YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
塩酸ジラゼプの血球、血小板に対する結合性の動物種差
小島 順司吉村 三夫
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1995 年 115 巻 10 号 p. 823-831

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The whole blood of human, rabbit and dog spiked with dilazep was fractionated by discontinuous density gradients of Ficoll-Paque, and the species difference of distribution to blood components was elucidated. In order to quantatively evaluate its blood distribution, the binding property of dilazep to the isolated erythrocytes and platelets was also studied. Dilazep undergoes saturable binding to the erythrocytes. Therefore, the fitting of the data sets to binding models was carried out using the nonlinear least-square method, and binding parameters were calculated. This technique could be also applied to analyze directly the binding parameters for several whole blood components. In human and rabbit, dilazep was bound to the erythrocytes with a high affinity (human, KERY=0.466nM ; rabbit, KERY=0.0417nM), however, the affinity to the erythrocytes in dog was very low. On the other hand, the binding affinity to the platelets decreased in the order of rabbit>dog>human.

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© by the PHARMACEUTICAL SOCIETY OF JAPAN
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