大鼠耳蜗中的胆碱能毒蕈碱受体。
Cholinergic muscarinic receptors in rat cochlea.
作者信息
van Megen Y J, Klaassen A B, Rodrigues de Miranda J F, Kuijpers W
机构信息
Department of Otorhinolaryngology, University of Nijmegen, The Netherlands.
出版信息
Brain Res. 1988 Nov 22;474(1):185-8. doi: 10.1016/0006-8993(88)90682-8.
Specific 3H-1-quinuclidinylbenzilate (3H-1-QNB) binding to rat cochlea homogenates occurs to a homogeneous class of binding sites with Kd = 0.13 +/- 0.01 nM and Bmax = 0.57 +/- 0.07 fmol per cochlea. Binding is stereoselectively inhibited by benzetimide enantiomers. Dexetimide was more effective than levetimide in displacing 3H-1-QNB from its binding sites (Ki = 4 x 10(-10) M and 6.5 x 10(-6) M, respectively). Pirenzepine inhibits 3H-1-QNB binding with low affinity (Ki = 2 x 10(-6) M), classifying the binding sites as muscarinic M2 receptors.
特异性3H-1-喹核醇基苯甲酸酯（3H-1-QNB）与大鼠耳蜗匀浆的结合发生在一类同质的结合位点上，解离常数（Kd）为0.13±0.01 nM，每只耳蜗的最大结合量（Bmax）为0.57±0.07 fmol。苯甲酰亚胺对映体可立体选择性地抑制该结合。右苯甲酰亚胺在将3H-1-QNB从其结合位点上置换下来方面比左苯甲酰亚胺更有效（解离常数分别为4×10⁻¹⁰ M和6.5×10⁻⁶ M）。哌仑西平以低亲和力抑制3H-1-QNB结合（解离常数为2×10⁻⁶ M），将这些结合位点归类为毒蕈碱M2受体。
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