DEVELOPMENTAL REGULATION OF THE A-TYPE POTASSIUM- CHANNEL CURRENT IN HIPPOCAMPAL NEURONS: ROLE OF THE Kv1.1 SUBUNIT T. FALK, a R. K. KILANI, b L. A. STRAZDAS, b R. S. BORDERS, b J. V. STEIDL, a1 A. J. YOOL a AND S. J. SHERMAN a,b * a Department of Physiology b Department of Neurology, The University of Arizona, 1501 North Campbell Avenue, Tucson, AZ 85724, USA Abstract—The rapidly inactivating A-type K current (I A ) is prominent in hippocampal neurons; and the speed of its inactivation may regulate electrical excitability. The auxiliary K channel subunit Kv1.1 confers fast inactivation to Shak- er-related channels and is postulated to affect I A . Whole-cell patch clamp recordings of rat hippocampal pyramidal neu- rons in primary culture showed a developmental decrease in the time constant of inactivation ( in ) of voltage-gated K currents: 17.91.5 ms in young neurons (5–7 days in vitro; n53, meanS.E.M.); 9.91.0 ms in mature neurons (12–15 days in vitro; n72, meanS.E.M., P<0.01). During the same developmental time, the level of Kv1.1 transcript increased more than two-fold in vitro and in vivo, determined by semi- quantitative reverse transcriptase-polymerase chain reaction for hippocampus. The hypothesis that up-regulation of Kv1.1 led to the changes in in was tested in vitro, using antisense knockdown. Kv1.1-specific antisense DNA was introduced with a modified herpes virus co-expressing en- hanced green fluorescent protein and knockdown of Kv1.1 was verified by immunocytochemistry. Following transduc- tion with the antisense virus, mature neurons reverted to in values characteristic of young neurons: 18.32.4 ms (n20). The effect of antisense knockdown on electrical excitability was tested using current-clamp protocols to induce repetitive firing. Treatment with the antisense virus increased the inter- spike interval over a range of membrane depolarization (baseline membrane potential40 to 20 mV). This effect was most pronounced at 40 mV, where the ISI of the first pair of action potentials was nearly doubled. These data indicate that Kv1.1 contributes to the devel- opmental control of I A in hippocampal neurons and that the magnitude of effect is sufficient to regulate electrical excit- ability. Viral-mediated antisense knockdown of Kv1.1 is ca- pable of decreasing the electrical excitability of post-mitotic hippocampal neurons, suggesting this approach has appli- cability to gene therapy of neurological diseases associated with hyperexcitability. © 2003 IBRO. Published by Elsevier Science Ltd. All rights reserved. Key words: antisense DNA, herpes simplex virus 1, voltage clamp, gene therapy. Profound changes in neuronal excitability occur within the hippocampus during early postnatal brain development (Johnston, 1996; Swann et al., 1990) and result from the regulation of numerous individual genes. Defining the mo- lecular basis of these changes is a formidable challenge, but will be rewarding in our understanding of both normal development and the pathophysiology of disorders such as epilepsy. Voltage-gated K + channels play a fundamental role in controlling neuronal excitability and are critical de- terminants of the interspike interval (ISI) during repetitive firing (Hille, 1992). In this regard, the degree and speed of K + channel inactivation following an action potential is a major regulatory influence in determining the firing rate. The A-type current (I A ), initially described in molluscan systems, is a transient outward K + current that contributes to mechanisms of learning and memory (Storm, 1987; Johnston et al., 2000; Giese et al., 2001) and is prominent in mammalian hippocampus (Hoffman et al., 1997). The I A current of the hippocampus is defined by its electrophysi- ological characteristics of rapid inactivation following de- polarization. Due to the immense diversity of K + channels, it is likely that there are several subtypes of K + channels that, in sum, give rise to the macroscopic I A current (Song, 2002). At the present time, there is a paucity of information concerning which K + channels species contribute to I A in different brain regions or in different stages of develop- ment. In this report, we studied the developmental time course of Kv1.1, an auxiliary subunit of voltage-gated K + channels, and then correlated the level of expression of this gene to the electrophysiological properties of develop- ing hippocampal neurons. The K + channel complex con- sists of tetrameric pore-forming -subunits and auxiliary -subunits that play a modulatory role (Pongs et al., 1999). A simplified nomenclature has been suggested which di- vides the -subunits into 3 sub-families (Kv1.n, Kv2.1, Kv3.1), Kv1.n having three members (England et al., 1995). Kv1.n, and Kv3.1 subunits are known to regulate inactivation properties of the channel complex (Rettig et al., 1994) and Kv2.1 acts as a chaperone molecule (Pongs et al., 1999) that guides sub-cellular localization of -subunits. Since Kv1.1 associates with -subunits in the 1 Present address: Department of Drug Safety Evaluation, Pfizer, Inc., San Diego, CA, USA. *Correspondence to: S. J. Sherman, Department of Neurology, The University of Arizona, 1501 North Campbell Avenue, Tucson, AZ 85724, USA. Tel: +1-520-626-2319; fax: +1-520-626-5999. E-mail address: ssherman@u.arizona.edu (S. J. Sherman). Abbreviations: EGTA, ethylene glycol-bis (b-aminoethyl ether)- N,N,N',N'-tetraacetic acid; eGFP, enhanced green fluorescent protein; HEPES, N-(2-hydroxyethyl)piperazine-N'-2-ethanesulfonic acid; I A , A- type K + current; ISI, interspike interval; I SS , steady-state current; MEM, minimal essential medium; PBS, phosphate-buffered saline; in , time constant of inactivation; RT-PCR, reverse transcriptase polymerase chain reaction; Vm, baseline membrane potential. Neuroscience 120 (2003) 387– 404 0306-4522/03$30.00+0.00 © 2003 IBRO. Published by Elsevier Science Ltd. All rights reserved. doi:10.1016/S0306-4522(03)00044-7 387