Relationship between Hypoglycemic Activity and Binding Ability with Bovine Serum Albumin of Sulfonylurea Related Compounds

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  • スルホニル尿素系化合物の血糖降下作用と牛血清アルブミン結合性との関係
  • スルホニル ニョウソケイ カゴウブツ ノ ケットウ コウカ サヨウ ト ウシ

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Description

The hypoglycemic activity of 20 sulfonylurea related compounds (SU) was examined after oral administration by the use of rat. Two calculated values, (1) decreasing percentage of blood sugar concentration at 2 hours compared with that at 0 time and (2) area of the blood sugar concentration curve from 0 to 7 hours (S-value) were used to evaluate the hypoglycemic effect of SU. The relationship between the primary binding constant for bovine serum albumin-SU (K1) related to the hydrophobicity of SU molecule and the S value was investigated. No linear relationship was obtained and a parabola type relationship could be applied between log K1 and log S. It was concluded that the hypoglycemic activity of SU was influenced considerably by its binding ability to bovine serum albumin and an appropriate binding constant (K1) of SU may be required to obtain most efficient activity.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 101 (10), 926-931, 1981

    The Pharmaceutical Society of Japan

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