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为研究甲基汞对大鼠脑α1-肾上腺素受体的影响以及拮抗剂对甲基汞引起该受体特异结合抑制的恢复效果,本文应用放射性配体结合技术进行了体内外试验研究。结果显示:氯化甲基汞能明显抑制大鼠脑α1-肾上腺素受体与[3H]prazosin的特异结合,IC50为2.89μmol/L。二巯基丙磺酸钠、二巯基丁二酸钠,半胱氨酸能使被氯化甲基汞抑制的[3H]prozosin结合得到不同程度的恢复。表明甲基汞与巯基基团的结合是脑α1-肾上腺素受体受其抑制的分子机制。而含巯基的化合物能把与受体上巯基基团结合的甲基汞竞争下来,从而恢复α1-肾上腺素受体与配体的结合能力。
In order to study the effect of methylmercury on α1-adrenergic receptor in rat brain and the effect of antagonist on methylmercury-induced inhibition of specific binding of this receptor, radioligand binding technique was used to study in vitro and in vivo. The results showed that methylmercury chloride could significantly inhibit the specific binding of α1-adrenoceptor to [3H] prazosin in rat brain with IC50 of 2.89μmol / L. Sodium dimercaptopropane sulfonate, sodium dimercaptosuccinate, and cysteine could restore [3H] prozosin inhibited by methylmercury chloride to some extent. This suggests that the binding of methylmercury to sulfhydryl groups is a molecular mechanism by which the [alpha] 1-adrenoceptor is inhibited. While thiol-containing compounds compete with methylmercury bound to the sulfhydryl group on the receptor, thereby restoring the binding capacity of the α1-adrenoceptor to the ligand.