Identification of four brain areas each enriched in a unique muscarinic receptor subtype.
Identification of four brain areas each enriched in a unique muscarinic receptor subtype.
复制标题
鉴定出四个大脑区域，每个区域都富含独特的毒蕈碱受体亚型。
DOI：
10.1016/0024-3205(90)90413-l
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发表时间：
1990
期刊：
影响因子：
6.1
通讯作者：
MesserJr,WS
中科院分区：
文献类型：
--
作者：
Hoss,W;Ellerbrock,BR;Goldman,PS;Collins,DA;MesserJr,WS
通过放射自显影和图像分析在大鼠大脑的选定区域确定毒蕈碱激动剂和拮抗剂的亲和力。在冠状切片中测量0.2 nM [3H]-QNB与齿状回、上丘、菱形丘脑和黑质结合的抑制的IC50值和Hill系数。哌仑西平对齿状回和 AF-DX 116（上丘）的受体表现出高亲和力。哌仑西平和 AF-DX 116 均对黑质具有高亲和力，而对菱形丘脑具有低亲和力。 Gallamine 对上丘受体的偏好是齿状回受体的 50 倍。阿米替林的选择性较低，对黑质受体表现出适度的偏好，而 4-DAMP 基本上是非选择性的。卡巴胆碱是最具选择性的激动剂，对上丘受体的偏好是齿状回受体的 4000 倍。除 RS 86 外的其他激动剂也对上丘受体具有选择性，顺序为卡巴胆碱⪢槟榔碱 > 氨甲酰胆碱 > McN A343 = 氧化震颤素 = 毛果芸香碱。
The affinities of muscarinic agonists and antagonists were determined by autoradiography and image analysis in selected areas of the rat brain. IC50values and Hill coefficients for the inhibition of the binding of 0.2 nM [3H]-QNB to dentate gyrus, superior colliculus, rhomboid thalamus and substantia nigra were measured in coronal sections. Pirenzepine displayed a high affinity for receptors in the dentate gyrus and AF-DX 116, the superior colliculus. Both pirenzepine and AF-DX 116 had high affinities for the substantia nigra and low affinities for the rhomboid thalamus. Gallamine displayed a 50-fold preference for superior colliculus over dentate gyrus receptors. Amitriptyline was less selective, showing a modest preference for substantia nigra receptors and 4-DAMP was essentially nonselective. Carbachol was the most selective agonist with a 4000-fold preference for superior colliculus over dentate gyrus receptors. Other agonists except RS 86 were also selective for superior colliculus receptors in the order carbachol ⪢ arecoline > bethanechol > McN A343 = oxotremorine = pilocarpine.