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[3H]-东莨菪碱与大鼠脑内毒蕈碱受体的结合:完整脑片与匀浆结果的比较

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

作者信息

Gilbert R F, Hanley M R, Iversen L L

出版信息

Br J Pharmacol. 1979 Mar;65(3):451-6. doi: 10.1111/j.1476-5381.1979.tb07850.x.

Abstract
  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.
摘要
  1. 比较了[3H] -(±)-喹核醇基苯甲酸酯([3H] -(±)-QNB)与大鼠脑切片和匀浆制剂中毒蕈碱位点的结合情况。2. 提供的证据支持这样一种观点,即只有QNB的(-)-对映体与毒蕈碱位点具有高亲和力结合。3. 切片中[3H] -(-)-QNB结合的Kd值比匀浆中测得的值高八倍。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. 有人提出,这些结果可能反映了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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Muscarinic cholinergic binding in rat brain.大鼠脑中的毒蕈碱型胆碱能结合
Proc Natl Acad Sci U S A. 1974 May;71(5):1725-9. doi: 10.1073/pnas.71.5.1725.
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Biochemical studies on muscarinic acetylcholine receptors.毒蕈碱型乙酰胆碱受体的生化研究
J Neurochem. 1976 Jul;27(1):7-16. doi: 10.1111/j.1471-4159.1976.tb01536.x.

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