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[3H]-Quinuclidinyl benzilate binding to muscarinic receptors in rat brain: comparison of results from intact brain slices and homogenates.

机译:[3H]-奎宁环烷基苯磺酸盐与大鼠脑中毒蕈碱受体的结合:完整脑切片和匀浆物的结果比较。

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摘要

1. The binding of [3H]-( +/- )-quinuclidinyl benzilate ([3H]-( +/- )-QNB) to muscarinic sites in rat brain slice and homogenate preparations was compared. 2. Evidence is presented in support of the view that only the (-)-enantiomer of QNB binds with high affinity to muscarinic sites. 3. The Kd value for [3H]-(-)-QNB binding in slices was eight times higher than that measured in homogenates. 4. Similarly, the potencies of various muscarinic ligands as inhibitors of [3H]-(-)-QNB binding were consistently lower in slices than in homogenates. 5. It is proposed that the results may reflect differences in the binding properties of muscarinic receptors in intact tissue slice and homogenate preparations.
机译:1.比较了[3H]-(+/-)-苯并喹啉基苄基酸盐([3H]-(+/-)-QNB)与大鼠脑切片和匀浆制剂中毒蕈碱的结合。 2.提供证据支持仅QNB的(-)-对映体与毒蕈碱位点结合的观点。 3.切片中[3H]-(-)-QNB结合的Kd值比匀浆中的Kd值高八倍。 4.同样,各种毒蕈碱配体作为[3H]-(-)-QNB结合抑制剂的效力在切片中始终低于匀浆。 5.建议结果可能反映完整组织切片和匀浆制剂中毒蕈碱受体结合特性的差异。

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