• Title/Summary/Keyword: ED50

Search Result 430, Processing Time 0.025 seconds

Synthesis of 8-Alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-ones and Evaluation of their Anticonvulsant Properties

  • Sun, Xian-Yu;Jin, Yun-Zhe;Li, Fu-Nan;Li, Gao;Chai, Kyu-Yun;Quan, Zhe-Shan
    • Archives of Pharmacal Research
    • /
    • v.29 no.12
    • /
    • pp.1080-1085
    • /
    • 2006
  • A series of 8-alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-one derivatives were synthesized using 7-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and the subcutaneous pentylenetetrazole test (sc-PTZ), and their neurotoxicities were measured by the rotarod neurotoxicity test (Tox). The tests demonstrated that 8-hexyloxy-4,5-dihydro-[1.2.4]triazole[4.3-a]quinoline-1-one (4e) and 8-heptyloxy-4,5-dihydro-[1,2,4]triazole[4, 3-a]quinoline-1-one (4f) were the most potent anticonvulsants, with 4e having $ED_{50}$ values of 17.17 mg/kg and 24.55 mg/kg and protective index ($PI=TD_{50}/ED_{50}$) values of 41.9 and 29.3 in the MES and sc-PTZ tests, respectively, and 4f having $ED_{50}$ values of 19.7 mg/kg and 21.2 mg/kg and PI values of 36.5 and 33.9 in the MES and sc-PTZ tests, respectively. The PI values of 4e and 4f were many fold better than that of the marketed drugs phenytoin, carbamazepine, phenobarbital and valproate, which have PI values in the range of 1.6-8.1 in the MES test and <0.22-5.2 in the sc-PTZ test. Structure-activity relationships were also discussed.

A Behavioral Study of Promethazine Interaction with Analgesic Effect of Diclofenac: Pain Combination Therapy

  • Amidi, Niloofar;Izadidastenaei, Zohreh;Araghchian, Malihe;Ahmadimoghaddam, Davoud
    • Journal of Pharmacopuncture
    • /
    • v.23 no.1
    • /
    • pp.18-24
    • /
    • 2020
  • Objectives: Pain is considered as a cause of sickness and the most prevalent symptom which makes people visit a physician. Nowadays, combination therapy is becoming useful to relieve chronic and postsurgical pain. The aim of this study was to study the promethazine (as an antihistamine) interactions with antinociceptive effect of diclofenac (as a non-steroidal anti-inflammatory drugs). Methods: In initial part of the study, we investigate the analgesic effect of diclofenac. Using writhing test, we demonstrate that diclofenac significantly reduces writhe response induced by acetic acid in a dose-dependent manner. In this study, we evaluate the combination effect of promethazine on diclofenac analgesic effect. Results: We observed that diclofenac inhibited pain in the dose dependent manner which means that by increasing dose of diclofenac a significant decrease in pain was observed. This experimental setup allowed calculation of the dose that caused 50% antinociception (ED50) for diclofenac. The ED50 for diclofenac in this study was determined to be 9.1 mg/kg according our previous study. Additionally, promethazine was showed a dose-dependent inhibition of writhes. The combination of different doses of promethazine (2, 4, 6 mg / kg) with diclofenac ED50 (9.1 mg / kg) was injected to mice. Promethazine 4 and 6 mg / kg in combination with diclofenac had significantly led to increase analgesic effect of diclofenac. Conclusion: In conclusion, these results add important information to the existing knowledge on combination of diclofenac and antihistamine in pain therapies to be used in clinical practice and maybe helpful in designing the future guidelines.

Macroprolactinoma in a young man presenting with erectile dysfunction

  • Song, Seung-Hun;Lee, Jinil;Kim, Dong Suk
    • Clinical and Experimental Reproductive Medicine
    • /
    • v.46 no.4
    • /
    • pp.202-205
    • /
    • 2019
  • Hyperprolactinemia due to a pituitary adenoma is a rare cause of erectile dysfunction (ED). The prevalence of clinically apparent prolactinomas is reported to be from 6-10 to 50 per 100,000. A few reports have been published of prolactinoma presenting with ED. Here, we report a rare case of a young man who presented with ED as a chief complaint and who was diagnosed with a huge prolactinoma, and we discuss a related fertility issue.

