• Title/Summary/Keyword: bradykinin antagonistic

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Bradykinin Antagonistic Activities of Antihistamine Agents Containing Piperazine Moiety (피페라진계 항히스타민제들의 브라디키닌 길항작용)

  • 정성현;이소영;윤혜숙
    • YAKHAK HOEJI
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    • v.37 no.6
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    • pp.625-630
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    • 1993
  • Among the six antihistamine agents tested in this study, homochlorcyclizine showed the highest bradykinin antagonistic activity in the receptor binding assay as well as the isolated rat ileum assay. Schild plot analysis of bradykinin-induced ileal contraction in the presence of three different concentrations of homochlorcyclizine revealed a pA$_{2}$=6.26, and a correlation coefficient of 0.984. Homochlorcyclizine of (100 $\mu{M}$ final concentration) also showed 25% antagonistic activity in the receptor binding assay.

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Bradykinin Antagonistic Activities of Scutellariae Radix (황금의 Bradykinin 길항작용)

  • Chung, Sung-Hyun;Choi, Jin-Jae;Yoo, Kyung-Sook;Yun-Choi, Hye-Sook
    • Korean Journal of Pharmacognosy
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    • v.22 no.3
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    • pp.192-196
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    • 1991
  • Ether-soluble flavonoid and neutral fraction (Fr. C) prepared from EtOAc extract of Scutellariae Radix showed inhibitory activities against bradykinin (BK) ; inhibited BK-induced ileum or uterus contractions, antagonized BK-induced plasma extravasation and protected mice from endotoxic shock, reduced acetic acid-induced writhing in mice.

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Flavonoids with Bradykinin Antagonistic Effects from Scutellariae Radix

  • YunChoi, Hye-Sook;Yoo, Kyung-Sook;Chung, Sung-Hyun;Yang, Hyun-Sook;Choi, Jin-Jae;Kim, Young-Joo
    • Korean Journal of Pharmacognosy
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    • v.23 no.4
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    • pp.234-239
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    • 1992
  • Seven flavonoid components were isolated from fr. C of Scutellariae radix which showed antagonistic effects against bradykinin(BK). The results indicated that two oxygen functions (either -OH or $-OCH_3$) at 2'- and 6'-positions and/or an oxygen function at 6-position of flavone seemed to be favored for the BK inhibitory activities. Skullcapflavone-II(IV) which contains $6-OCH_3$, 2'-OH and $6-OCH_3$ in the structure was the most active among the flavones tested.

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Developing a pharmacophore model for nonpeptide bradykinin antagonists

  • Park, Hae-Young;Choi, Su-Young;Lee, Su-Jin;Koh, Hune-Yeong;Pae, Ae-Nim
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.176.1-176.1
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    • 2003
  • Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics. To understand the structural basis for the bradykinin antagonistic activity and to guide the design of more potent compounds we analysed the three dimensional pharmacophore model. Seven active compounds very recently reported such as FR 167344, FR 173657, LF 160687, and bradyzide were used as our pharmacophore model analysis. (omitted)

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Screening of Plant Materials for the Antagonistic Effects against Angiotensin or Bradykinin (Angiotensin 또는 Bradykinin 길항작용 식물의 검색)

  • Yun, Hye-Sook;Kim, Young-Sook;Kim, Sun-Ok;Chung, Sung-Hyun
    • Korean Journal of Pharmacognosy
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    • v.14 no.4
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    • pp.145-148
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    • 1983
  • Angiotensins and bradykinin play important roles in blood pressure regulation and in other physiological and pathological conditions. The present work is aimed to investigate potential antagonists against either angiotensin or bradykinin from plant sources. Each methanol extract of selected 25 plants was solvent fractionated to three fractions. The effects of total of 75 plant samples against the contractions induced by angiotensin I or bradykinin in rat ileum were measured. The results are summarized.

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Evaluation of Some Flavonoids as Potential Bradykinin Antagonists

  • Choi, Hye-Sook;Chung, Sung-Hyun;Kim, Young-Joo
    • Archives of Pharmacal Research
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    • v.16 no.4
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    • pp.283-288
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    • 1993
  • Fourteen flavonoids were evaluated for their effects as potential bradykinin (BK) antagonists. The compounds were evaluatd in several in vitro and in vivo (oral administration) systems ; inhibition of BK induced contractions in isolated rat ileum and uterus, antagonistic effects of BK induced plasma extravasation, reduction of acetic acid induced withing nociception and protection from endotoxic shock. Skullcapflavone II (3), baicalein (5), 5-methoxyflavone (11), 6-methoxyflavone (12) and 2'-methoxyflavone (14) showed effects in all the tests although the order of potency were somewhat varied.

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Effect of Alisols Isolated from Alisma orientale Jazep. Against Several Agonists in Isolated Rat Ileum (택사의 Alisol성분들이 몇가지 Agonist에 의한 적출장관 수축에 미치는 영향)

  • YunChoi, Hye-Sook;Chung, Sung-Hyun;Kim, Young-Sook
    • Korean Journal of Pharmacognosy
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    • v.12 no.4
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    • pp.200-202
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    • 1981
  • Alisol B(II) and alisol B monoacetate (III) isolated from the rhizome of Alisma orientale Jazepczuk (Alismataceae) showed antagonistic effects against the contractions induced by angiotensin and bradykinin in rat ileum. However, they seem to be nonspecific antagonism.

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