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大鼠脑中不可被乙酰胆碱置换的3[H]埃博霉素结合

Non-acetylcholine displaceable 3[H]epibatidine binding in the rat brain.

作者信息

Plenge P, Mellerup E

机构信息

Department of Pharmacology, University of Copenhagen, Denmark.

出版信息

Neurosci Lett. 1998 May 22;248(1):65-7. doi: 10.1016/s0304-3940(98)00329-2.

Abstract

Using autoradiography two types of 3[H]epibatidine binding in rat brain was found, the by far most widespread was nicotine displaceable, and represented nicotinic cholinergic receptors, probably the two subtypes alpha4beta2 and alpha3beta4. Using acetylcholine and nicotine in concentrations able to displace 3[H]epibatidine from the alpha4beta2 and alpha3beta4 subunits, in a few brain structures a non-acetylcholine and non-nicotine displaceable 3[H]epibatidine binding was found. The binding was almost exclusively localised to the medial and lateral habenula, interpeduncular nucleus and pineal gland; at 0.1 nM 3[H]epibatidine it represented about 40% of the total 3[H]epibatidine binding. A literature search directed at neurotransmitters in habenula did not demonstrate any neurotransmitter with this anatomical distribution in the brain, suggesting that the non-acetylcholine displaceable 3[H]epibatidine binding represents a binding site, not previously described.

摘要

通过放射自显影法,在大鼠脑中发现了两种类型的3[H]埃博霉素结合,其中分布最广泛的是可被尼古丁取代的,代表烟碱型胆碱能受体,可能是α4β2和α3β4两种亚型。使用能够从α4β2和α3β4亚基上取代3[H]埃博霉素的乙酰胆碱和尼古丁浓度,在一些脑结构中发现了一种不可被乙酰胆碱和尼古丁取代的3[H]埃博霉素结合。这种结合几乎完全定位于内侧和外侧缰核、脚间核和松果体;在0.1 nM的3[H]埃博霉素浓度下,它占总3[H]埃博霉素结合的约40%。针对缰核中神经递质的文献检索未发现任何在脑中具有这种解剖分布的神经递质,这表明不可被乙酰胆碱取代的3[H]埃博霉素结合代表了一个以前未描述过的结合位点。

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