Application of a Pilot-Scale Electrodialysis System for Groundwater Polluted with Arsenic and Manganese (파일롯 규모 전기투석 막여과 시스템을 이용한 비소와 망간오염 지하수 처리)

  • Choi, Su Young;Kwon, Min Wook;Park, Ki Young;Cha, Ho Young;Kim, Hee Jun;Kweon, Ji Hyang
    • Journal of Korean Society on Water Environment
    • /
    • v.33 no.3
    • /
    • pp.334-340
    • /
    • 2017
  • A pilot-scale electrodialysis system was designed and constructed to treat groundwater polluted with arsenic and manganese. Synthetic groundwater, in which some amount of arsenic and manganese was added to make 500 mg/L of Mn and $50{\mu}g/L$ of As, was used as a feed for the ED system. The limiting current density, linear water velocity, applied voltage, and membrane surface area were investigated to obtain efficient and economic operation of the ED system. The linear water velocity was increased 0.74 cm/s to 11 cm/s based on evaluation of limiting current density. The water quality of diluate for 85 minutes of operation was satisfied with water quality criteria for drinking water using the ED system with 14 pairs of ion exchange membranes. The increased membrane pairs to 21 and 42 pairs were very effective to reduce conductivities of the diluate. The operation cost of the ED system was assessed using specific energy consumption, which was $1.065{\sim}1.2kWh/m^3$. Considering low salt concentrations of the groundwater, improvement of the ED system are required to increase current utilization and to apply low voltage while the ED system was applicable to produce drinking water.

RECENT DEVELOPMENTS OF MEMBRANE TECHNOLOGY IN JAPAN

  • Kimura, Shoji
    • Membrane Journal
    • /
    • v.1 no.1
    • /
    • pp.5-12
    • /
    • 1991
  • Since the discovery of the Loeb-Sourirajan reverse osmosis membrane, thirty years have passed and many membrane technologies and new membranes for applications have been developed in the world. In the early stage of these developments Japan has not contributed much, but from the middle of 70ties Japan has started its own R&D projects starting from the desalination technology, and now various private industries and government ministries are actively engaging in R & D of membrane technologies in Japan. In Table 1 the chronological developments of important events of developments and projects relating membrane technologies inside and outside of Japan are introduced and their details will be explained. The first membrane technology applied in the Japanese industry was a electrodialysis(ED) process using ion-exchange membranes. These membranes were first developed in early 50ties and the Japanese government decided to use this method for concentration of sea-water to produce salt, which was then produced by solar evaporation. This development program started from 1960 by the Japan Monopoly Corp.(at that time). To apply ED process for sea-water concentration it was necessary to develop ion-exchange membranes having very low electric resistance to avoid energy loss due to Joule heat, and those having selectivity to permeate single valent ions only to avoid scale formation in the ED stacks. Three Japanese companies, Asahi Glass, Asahi Chemical and Tokuyama Soda, have succeeded to develop such membranes, and until 1971 all of the seven salt manufacturing companies had adopted ED for production of food salt.

  • PDF

The Awareness and Performance of the Forensic Nursing Role in Emergency Departments (응급실 간호사의 법의간호학적 역할의 인지와 수행정도)

  • Han, Mi-Hyun;Hong, Hae-Sook
    • Journal of Korean Biological Nursing Science
    • /
    • v.14 no.4
    • /
    • pp.291-299
    • /
    • 2012
  • Purpose: This study attempted to measure the awareness and performance of the forensic nursing role among the emergency department (ED) nurses to emphasize the presence of forensic nurses in ED and suggest encouraging essential forensic nursing education. Methods: A quantitative descriptive survey using a questionnaire was carried out to the nurses, who had a minimum of 6 months experience in the ED. This study was conducted at 7 hospitals in the Republic of Korea. Results: A total of 124 nurses were enrolled. As to the Awareness of the forensic nursing role, all the core data obtained an average of 3.39 points out of 4 points, and the documentation category was the highest score of 3.57. For the performance of the forensic nursing role, all the core data obtained an average of 2.50 points out of 4 points, and a documentation category acquired the highest score of 2.91. There is a significant correlation of (r=.452, p<.001) the awareness and performance of the forensic nursing role. Conclusion: Currently, the awareness regarding the forensic nursing role is low level. Therefore, the performance of forensic nursing role has also become low level. Consequently, forensic nursing education is essential for ED nurses to preserve evidence accurately.

Influencing Factors on Forensic Nursing Role Performance of Emergency Department Nurses (응급실 간호사의 법의간호학적 역할 수행에 미치는 영향요인)

  • Kim, Geu-Rin;Sung, Mi Hae
    • Journal of Korean Clinical Nursing Research
    • /
    • v.20 no.1
    • /
    • pp.64-74
    • /
    • 2014
  • Purpose: Purpose of this study was to identify the factors influencing forensic nursing performance role of Emergency Department(ED) nurses. Methods: The study was conducted with 120 ED nurses from Busan. Data were collected during July, 2013 and analyzed using SPSS Win 19.0 program. Results: There were positive correlations between awareness of the forensic nursing role and forensic interest (r=.29, p=.001), between awareness of the forensic nursing role and forensic nursing performance role (r=.54, p<.001), and between forensic experience and forensic nursing performance role (r=.26, p=.004). Awareness of forensic nursing role (${\beta}=.50$, p<.001) and experience in forensics (${\beta}=.24$, p<.001) were significant predictors of forensic nursing role performance and explained 35.9% of the variance. Conclusion: To improve forensic experience, medical institutions should provide education and training for ED nurses to increase their indirect experience. Periodic assessment should also be done. Nurses with training assigned to the ED will enhance the forensic nursing role performance.

