• 제목/요약/키워드: analgesic activity

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KI-60606의 일반약리작용시험 (General Pharmacology of KI-60606)

  • 김은주;김현진;김동연
    • Biomolecules & Therapeutics
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    • 제10권2호
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    • pp.89-98
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    • 2002
  • In this study general pharmacological profiles of KI-60606 on the central nervous system, the cardiovascular system and the other organs were investigated. The dosages given were 0,5, 10 and 25 mg/kg and drugs were administered intravenously. The animals used for this study were mice, rats, cats and guinea pigs. KI-60606 showed no effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital-induced hypnosis time, body temperature, analgesic activity, anticonvulsant activity and contraction of nictitating membrane in cats. Furthermore KI-60606 showed no effects on blood pressure, heart rate, LVP (left ventricular peak systolic pressure), LVEDP (left ventricular end diastolic pressure), LVDP (left ventricular developing pressure), DP(double product), CFR(coronary flow rate), smooth muscle contraction using guinea pig ileum and gastric secretion at all dosage tested except the increase of gastrointestinal transport and urinary $K^+$ excretion.

고상법에 의한 Dermorphin 유사체의 합성과 생물학적 활성에 관한 연구 (Synthesis of Dermorphin Analogues by the Solid Phase Method and Biological Activity)

  • 한만소
    • 한국응용과학기술학회지
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    • 제19권4호
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    • pp.281-290
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    • 2002
  • Dermorphin is a hepta peptide(H-Tyr-DAla-Phe-Gly-Tyr-Pro-Ser-$NH_{2}$)with exceptionally potent and long-lasting peripheral and central activity. Dermorphin analogues, dermorphionyl(DMP)-Lys-$NH_{2}$ and DMP-Lys-Lys-$NH_{2}$ have been prepared in order to examine the effect of opiod activity. Dermorphin analogues were synthesized by the solid phase method. The crude peptide was purified by gel filter on a Sephadex LH-20, characterized with HPLC and amino acid analyzer. Analgesic potency was estimated by writhing syndrome method and Randall-Selitto method. As a result, dermorphin analogues have lower potency than that of morphine.

General Pharmacology of PEG-Hemoglobin SB1

  • Kim, Eun-Joo;Lee, Rae-Kyong;Bak, Ji-Yeong;Choi, Gyu-Kap
    • Biomolecules & Therapeutics
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    • 제7권2호
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    • pp.170-177
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    • 1999
  • PEG-hemoglobin SB1 (SB1), which is a hemoglobin-based oxygen carrier, is intended to use as a safe blood substitute against brain ischemia and stroke. The general pharmacological profiles of SB1 were studied. The doses given were 0, 5, 10, 20 ml/kg and drugs were administered intravenously. The animals used for this study were mouse, rat and guinea pig. SB1 showed no effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital sleeping time, anticonvulsant activity, analgesic activity, blood pressure and heart rate, left ventricular peak systolic pressure, left ventricular end diastolic pressure, left ventricular developing pressure, double product, heart rate, coronary flow rate, smooth muscle contraction using guinea pig ileum, gastrointestinal transport, gastric secretion, urinary volume and electrolyte excretion at all doses tested except the decrease of body temperature. These findings demonstrated that SB1 possesses no general pharmacological effects at all doses tested.

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애엽 추출물의 항위궤양에 대한 기전 (A Mechanism of Gastric Antiulceration by the Extract of Artemisiae asiatica)

  • 황귀서;이정석;윤여표
    • 대한예방한의학회지
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    • 제1권1호
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    • pp.118-125
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    • 1997
  • In oriental medicine, Artemisiae asiatica (AA) has been used as analgesic, antiinflammatory agent, and coagulatory agent. Furthermore, eupatilin, a kind of flavonoids, is known as the active principle component of AA. This study was undertaken to determine the gastric antiulceration of AA and to elucidate its mechanism. AA showed the inhibitory effect on gastric ulceration induced by EtOH/HCl and aspirin. To elucidate its mechanism, the effect of AA on lipidperoxide level in gastric mucosa, microsome lipidperoxidation, iron -dependent lipidperoxidation, and neutrophil activation were examined. It is suggested that the antiperoxidative and antineutrophil activity of AA play important roles as a possible mechanism. These results suggest that AA might have gastric antiulceration activity due to antilipidperoxdative and antineutrophil activity.

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Antioxident components from Aralia continentalis

  • Kim, Ju-Sun;Kang, Sam-Sik;Park, Jae-Sue
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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    • pp.182-182
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    • 1998
  • The root of Aralia continentalis Kitagawa(Araliaceae) have been used as an analgesic and fever remedy, and for treatment of rheumatism in Chinese medicine, whereas the young leaves are used for salad. An antioxidant activity of the young leaves of A continentalis was determined by measuring lipid peroxide produced when a mouse liver homogenate was exposed to the air at 37$^{\circ}C$, using 2-thiobarbituric acid(TBA) and by evaluation the radical scavenging activity on 1,l-diphenyl-2 picrylhydrazyl (DPPH) radical. Bioassay guided fractionation of MeOH extract isolated six flavonoid compounds as active components from EtOAc fraction. Adenosine and two saponins were isolated from the weak active BuOH fraction. The antioxidant effect by DPPH radical scavenging activity showed that quercetin was the most active among these compounds. Hyperoside and kaempferol were also active, while 6"-O-acetyl astragalin, astragalin, trifolin, adenosine, oleanolic acid 28-O-glucosyl ester and salsoloside C methyl ester were almost inactive. All the compounds were identified by spectroscopic methods.

