Pedarzani P, Storm J F
Institute of Neurophysiology, University of Oslo, Norway.
Proc Natl Acad Sci U S A. 1995 Dec 5;92(25):11716-20. doi: 10.1073/pnas.92.25.11716.
Ion channels underlying the electrical activity of neurons can be regulated by neurotransmitters via two basic mechanisms: ligand binding and covalent modification. Whereas neurotransmitters often act by binding directly to ion channels, the intracellular messenger cyclic AMP is thought usually to act indirectly, by activating protein kinase A, which in turn can phosphorylate channel proteins. Here we show that cyclic AMP, and transmitters acting via cyclic AMP, can act in a protein kinase A-independent manner in the brain. In hippocampal pyramidal cells, cyclic AMP and norepinephrine were found to cause a depolarization by enhancing the hyperpolarization-activated mixed cation current, IQ (also called Ih). This effect persisted even after protein kinase A activity was blocked, thus strongly suggesting a kinase-independent action of cyclic AMP. The modulation of this current by ascending monoaminergic fibers from the brainstem is likely to be a widespread mechanism, participating in the state control of the brain during arousal and attention.
配体结合和共价修饰。神经递质通常通过直接结合离子通道发挥作用,而细胞内信使环磷酸腺苷(cAMP)通常被认为是通过激活蛋白激酶A间接发挥作用,蛋白激酶A进而可使通道蛋白磷酸化。在此我们表明,cAMP以及通过cAMP起作用的递质可在大脑中以不依赖蛋白激酶A的方式发挥作用。在海马锥体细胞中,发现cAMP和去甲肾上腺素通过增强超极化激活的混合阳离子电流(IQ,也称为Ih)引起去极化。即使在蛋白激酶A活性被阻断后,这种效应仍然存在,因此有力地表明了cAMP的激酶非依赖性作用。来自脑干的上行单胺能纤维对这种电流的调制可能是一种广泛存在的机制,参与觉醒和注意力期间大脑的状态控制。