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豚鼠耳蜗核和听神经中的毒蕈碱受体。

Muscarinic receptors in the cochlear nucleus and auditory nerve of the guinea pig.

作者信息

Whipple M R, Drescher D G

出版信息

J Neurochem. 1984 Jul;43(1):192-8. doi: 10.1111/j.1471-4159.1984.tb06696.x.

Abstract

The specific-binding properties of l-[3H]quinuclidinyl benzilate, a muscarinic acetylcholine-receptor antagonist, were investigated in synaptic and other membrane preparations of the guinea pig cochlear nucleus and auditory nerve. Binding parameters for all experiments were consistent with a single binding site with a Hill coefficient of 1.0. The binding of the ligand was specific and of high affinity, with values of KD in the range of 30-80 pM. Bmax was 0.352 +/- 0.023 pmol/mg protein for the dorsal cochlear nucleus and 0.215 +/- 0.011 pmol/mg protein for the ventral cochlear nucleus. The dorsal cochlear nucleus/ventral cochlear nucleus ratio for density of muscarinic receptors (1.6/1.0) was maintained across two different buffer systems, which varied with respect to the inclusion of proteolysis inhibitors. The results for auditory nerve indicated a level of binding much below that of the cochlear nucleus, with Bmax = 0.052 +/- 0.011 pmol/mg protein. The results of specific-binding experiments for l-[3H]quinuclidinyl benzilate support a role for acetylcholine as a neurotransmitter in the cochlear nucleus. The greater density of muscarinic receptors in the dorsal cochlear nucleus may indicate greater cholinergic activity in the dorsal relative to the ventral cochlear nucleus.

摘要

在豚鼠耳蜗核和听神经的突触及其他膜制剂中,研究了毒蕈碱型乙酰胆碱受体拮抗剂l-[3H]东莨菪碱的特异性结合特性。所有实验的结合参数均与希尔系数为1.0的单一结合位点一致。配体的结合具有特异性且亲和力高,KD值在30 - 80 pM范围内。背侧耳蜗核的Bmax为0.352±0.023 pmol/mg蛋白,腹侧耳蜗核为0.215±0.011 pmol/mg蛋白。在两种不同的缓冲系统中,毒蕈碱受体密度的背侧耳蜗核/腹侧耳蜗核比值(1.6/1.0)保持不变,这两种缓冲系统在是否包含蛋白水解抑制剂方面有所不同。听神经的结果表明结合水平远低于耳蜗核,Bmax = 0.052±0.011 pmol/mg蛋白。l-[3H]东莨菪碱特异性结合实验的结果支持乙酰胆碱作为耳蜗核神经递质的作用。背侧耳蜗核中毒蕈碱受体密度更高可能表明相对于腹侧耳蜗核,背侧的胆碱能活性更高。

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