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최재묵(Jae Mook Choi),이성학(Sung Hak Lee),김일환(Il Hwan Kim),박지은(Jie Eun Park),김덕열(Deog Yeor Kim),노현정(Hyun Jung Noh),김택로(Taekrho Kim),최광도(Do-Gwang Choi),김영훈(Young Hoon Kim),김진완(Jin Wan Kim),장준환(Joon Hwan Jan 한국독성학회 2004 Toxicological Research Vol.20 No.2
Safety pharmacological properties of CJ-11555, an anti-cirrhotic agent, were investigated in experimental animals and in vitro test system. CJ-11555 had no effects on normal body temperature in rats, motor coordination, chemoshock induced by pentetrazol, electric shock induced by electric shocker and writhing syndromes in mice at dose levels of 100, 300 and 1,000 mg/kg. CJ-11555 inhibited intestinal activity and prolonged hexobarbital-induced sleeping time in mice at the dose level of 1,000 mg/kg. CJ-11555 affected on general activity and behaviour tests in SD rats, such as<br/> lacrimation, ptosis, piloerection, decreased body tone, abnormal dispersion within the cage, diarrhoea, red colored faeces, slight hypothermia and decreased grooming, at the dose level of 1,000mg/kg in rats. CJ-11555 was effected on cardiovascular and respiratory system in anesthetized beagle dogs, such as tachycardia, increase of mean blood pressure and decrease of PR interval, decrease of respiratory rate and minute volume, at dose levels of 10 and <br/> 30mg/kg. However, these effects were also observed in vehicle treated anesthetized beagle dogs. In in vitro experiments, CJ-<br/> 11555 inhibited agonists (histamine, acetyl-choline or BaCl2) induced contraction of isolated guinea-pig at the concentration of 30x10-6 M. CJ-11555 was weekly inhibited hERG channel current at concentrations of 10 and 30x10-6 M, and IC50 was estimated to be higher than 30x10-6 M. Based on these results, it was concluded that CJ-11555 affected on cardiovascular and respiratory system, general activity and behaviour and hexobarbital-induced sleeping time at the dose level of 1,000 mg/kg and contraction of the smooth muscle and hERG channel current at the concentration of 30x10-6 M.
최재묵(Jae-Mook Choi),이성학(Sung-Hak Lee),김일환(Il-Hwan Kim),박지은(Jie-Eun Park),김덕열(Deog-Yeor Kim),노현정(Hyun-Jung Noh),김택로(Taekrho Kim),최광도(Do-Gwang Choi),김영훈(Young-Hoon Kim),김진완(Jin-Wan Kim),장준환(Joon-Hwan Jan 한국독성학회 2004 Toxicological Research Vol.20 No.1
Safety pharmacological properties of CJ-11555, an anti-cirrhotic agent, were investigated in experimental animals and in vitro test system. CJ-11555 had no effects on normal body temperature in rats, motor coordination, chemoshock induced by pentetrazol, electric shock induced by electric shocker and writhing syndromes in mice at dose levels of 100, 300 and 1,000 mg/kg. CJ-11555 inhibited intestinal activity and prolonged hexobarbital-induced sleeping time in mice at the dose level of 1,000 mg/kg. CJ-11555 affected on general activity and behaviour tests in SD rats, such as lacrimation, ptosis, piloerection, decreased body tone, abnormal dispersion within the cage, diarrhoea, red colored faeces, slight hypothermia and decreased grooming, at the dose level of 1,000<br/> mg/kg in rats. CJ-11555 was effected on cardiovascular and respiratory system in anesthetized beagle dogs, such as tachycardia, increase of mean blood pressure and decrease of PR interval, decrease of respiratory rate and minute volume, at dose levels of 10 and 30 mg/kg. However, these effects were also observed in vehicle treated anesthetized beagle dogs. In in vitro experiments, CJ-11555 inhibited agonists (histamine, acetyl-choline or BaCl2) induced contraction of isolated guinea-pig at the concentration of 30×10-6 M. CJ-11555 was weekly inhibited hERG channel current at concentrations of 10 and 30×10-6 M, and IC50 was estimated to be higher than 30×10-6 M. Based on these results, it was concluded that CJ-11555 affected on cardiovascular and respiratory system, general activity and behaviour and hexobarbital-induced sleeping time at the dose level of 1,000 mg/kg and contraction of the smooth muscle and hERG channel current at the concentration of 30×10-6 M.