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Ginkgetin, a plant biflavone from Ginkgo biloba leaves, inhibits release of cytokines from human PMMC

  • Kim, Hee-Kee;Son, Kun-Ho;Chang, Hyeun-Wook;Kang, Sam-Sik;Kim, Hyun-Pyo
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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    • pp.195-195
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    • 1998
  • Ginkgetin was previously reported as an inhibitor of group II phospholipase A$_2$. It also inhibited in vitro arachidonate release from the activated macrophages and lymphocyte proliferation. These previous studies suggested an anti-inflammatory nature of ginkgetin, especially on chronic inflammation. In fact, ginkgetin showed potent anti-inflammatory activity against rat adjuvant-induced arthritis, a chronic inflammatory animal model, with comparable analgesic activity. In order to investigate the action mechanisms, tumor necrosis factor and interferone release were studied from human PMMC. It was found that ginkgetin clearly inhibited release of these cytoknes from human PMMC. Ginkgetin was also found to inhibit immunoglobulin M production at 1 - 10 uM. These results may contribute to antiarthritic activity of ginkgetin in vivo.

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Anti-inflammatory Activity of Propolis

  • Park, Eun-Hee;Kim, Sun-Hee;Park, Soo-Sun
    • Archives of Pharmacal Research
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    • 제19권5호
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    • pp.337-341
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    • 1996
  • Propolid (bee-glue), known as a folk medicine, is a lipo;hilic material found in honeybee hives. In the present study on the anti-inflammatory effect of Korean propolis, it was extracted with ethanol, and used as a test material. The $LD_{50}$ value with the oral administration of ethanolic extract of Korean propolis (EEKP) was higher than 2g/kg in mice. The oral administration of the propolis extract (100mg/kg) significantly inhibited the development of hind paw edema induced by carrageenin in rats. the oral pretreatment of the propolis extract markedly inhibited the increase in vascular permeability and the number of writhing induced by acetic acetic acid in mice. Propolis extract, 50 and 100 mg/kg p.o. per day for 7 days, produced a significant inhibitory effect on granuloma and exudate formation in rats. This inhibitory effect was enhanced with the concomitant use of prednisolone (2.5 mg/kg). These results suggest that Korean propolis apparently has a strong anti-inflammatory activity.

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Anti-diabetic Agents from Medicinal Plants Inhibitory Activity of Schizonepeta tenuifolia Spikes on the Diabetogenesis by Streptozotocin in Mice

  • Kim, Chang-Jong;Lim, Jung-Sik;Cho, Seung-Kil
    • Archives of Pharmacal Research
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    • 제19권6호
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    • pp.441-446
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    • 1996
  • The Schizonepeta tenuifolia spikes (STS) have been used as a traditional folk medicine for antiinflammatory, analgesic, anti-pyretic and anti-spasmodic purpose in Korea. Phytosterols (mixture of campesterol 3.68%, stigmasterol 2.30% and ${\beta}$-sitosterol 94.02%) and hesperidin were isolated by chromatography from ether and n-BuOH fractions of STS respectively. These compounds significantly reduced the blood glucose level and lessened the loss of body weight and water consumption dose-dependently when administered at a i.p. doses of 10 and 20 mg/kg for 4 days after the i.v. injection of streptozotocin (I 80 mg/kg). In the morphologic study, these compounds showed protective activity on the pancreatic islets, especially .betha.-cells, from the degenerative changes by streptozotocin.

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AS6의 일반약리작용시험 (General Pharmacology of AS6)

  • 김현진;최규갑;도선희;김은주;차경회
    • Biomolecules & Therapeutics
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    • 제10권4호
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    • pp.258-267
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    • 2002
  • In this study the general pharmacological profiles of AS6 on the central nervous system, cardiovascular and the other organs were investigated. The dosages given were 0, 250, 500 and 1000 mg/kg and drugs were orally administered. The animals used for this study were mice, rats and guinea pigs. Significant increases (p<0.01) in the charcoal transport capacity were observed at the high dose of 1000 mg/kg and significant increases in retardation of pain threshold were observed in the test using acetic acid in all dosed animals. However, AS6 showed no noticeable effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital-induced sleep time, body temperature, analgesic activity in the test using hot plate method and anticonvulsant activity. Furthermore no noticeable effects were observed in cardiovascular functions in the isolated rat heart, contraction and relaxation of the smooth muscle in the isolated guinea ileum, gastric secretion and renal function.

Cinnarizine을 Propranolol이나 Metoprolol과 병용할 때의 행동약리학적 연구 (Pharmacological Studies on the Behavioral Effects of Cinnarizine Coadministered with Propranolol or Metoprolol)

  • 허인회;안형수
    • 약학회지
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    • 제29권1호
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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.

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