Department of Pharmacology and Therapeutics, University of Florida, Gainesville, FL 32610-0267, USA.
Br J Pharmacol. 2010 Aug;160(8):1903-5. doi: 10.1111/j.1476-5381.2010.00868.x.
Li and Steinbach apply nonstationary noise analysis to the whole-cell current responses of low sensitivity alpha4beta2 nAChR stably-expressed in HEK cells. These receptors represent one of the most important nAChR subtypes in brain, and also one of the most difficult to study in native tissues. They found the activating properties of the full agonists ACh and nicotine to be similar with regard to P(open) and single channel conductance, whereas the weak alpha4beta2 partial agonist cytisine caused channels to open with low probability but increased single channel conductance. When optimally stimulated by either of the full agonists, approximately 80% of the available receptors opened at the peak of the response. However, comparisons of whole-cell current to estimates of total cell surface receptors, indicated that only about 7% of the total receptor population can be activated. These observations provide important and intriguing new pieces of the brain nicotine receptor puzzle.
李和斯坦巴赫将非平稳噪声分析应用于稳定表达于 HEK 细胞的低敏感性 alpha4beta2 nAChR 的全细胞电流反应。这些受体是大脑中最重要的 nAChR 亚型之一，也是在天然组织中最难研究的受体之一。他们发现，全激动剂 ACh 和尼古丁的激活特性在 P(open)和单通道电导方面相似，而弱的 alpha4beta2 部分激动剂 cytisine 导致通道以低概率打开，但增加了单通道电导。当被全激动剂之一最佳刺激时，大约 80%的可用受体在反应峰时打开。然而，将全细胞电流与总细胞表面受体的估计值进行比较表明，只有大约 7%的总受体群体可以被激活。这些观察结果为大脑尼古丁受体之谜提供了重要而有趣的新线索。
