The roles of P(2X1)and P(2T AC)receptors in ADP-evoked calcium signalling in human platelets

Cell Calcium. 2000 Aug;28(2):119-26. doi: 10.1054/ceca.2000.0139.

Abstract

The roles of P(2X1)and P(2T AC)receptors in ADP-evoked Ca(2+)signalling were investigated in fura-2-loaded human platelets. Desensitization of the P(2X1)receptor with the selective agonist, alphabeta-methylene ATP, reduced the integral of the ADP-evoked rise in [Ca(2+)](i)to about 90% of control; a reduction equivalent to the integral of the P(2X1)-evoked response alone. After elevating cAMP or cGMP levels using prostaglandin E(1)or sodium nitroprusside, prior P(2X1)desensitization reduced the integral of the ADP-evoked response to about 70% of control. This reduction was greater than the integral of the P(2X1)-evoked response alone under the same conditions, suggesting rapidly activated Ca(2+)entry via the P(2X1)receptor potentiates Ca(2+)responses evoked via the phospholipase C-coupled P(2Y1)receptor. The P(2T AC)receptor antagonist, AR-C69931MX, at a concentration completely inhibiting aggregation, did not significantly affect the initial peaks but caused a significant reduction in the integrals of the ADP-evoked rises in [Ca(2+)](i)to about 71% or 77% of controls in the presence or absence of external Ca(2+)respectively. This suggests that the main effect of lowering cAMP levels after inhibition of adenylyl cyclase via P(2T AC)receptors may be reduced Ca(2+)removal from the cytosol. These results indicate that both the P(2X1)and P(2T AC)receptors play a significant role in ADP-evoked Ca(2+)signalling in human platelets.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Diphosphate / pharmacology
  • Adenosine Monophosphate / analogs & derivatives
  • Adenosine Monophosphate / pharmacology
  • Adenosine Triphosphate / analogs & derivatives
  • Adenosine Triphosphate / pharmacology
  • Blood Platelets / drug effects
  • Blood Platelets / metabolism*
  • Calcium Signaling* / drug effects
  • Humans
  • Membrane Proteins*
  • Platelet Aggregation Inhibitors / pharmacology
  • Purinergic P2 Receptor Agonists
  • Purinergic P2 Receptor Antagonists
  • Receptors, Purinergic P2 / metabolism*
  • Receptors, Purinergic P2X
  • Receptors, Purinergic P2Y12

Substances

  • Membrane Proteins
  • P2RY12 protein, human
  • Platelet Aggregation Inhibitors
  • Purinergic P2 Receptor Agonists
  • Purinergic P2 Receptor Antagonists
  • Receptors, Purinergic P2
  • Receptors, Purinergic P2X
  • Receptors, Purinergic P2Y12
  • Adenosine Monophosphate
  • Adenosine Diphosphate
  • cangrelor
  • Adenosine Triphosphate
  • alpha,beta-methyleneadenosine 5'-triphosphate