家蝇头部和大鼠脑中的二苯羟乙酸奎宁环酯结合
Quinuclidinyl benzilate binding in house fly heads and rat brain.
作者信息
Jones S W, Sumikawa K
出版信息
J Neurochem. 1981 Feb;36(2):454-9. doi: 10.1111/j.1471-4159.1981.tb01614.x.
House fly heads contain a binding site for 3-quinuclidinyl benzilate (QNB) that is quite similar in pharmacology to the muscarinic acetylcholine receptor of vertebrate tissues. The house fly site binds [3H]QNB reversibly with a Kd of 260 pM and Bmax of 1 pmol/g of heads from direct binding measurements. The Kd calculated from the ratio of the dissociation rate constant (2 x 10(-4)sec-1) to the association rate constant (2.5 x 10(6) M-1sec-1) was 80 pM. The house fly site binds (-)quinuclidinyl benzilate preferentially, as do classic muscarinic receptors. The binding is also sensitive to other muscarinic antagonists and agonists. Nicotinic and other drugs are no more effective on the house fly site than they are on the rat brain muscarinic receptor itself. These binding studies suggest that the house fly QNB binding site is a muscarinic receptor.
家蝇头部含有一个与3-喹核醇基苯甲酸酯（QNB）的结合位点，其药理学性质与脊椎动物组织中的毒蕈碱型乙酰胆碱受体非常相似。通过直接结合测量，家蝇的该位点与[3H]QNB可逆性结合，解离常数（Kd）为260皮摩尔，每克头部的最大结合量（Bmax）为1皮摩尔。根据解离速率常数（2×10^(-4)秒^(-1)）与结合速率常数（2.5×10^(6) M^(-1)秒^(-1)）的比值计算出的Kd为80皮摩尔。与经典的毒蕈碱型受体一样，家蝇的该位点优先结合（-）喹核醇基苯甲酸酯。该结合对其他毒蕈碱型拮抗剂和激动剂也敏感。烟碱类和其他药物对家蝇的该位点并不比对大鼠脑毒蕈碱型受体本身更有效。这些结合研究表明，家蝇的QNB结合位点是一种毒蕈碱型受体。
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