Receptor-Mediated Modulation of Voltage-Dependent Ca^<2+> Channels via Heterotrimeric G-proteins in Neurons

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Author(s)

Abstract

The activity of voltage-dependent Ca<SUP>2+</SUP> channels is highly regulated by neurotransmitter receptors coupled to heterotrimeric G-proteins. In the expression studies using cloned Ca<SUP>2+</SUP> channel subunits, it has been clarified that the main mechanism of the inhibition of N-type channel current is mediated directly by G-protein βγ subunits in a membrane-delimited and voltage-sensitive manner. In addition, recent studies have also clarified that N-type channels are modulated by several G-protein α subunits in different ways. Among them, G<SUB>αo</SUB> mediates a voltage-resistant inhibition of N-type current by neurotransmitters. This type of inhibition is more apparent in the case of P/Q-type channels in both native cells and expression systems. Moreover, other G-protein subunits, such as G<SUB>αq</SUB> and G<SUB>αs</SUB>, also seem to regulate N-type channels in a membrane-delimited manner. The fine tunings of Ca<SUP>2+</SUP> channel activity by intracellular proteins have physiological and pathological meanings in the regulation of Ca<SUP>2+</SUP> influx into excitable cells by neurotransmitters and pharmacological implications as novel drug targets for controlling Ca<SUP>2+</SUP> influx.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 81(4), 324-331, 1999-12-01

    The Japanese Pharmacological Society

References:  55

Cited by:  1

Codes

  • NII Article ID (NAID)
    10008197430
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    00215198
  • NDL Article ID
    4948488
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  CJPref  NDL  J-STAGE 
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