contraction produced by acetylcholine, oxytocin, serotonin and histamine in the above-mentioned preparations. It did not influence gastric secretion, pH and acid output at 6000 IU/kg, iv in rats, but showed a significant increase in intestinal propulsion of mice at 6000 IU/kg, iv. Its administration (60, 600, 6000 lU/kg, iv) caused no effect on urine and electrolyte excretion in rats. These results indicate that LB-00014 does not exsert any of serious pharmacological effects.

• The Korean Journal of Pharmacology
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• v.30 no.1
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• pp.49-57
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• 1994

The binding properties of oxomemazine to muscarinic receptors using the ability of oxomemazine to inhibit $[^3H]QNB$ binding in membrane fractions of rat cerebrum and guinea pig ventricle and ileum were investigated. $[^3H]QNB$ bound to a single class of muscarinic receptors with a dissociation constant of approximately 60 pM in three tissue preparations. Pirenzepine and oxomemazine inhibited $[^3H]QNB$ binding in cerebrum with a Hill coefficient lower than unity, and the inhibition data were best described by a two-site model. The relative densities of the high $(M_1)\;and\;low\;(M_2)$ affinity sites for pirenzepine were 60 and 40%, with corresponding Ki values of 16 and 431 nM, and those $(O_H\;and\;O_L)$ for oxomemazine 40 and 60%, with corresponding Ki values of 80 and 1350 nM. However, the inhibition data of both drugs vs $[^3H]QNB$ in ventricle and ileum appeared to obey the law of mass-action (Hill coefficient close to 1). The apparent Ki values of pirenzepine were 850 and 250 nM, and those of oxomemazine 1460 and 570 nM in ventricle and ileum, respectively. Thus, oxomemazine like pirenzepine has high affinity for cerebrum, moderate affinity for ileum and low affinity for ventricle. These results suggest that oxomemazine could recognize the muscarinic receptor subtypes with a high affinity for the $M_1$ sites.

• 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.