• 약학회지
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• 제37권6호
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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.

• 생약학회지
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• 제22권3호
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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.

• 생약학회지
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• 제23권4호
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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.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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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)

• 생약학회지
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• 제14권4호
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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.

• Archives of Pharmacal Research
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• 제16권4호
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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.

• 생약학회지
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• 제12권4호
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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.