골수염 치료제인 항생제비드 ( CJ-40003 ) 유효성분의 일반약리작용
김영훈(Young Hoon Kim),최재묵(Jae Mook Choi),온윤성(Yoon Seong On),연규정(Kyu Jeong Yeon),이윤하(Youn Ha Lee),김제학(Je Hak Kim),이영수(Young Soo Lee) 한국응용약물학회 1999 Biomolecules & Therapeutics(구 응용약물학회지) Vol.7 No.1
A new antibiotic bead, CJ-40003 is a combination of three antibiotics, tobramycin, vancomycin and cefazolin embedded in bone cement, for the treatment of osteomyelitis. To evaluate the general pharmacological properties of CJ-40003, the effects of its active ingredients were investigated in mice, rats, dogs and isolated guinea pig ileum. The combination of three antibiotics (CA) did not affect general behavior, central nervous system, smooth muscles, gastrointestinal system, cardiovascular and respiratory system and water and electrolytes excretion when administered intravenously at the doses of 0.3, 1 and 3 mg/kg, respectively, into experimental animals. The CA had no effect on the contractile response of the isolated guinea pig ileum to various spasmogen at concentrations of 1, 3 and 10 ㎍/ml, respectively. In conclusion, the active ingredients of CJ-40003 showed no pharmacological effect in these studies.
유전자 재조합 B 형 간염 바이러스 표면 항원 , CJC-50100 의 일반약리작용
정성학(Seong Hak Jeong),최재묵(Jae Mook Choi),이남중(Nam Jung Lee),전형수(Hyung Soo Jeon),김연희(Yon Hee Kim),김재승(Jae Seung Kim),하석훈(Suk Hoon Ha),김영훈(Young Hoon Kim),이나경(Na Gyung Lee),김제학(Je Hak Kim),박완제(Wan Je Park 한국응용약물학회 2001 Biomolecules & Therapeutics(구 응용약물학회지) Vol.9 No.1
N/A CJC-50100 is a recombinant hepatitis B virus surface antigen (HBsAg) expressed in yeast. The general pharmacological properties of CJC-50100 were evaluated in mice, rats, dogs and isolated guinea pig ileum. The doses were 0.33∼33.3 ㎍/㎏ i.m. for mice and rats and 3.3∼9.9 ㎍/㎏ i.v. for dogs. The concentrations of 0.002∼0.02 ㎍/mlwere used for the assay with guinea pig ileum. Intramuscular administration of CJC-50100 at the doses did not alter general behavior and the responses for central nervous system, smooth muscle, gastrointestinal system, cardiovascular and respiratory system, and water and electrolytes excretion. In summary, CJC-50100 had no pharmacological effect in these studies even up to the 100-fold of the expected clinical dose, 20 ㎍/man/60 kg.
김영훈(Young Hoon Kim),최재묵(Jae Mook Choi),홍선표(Sun Pyo Hong),문상범(Sang Bum Moon),김수옥(Soo Ok Kim),이윤하(Younha Lee),이영수(Young Soo Lee) 한국독성학회 1999 Toxicological Research Vol.15 No.2
To develop the second generation Japanese encephalitis (JE) vaccine, an attenuated JE vaccine virus strain SA14-14-2 (PDK) was adapted to Vero cell. The resulting virus SA14-14-2 (Vero) was purified using sucrose density gradient, inactivated with formalin and mixed with alum hydroxide to prepare the test vaccine named CJ-50003. The general pharmacological properties of CJ-50003 were evaluated in mice, rats, dogs and isolated guinea pig ileum. The doses were 0.16~ 16 ㎍/kg i.m. for mice and rats and 0.48-1.6 ㎍/kg i.v. for dogs. The concentration of 0.0016-0.16 mg/ml were used for the assay with guinea pig ileum. lntramuscular administration of CJ-50003 at the doses did not alter general behavior and the responses for central nervous system, smooth muscles, gastrointestinal system, cardiovascular and respiratory system and water and electrolytes excretion. In summary, CJ-50003 had no pharmacological effect in these studies even up to the 100-fold of the expected clinical dose, 5 ㎍/man/30 kg.
