Cell Calcium 35 (2004) 357–365 A store-operated mechanism determines the activity of the electrically excitable glucagon-secreting pancreatic -cell Yi-Jia Liu 1 , Elaine Vieira 1 , Erik Gylfe Department of Medical Cell Biology, Uppsala University Biomedical Centre, Husargatan 3, Box 571, SE-752 37 Uppsala, Sweden Received 7 August 2003; received in revised form 3 October 2003; accepted 15 October 2003 Abstract The glucagon-releasing pancreatic -cells are electrically excitable cells but the signal transduction leading to depolarization and secre- tion is not well understood. To clarify the mechanisms we studied [Ca 2+ ] i and membrane potential in individual mouse pancreatic -cells using fluorescent indicators. The physiological secretagogue l-adrenaline increased [Ca 2+ ] i causing a peak, which was often followed by maintained oscillations or sustained elevation. The early effect was due to mobilization of Ca 2+ from the endoplasmic reticulum (ER) and the late one to activation of store-operated influx of the ion resulting in depolarization and Ca 2+ influx through voltage-dependent L-type channels. Consistent with such mechanisms, the effects of adrenaline on [Ca 2+ ] i and membrane potential were mimicked by inhibitors of the sarco(endo)plasmic reticulum Ca 2+ ATPase. The -cells express ATP-regulated K + (K ATP ) channels, whose activation by diazoxide leads to hyperpolarization. The resulting inhibition of the voltage-dependent [Ca 2+ ] i response to adrenaline was reversed when the K ATP channels were inhibited by tolbutamide. However, tolbutamide alone rarely affected [Ca 2+ ] i , indicating that the K ATP channels are nor- mally closed in mouse -cells. Glucose, which is the major physiological inhibitor of glucagon secretion, hyperpolarized the -cells and inhibited the late [Ca 2+ ] i response to adrenaline. At concentrations as low as 3 mM, glucose had a pronounced stimulatory effect on Ca 2+ sequestration in the ER amplifying the early [Ca 2+ ] i response to adrenaline. We propose that adrenaline stimulation and glucose inhibition of the -cell involve modulation of a store-operated current, which controls a depolarizing cascade leading to opening of L-type Ca 2+ channels. Such a control mechanism may be unique among excitable cells. © 2003 Elsevier Ltd. All rights reserved. Keywords: Glucagon secretion; Store-operated Ca 2+ channel; Endoplasmic reticulum calcium sequestration; Endoplasmic reticulum calcium release; Membrane potential 1. Introduction Diabetes mellitus is characterized by hyperglycemia due to insulin deficiency, which is caused by pancreatic -cell destruction or disturbed secretion of the hormone. In both types 1 and 2 diabetes, failure of glucose to inhibit the se- cretion of blood glucose-elevating glucagon aggravates the hyperglycemia [1–3]. Moreover, glucagon secretion is not appropriately stimulated when blood glucose falls to low concentrations, a potentially life-threatening condition in insulin-treated diabetic subjects [4]. Whereas considerable attention has been focussed on insulin secretion from the -cell, much less is known about glucagon release from the pancreatic -cell. It has been proposed that insulin [5,6], Corresponding author. Tel.: +46-18-4714428; fax: +46-18-4714059. E-mail address: erik.gylfe@medcellbiol.uu.se (E. Gylfe). 1 Drs. Vieira and Liu contributed equally to the article. GABA [7], or Zn 2+ [8] co-secreted with insulin from the -cell, mediates glucose inhibition of glucagon secretion. Although such mechanisms may contribute, they cannot ex- plain why glucose inhibits glucagon secretion from purified -cells [9], and why secretion is inhibited at lower sugar concentrations than those stimulating the secretory activity of the -cell [10]. Metabolism of glucose is essential both for stimulation of insulin release [11] and inhibition of glucagon secretion [12,13]. In the -cell the closure of the ATP-sensitive K + (K ATP ) channels has a central role in stimulus-secretion coupling, transducing the increase in ATP/ADP ratio ob- tained with glucose metabolism into depolarization with re- sulting opening of voltage-dependent L-type Ca 2+ channels [11]. There are diverging opinions about the presence of K ATP channels in the -cell and their possible involvement in the regulation of glucagon secretion [6,14–18]. Since glucose inhibits glucagon release, it is apparent that a fun- 0143-4160/$ – see front matter © 2003 Elsevier Ltd. All rights reserved. doi:10.1016/j.ceca.2003.10.002