Effects of YT : 146 [2 : (1 : Octyny1) Adenosine], an Adenosine A_<2A> Receptor Agonist, on cAMP Production and Noradrenaline Release in PC12 Cells

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Abstract

Effects of YT-146 [2-(1-octynyl) adenosine], an adenosine A<SUB>2</SUB> receptor agonist, on cAMP production and noradrenaline (NA) release were investigated in PC12 cells. YT-146 caused a concentration-dependent cAMP accumulation (EC<SUB>50</SUB>: 1.2±0.9 nM). In [<SUP>3</SUP>H]NA-prelabeled cells, YT-146 increased the basal NA release and enhanced ATP-evoked NA release in a concentration-dependent manner (EC<SUB>50</SUB>: 0.23±0.15 nM). YT-146 augmented the maximal response to ATP without affecting the EC<SUB>50</SUB> value of ATP. These effects of YT-146 were inhibited by several adenosine receptor antagonists with a characteristic of adenosine A<SUB>2A</SUB> receptor subtype. The effects of YT-146 were mimicked by forskolin, dibutylyl cAMP and Sp-cAMPS, and inhibited by H-89, a cAMP-dependent protein kinase inhibitor. YT-146 had little effect on ATP-induced increase in intracellular Ca<SUP>2+</SUP> concentration. YT-146 enhanced the NA release induced by several different stimuli including Ca<SUP>2+</SUP> ionophore A23187. The present results suggest that YT-146 is a potent agonist on adenosine A<SUB>2A</SUB> receptors in PC12 cells and causes a cAMP-dependent enhancement of NA release by affecting the exocytosis process at a point downstream of the intracellular Ca<SUP>2+</SUP> increase.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 78(3), 269-277, 1998-11-01

    The Japanese Pharmacological Society

References:  38

Cited by:  3

Codes

  • NII Article ID (NAID)
    10008681058
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    00215198
  • NDL Article ID
    4610815
  • 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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