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Pharmacolgocial Characterization of LB50016, N-(4-Amino)Butyl 3-Phenylpyrrolidine Derivative, as a New 5-HT_{1A}Receptor Agonist

  • Lee, Chang-Ho;Oh, Jeong-In;Park, Hee-Dong;Kim, Hee-Jin;Park, Tae-Kyo;Kim, Jae-Soon;Hong, Chang-Yong;Lee, Seok-Jong;Ahn, Kyo-Han;Kim, Yong-Zu
    • Archives of Pharmacal Research
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    • v.22 no.2
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    • pp.157-164
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    • 1999

  • LB50016 was characterized as a selective and potent$ 5-HT_{1A}$ receptor agonist and evaluate it anxiolytic and antidepressant activities. It shows high affinity for $ 5-HT_{1A}$receptor, moderate affinity for $\alpha$2 adrenergic and $ 5-HT_{2A}$receptors and no significant affinity for other receptors tested. Hypothermia and increased serum corticosterone level were observed in LB50016-treated rats, which are mediated mostly by post synaptic $ 5-HT_{1A}$ receptor activation. In the mouse forced swim model for depression, LB50016-elicited dose-dependent reductions in immobility time, showing $ED_{50}$ of approximately 3 mg/kg i.p., which was blocked by pretreatment of NAN-190, $ 5-HT_{1A}$antagonist. In face-to-face test for anxiolytic activity in mice, estimated $ED_{50}$ was 2 mg/kg, i.p.. In isolation-induced aggression test with mice, fifty-fold increases in latency to attack were observed at 30 min and last up to 4 h after LB50016 treatment (3 mg/kg, i.p.). Taken together, LB50016-induced pharmacological activities are mediated by activation of $ 5-HT_{1A}$receptors, offering an effective therapeutic candidate in the management of anxiety and depression in humans.

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In vivo Efficacy of LB20304a against Experimental Respiratory Tract Infection in Mice (생쥐의 호흡기 감염에 대한 퀴놀론계 항생제 LB20304a의 치료 효과)

  • An, Mi-Jeong;Kim, Mu-Yong;Baek, Gyeong-Suk;Kim, In-Cheol;Gwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.40 no.4
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    • pp.438-441
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    • 1996

  • The therapeutic activity of LB20304a was examined on experimental respiratory tract infection (RTI) caused by Klebsiella pneumoniae DT-S in mice. A single oral dose of LB 20304a (1.2mg/mouse) showed a rapid bacteriocidal activity in lung tissue at 4,7 and 24h after administration of drug. The in vivo activity of LB20304a was comparable to that of ciprofloxacin against K. pneumoniae infection, although in vitro MIC of LB20304a was four-fold higher than that of ciprofloxacin.

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Effect of a New Fluoroquinolone LB20304a on Microflora of Caecum in Mice (새로운 플루오로퀴놀론계 항생제 LB20304a가 생쥐의 맹장내 세균총에 미치는 영향)

  • Ahn, Mi-Jeong;Paek, Kyoung-Sook;Kim, Mu-Yong;Kim, In-Chull;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.40 no.3
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    • pp.343-346
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    • 1996

  • The influence of LB20304a, a new fluoroquinolone antibiotic agent, on microflora of caecum in mice was compared with those of ciprofloxacin and piperacillin after administration of drugs for 5 days. Selective medium (CCFMA) was used for the isolation of Clostridium difficile from the specimens of mouse caecum. The emergence of C. difficile in mouse caecum induced by LB20304a was lower than that by ciprofloxacin or piperacillin at day 1 and day 7 after completing administration of drugs.

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Skin Permeation Characteristics of Estradiol Patches and Their Comparative Efficacy Test in Ovariectomized Rabbits (에스트라디올 패취의 피부투과 특성 및 난소제거 토끼에서의 비교 효력시험)

  • Ryoo, Je-Phil;Choi, Mi-Suk;Choi, Jong-Kun;Kim, Soo-Hyeon;Kim, Eung-Goo;Yoon, Byung-Il
    • Journal of Pharmaceutical Investigation
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    • v.25 no.1
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    • pp.47-54
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    • 1995

  • Transdermal patch formulations of estradiol to treat post-menopausal symptoms and prevent osteoporosis in women were developed and evaluated for the permeation characteristics through the excised hairless mouse abdorminal skin and the uterotropic effect on the ovariectomized rabbits. The design of patch formulations was optimized by varying several formulation parameters, such as type of enhancers, amount of enhancers, amount of drug loading and coating thickness. Compared to a commercially available transdermal product, several patch formulations showed the similar skin permeation profiles (following zero-order kinetics), but their skin permeation rates were lasted for the longer period (a week). In one-week uterotropic efficacy test in the ovariectimized rabbits, the selected patch formulations showed the positive effect in atrophy of the urogenital epithelium. The mean values of uterus weight in rabbits after application of patches containing estradiol were much higher than those in control group (containing no drug).

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