섬수 ( Bufonis Venenum ) 추출물의 약리작용
김영춘(Young Hoon Kim),정성학(Seong Hak Jeong),김종호(Jong Ho Kim),최재묵(Jae Mook Choi),지준환(Joon Hwan Ji),강재구(Jae Koo Kang),박종구(Jong Koo Park),김제학(Je Hak Kim),조희재(Hi Jae Cho) 한국응용약물학회 2001 Biomolecules & Therapeutics(구 응용약물학회지) Vol.9 No.1
N/A Bufonis Venenum is a toad venom and its main components are bufadienolides, namely resibufogenin, bufalin and cinobufagin. The desensitizing effect of Bufonis Venenum is useful for the treatment of the premature ejaculation in Chinese medicine. But, minor components of Bufonis Venenum cause problems such as topical burning, pain, and erectile dysfunction. To clarify and eliminate the components responsible for these side effects, we prepared two extracts of Bufonis Venenum with either 70% ethanol or ethylacetate and tested their pharmacological effects. The extract of Bufonis Venenum with 70% ethanol produced pain response in rat hind paw, and exhibited contraction of rabbit corpus cavernosal muscle in vitro. On the other hand, the ethylacetate extract did not cause pain and smooth muscle contraction. The desensitizing effect of the ethylacetate extract was similar to that of the 70% ethanol extract. In conclusion, these results show that the extract of Bufonis Venenum with ethylacetate does not have the components causing side effects and deserve further study for therapeutic potential in premature ejaculation in men.
안지오텐신 2 수용체 길항약 CJ-10513 이 고빈도 심실 pacing 견에서의 혈행동태에 미치는 영향
김영훈(Young Hoon Kim),정성목(Seong Mok Jeong),신재규(Jae Kyu Shin),최재묵(Jae Mook Choi),정성학(Seong Hak Jeong),배훈(Hoon Bae),이건호(Gun Ho Lee),김제학(Je Hak Kim),안양수(Yang Soo An) 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.2
Acute hemodynamic effects of CJ-10513, a non-peptide angiotensin II receptor antagonist, were examined in mongrel dogs treated with high frequency ventricular pacing for one week. Rapid ventricular pacing reduced mean blood pressure (mBP), LVdP/dt and cardiac output (CO), and increased the left ventricular end-diastolic pressure (LVEDP) and pulmonary capillary wedge pressure (PCWP). Continuous infusion of CJ-10513 at doses of 10 and 20 ㎍/kg/min, respectively, for 30 minutes reduced mBP, LVEDP and myocardial oxygen consumption rate (MVO₂) and shifted the cardiac function curve (CO-LVEDP curve) to the left in this dog model. In conclusion, CJ-10513 decreased the preload and afterload and increased the cardiac function in dogs with pacing-induced heart failure.
CJ-11555의 Sprague-Dawely 랫드를 이용한 단회 및 4주 반복경구투여 독성시험
김일환(Il-Hwan Kim),이성학(Sung-Hak Lee),최재묵(Jae-Mook Choi),박지은(Jie-Eun Park),김덕열(Deog-Yeor Kim),노현정(Hyun-Jung Noh),김택로(Taek-Rho Kim),이상호(Sang-Ho Lee),김영훈(Young-Hoon Kim),김진완(Jin-Wan Kim),장준환(Jun-Hwan Chang 한국독성학회 2004 Toxicological Research Vol.20 No.2
This study was to investigate single and repeated-dose toxicities of CJ-11555, an anticirrhotic agent, in Sprague-Dawley (SD) rats. In single-dose oral toxicity study, the test article were<br/> administered once by gavage to males and females at dose levels of 0 and 2,000 mg/kg. No dead animals and abnormal necropsy findings were found in control and CJ-11555 treated group. Therefore, the approximate lethal dose of CJ-11555 was considered to be higher than 2,000 mg/kg in rats. In the 4-week repeated oral toxicity study, the test article was administered once daily by gavage to<br/> male and female rats at dose levels of 0, 10, 50 and 200 mg/kg/day for 4-weeks. In clinical signs, yellow-colored urine and yellow hair coat were observed in the 50 and 200 mg/kg male and female<br/> groups. In hematology, erythrocyte count and hemoglobin were significantly decreased in the 200mg/kg male and female groups. In serum biochemistry, total cholesterol was significantly increased and aspartate aminotransferase (AST) was significantly decreased in the 50 or 200 mg/kg male and female groups. In histopathological examinations, centrilobular hepatocellular hypertrophy in the liver, congestion and pigmentation in the spleen, hyaline droplets in the kidney were observed in the 50 and 200 mg/kg male and female groups. In toxicokinetic study, CJ-11555 was dose-dependent in systemic exposure and showed better absorption in female with minimum accumulation after multidosing. Based on these results, it was concluded that the 4-week repeated oral dose of CJ-11555<br/> resulted in the suppression of AST activity and centrilobular hepatocellular hypertrophy in both sexes at a dose level of 50 or 200 mg/kg/day. The target organ was estimated to be liver, spleen and male's kidney. The no-observed-adverse-effect level (NOAEL) for CJ-11555 in rats following gavage for at least 4-week is 10 mg/kg/day.