Ethanol → Thromboxane

HRID 1708154

반응식

HRID 1708154 반응식
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C@H:6](O)/[CH:7]=[CH:8]/[C@@H:9]1[C@H:13]2[CH2:14]/[C:15](/O[C@H:12]2[CH2:11][C@H:10]1[OH:24])=[CH:16]/[CH2:17][CH2:18][CH2:19][C:20](O)=O.C(O)C.C(O)(=O)CCC/C=C\C/C=C\C/C=C\C/C=C\CCCCC.CCCCC[C@H](O)/C=C/[C@H]1OC(O)C[C@H](O)[C@@H]1C/C=C\CCCC(O)=O>C(Cl)(Cl)Cl.CS(C)=O>[CH3:20][CH2:19][CH2:18][CH2:17][CH2:16][CH2:15][CH2:14][C@@H:13]1[C@@H:9]([CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[O:24][CH2:10][CH2:11][CH2:12]1

참가 물질

7

반응물 4

HCID 702EthanolHCID 444899Arachidonic Acid2회HCID 5282411ProstacyclinHCID 5283137Thromboxane B2

생성물 1

HCID 114873Thromboxane

시약·촉매·용매 2

HCID 679Dimethyl Sulfoxide용매HCID 6212Chloroform용매

실험 절차

After addition of prostacyclin, human thrombocytes were isolated from platelet-rich plasma and suspended in Tyrode-Hepes buffer of pH 7.4 at 2×108 cells/ml. One ml aliquots of cells were incubated either with a compound according to the invention (0.1 to 100 μM) or a solvent (ethanol and/or dimethyl sulfoxide) at 37° C. for 3 minutes and thereafter with radioactively labelled arachidonic acid (3.5 μM) for 5 minutes. The reaction was stopped and the metabolites of arachidonic acid were extracted by adding methanol, chloroform and formic acid. After evaporation of the chloroform-containing layer to dryness under nitrogen, the residue obtained was resuspended in 50 μl chloroform and analyzed by thin layer chromatography. The distribution of the radioactivity of the different metabolites of arachidonic acid was measured using a TLC linear analyzer. By correlating the percentages of the amount of TXB2 formed under the action of thromboxane synthase in the presence of solvent and in the presence of different concentrations of compounds according to the invention, the following IC50 -values were determined graphically from semilogarithmic diagrams.

후처리

  1. customhuman thrombocytes were isolated from platelet-rich plasma
  2. extractionthe metabolites of arachidonic acid were extracted
  3. additionby adding methanol, chloroform and formic acid
  4. customAfter evaporation of the chloroform-
  5. additioncontaining layer to dryness under nitrogen
  6. customthe residue obtained

출처 및 근거

ORD 기록
ord-de49f389d979418f93b0bb672a26f757
출처 데이터셋
uspto-grants-1994_10
특허 번호
US05356921

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