Department of Psychiatry and Behavioral Sciences, Emory University, Atlanta, GA, USA.
Neuropharmacology. 2012 Mar;62(4):1671-83. doi: 10.1016/j.neuropharm.2011.11.013. Epub 2011 Dec 8.
The anterolateral cell group of the bed nucleus of the stria terminalis (BNST(ALG)) serves as an important relay station in stress circuitry. Limbic inputs to the BNST(ALG) are primarily glutamatergic and activity-dependent changes in this input have been implicated in abnormal behaviors associated with chronic stress and addiction. Significantly, local infusion of acetylcholine (ACh) receptor agonists into the BNST trigger stress-like cardiovascular responses, however, little is known about the effects of these agents on glutamatergic transmission in the BNST(ALG). Here, we show that glutamate- and ACh-containing fibers are found in close association in the BNST(ALG). Moreover, in the presence of the acetylcholinesterase inhibitor, eserine, endogenous ACh release evoked a long-lasting reduction of the amplitude of stimulus-evoked EPSCs. This effect was mimicked by exogenous application of the ACh analog, carbachol, which caused a reversible, dose-dependent, reduction of the evoked EPSC amplitude, and an increase in both the paired-pulse ratio and coefficient of variation, suggesting a presynaptic site of action. Uncoupling of postsynaptic G-proteins with intracellular GDP-β-S, or application of the nicotinic receptor antagonist, tubocurarine, failed to block the carbachol effect. In contrast, the carbachol effect was blocked by prior application of atropine or M(2) receptor-preferring antagonists, and was absent in M(2)/M(4) receptor knockout mice, suggesting that presynaptic M(2) receptors mediate the effect of ACh. Immunoelectron microscopy studies further revealed the presence of M(2) receptors on axon terminals that formed asymmetric synapses with BNST neurons. Our findings suggest that presynaptic M(2) receptors might be an important modulator of the stress circuit and hence a novel target for drug development.
终纹床核前外侧细胞群(BNST(ALG))作为应激回路中的一个重要中继站。BNST(ALG)的边缘输入主要是谷氨酸能的,并且这种输入的活性依赖性变化与慢性应激和成瘾相关的异常行为有关。值得注意的是,局部输注乙酰胆碱(ACh)受体激动剂到 BNST 会引发应激样心血管反应,然而,关于这些药物对 BNST(ALG)中谷氨酸能传递的影响知之甚少。在这里,我们发现谷氨酸和 ACh 包含的纤维在 BNST(ALG)中紧密相关。此外,在乙酰胆碱酯酶抑制剂 eserine 的存在下,内源性 ACh 释放会引起刺激诱发的 EPSC 幅度的长时间减少。这种效应被 ACh 类似物 carbachol 的外源性应用模拟,carbachol 引起刺激诱发的 EPSC 幅度的可逆、剂量依赖性减少,以及成对脉冲比和变异系数的增加,表明其作用于突触前部位。用细胞内 GDP-β-S 使突触后 G 蛋白解偶联,或应用烟碱受体拮抗剂筒箭毒碱,都不能阻断 carbachol 的作用。相反,carbachol 的作用被阿托品或 M(2)受体优先拮抗剂的预先应用所阻断,并且在 M(2)/M(4)受体敲除小鼠中缺失,这表明突触前 M(2)受体介导了 ACh 的作用。免疫电子显微镜研究进一步表明,M(2)受体存在于形成与 BNST 神经元形成不对称突触的轴突末梢上。我们的发现表明,突触前 M(2)受体可能是应激回路的重要调节剂,因此是药物开发的新靶点。