Characterization of voltage operated R-type Ca2+ channels in modulating somatostatin receptor subtype 2- and 3-dependent inhibition of insulin secretion from INS-1 cells

Cell Signal. 2008 Dec;20(12):2286-95. doi: 10.1016/j.cellsig.2008.08.015. Epub 2008 Aug 28.

Abstract

Somatostatin (SST) inhibits Ca(2+) entry into pancreatic B-cells via voltage-operated Ca(2+) channels (VOCCs) of L-type, leading to the suppression of insulin secretion. Activation of R-type channels increases insulin secretion. However, the role of R-type Ca(2+) channels (Ca(V)2.3) in mediating the effects of SST on insulin secretion has not been so far investigated. Here, we identify the SST-receptor subtypes (SSTR) expressed on insulin-producing INS-1 cells by RT-PCR and by functional assays. The role of R-type channels in regulating [Ca(2+)](i) in response to SST-treatment was detected by cell fluorescence imaging and patch-clamp technique. INS-1 expressed SSTR2 and SSTR3 and agonists (ag.) selective for these receptors reduced 10 nM exendin-4/20 mM glucose-stimulated insulin secretion. Surprisingly, SST and SST2-ag. transiently increased [Ca(2+)](i). Subsequently, these agonists led to a decrease in [Ca(2+)](i) below the basal levels. In contrast, SST3-ag. failed to induce a transient peak of [Ca(2+)](i). Instead, a persistent minor suppression of [Ca(2+)](i) was detected from 25 min. R-type channel blocker SNX-482 altered [Ca(2+)](i) in SST- and SST2-ag.-treated cells. Notably, the inhibition of insulin secretion by SST and SST2-ag., but not SST3-ag. was attenuated by SNX-482. Taken together, SST and SSTR2 regulate [Ca(2+)](i) and insulin secretion in INS-1 cells via R-type channels. In contrast, the R-type calcium channel does not mediate the effects of SST3-ag. on insulin secretion. We conclude that R-type channels play a major role in the inhibition of insulin secretion by somatostatin in INS-1 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Base Sequence
  • Calcium / metabolism
  • Calcium Channels, R-Type / drug effects
  • Calcium Channels, R-Type / physiology*
  • Electrophysiological Phenomena
  • Insulin / metabolism*
  • RNA, Messenger / metabolism
  • Rats
  • Receptors, Somatostatin / agonists
  • Receptors, Somatostatin / metabolism*
  • Somatostatin / metabolism*
  • Spectrometry, Fluorescence
  • Spider Venoms / pharmacology
  • Time Factors

Substances

  • Calcium Channels, R-Type
  • Insulin
  • RNA, Messenger
  • Receptors, Somatostatin
  • SNX 482
  • Spider Venoms
  • somatostatin receptor 3
  • Somatostatin
  • somatostatin receptor 2
  • Calcium