Characterization of an antifungal compound isolated from an antagonistic fungus Aspergillus terreus against phytopathogenic fungi (식물병원균 생육을 저해하는 Aspergillus terreus로부터 분리한 향균물질의 특성)

  • Kim, Keun-Ki;Kang, Jae-Gon;Choi, Yong-Lark;Yun, Han-Dae;Ha, Ho-Sung;Kang, Kyu-Young
    • The Korean Journal of Pesticide Science
    • /
    • v.2 no.1
    • /
    • pp.40-45
    • /
    • 1998
  • An antagonistic fungus inhibiting growth of various phytopathogenic fungi was isolated from greenhouse soils and identified. Mophological features of fruiting structures on potato dextrose agar and colorless globose to ovate heavy walled hyaline cells from the vegetative mycelium grown on MY20 agar indicate that this antagonist is Aspergillus terreus. The antagonistic activity is due to the production of antifungal compounds. An antifungal compound was purified from its culture filtrate using chloroform extraction, column chromatography, and thin layer chromatography. The purified antibiotic was effective to various phytopathogenic fungi and identified as butyrolactone I. $ED_{50}$ values measured by petri-plate assay through effective dosage(ED)-probit analysis were 9.7, 13.7, 23.3, 42.6 and 102.7 ppm on Botrytis cinerea, Rhizoctonia solani, Pythium ultimum, Phytophthora capsici, and Fusarium oxysporum, respectively.

  • PDF

Identification of Active Component Isolated from Croton tiglium and Coptis japonica Aqueous Mixture$(CP_2)$ and Studies of Its Cytotoxic Effect (파두와 황련의 수용성 혼합물$(CP_2)$부터 분리된 항암성분의 구조확인 및 세포독성에 대한 연구)

  • Kim, Jung-Han;Lee, Sang-Jun;Han, Young-Bok;Kim, Jong-Bae
    • YAKHAK HOEJI
    • /
    • v.38 no.1
    • /
    • pp.31-37
    • /
    • 1994
  • Active fraction, $P_2$, was Isolated from natural anti-cancer drug, $CP_2$, by HPLC. We confirmed that $P_2$ includes most of the Isoguanosine and minor components, Berberine and other protoberberine alkaloids, by $^1H-NMR$ and $^{13}C-NMR$ and measured tile cytotoxicity of $P_2$ against various tumor cell-lines.' $P_2$ was very effective to all tumor cell-lines, especially to human colon cancer SNU-C2A$(ED_{50};\;24{\mu}g)$ and liver cancer HEP-3B$(ED_{50};\;27{\mu}g)$.

  • PDF

L1210 및 K562 세포에 대한 노루발의 세포독성 성분

  • 배기환;이상명
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1994.04a
    • /
    • pp.246-246
    • /
    • 1994
  • 연구목적: 생약으로 부터 항암제 개발연구의 일환으로 민간에서 조경. 지혈 등에 사용되고있는 노루발(Pyrola japonica)의 세포독성 물질과 그의 화학적구조를 규명하기 위해서 본 연구를 실시하였다. 실험 방법 : 옴건한 노루발의 지하부를 methanol로 환류 추출하여 얻은 methanol extract를 n-hexane, ethylacetate, n-butanol 순으로 분획하였다. 그 후 각각의 분획을 L1210 세포에 대하여 in vitro에서 실험한 결과 n-heane, ethylacetate 분획에서 강한 활성이 나타남을 알 수 있었다. 따라서 n-hexane, ethylacetate 분획을 반복하여 silica gel column chromatography 하여 1종의 활성물질과 4종의 비활성물질을 단리하였다. 실험결과 : 단리된 활성물질은 각종 spectral data를 검토하여 chimaphilin (L1210의 ED$_{50}$ : 0.6 $\mu\textrm{g}$/ml, K562의 ED$_{50}$ :< 0.6 $\mu\textrm{g}$/ml) 임을 확인하였고 이 물질은 5,8-dihydro-2.7-dimethyl-4-naphtoquione의 변성물질 임을 알 수 있었다.있었다.

  • PDF