PMID- 1647969 OWN - NLM STAT- MEDLINE DCOM- 19910802 LR - 20191210 IS - 0014-5793 (Print) IS - 0014-5793 (Linking) VI - 284 IP - 1 DP - 1991 Jun 17 TI - Calcium mobilization in human platelets by receptor agonists and calcium-ATPase inhibitors. PG - 1-4 AB - Inhibitors of the endoplasmic reticulum Ca(2+)-ATPase like thapsigargin (TG) and 2,5-di (tert-butyl)-1,4-benzohydroquinone (tBuBHQ) cause increases in cytosolic calcium in intact human platelets resulting from prevention of reuptake. A maximal concentration of TG (0.2 microM) mobilized 100% of sequestered Ca2+ compared to the action of a receptor agonist like thrombin (0.1 U/ml). A maximal dose of tBuBHQ (50 microM) stimulated release of about 40% of intracellular calcium compared to thrombin and TG. The reduced ability of tBuBHQ to release calcium can be explained with an inhibitory effect on the cyclooxygenase pathway (Ki approximately 7 microM). Therefore tBuBHQ is not able to cause platelet aggregation compared to TG. In the presence of a cyclooxygenase inhibitor or a thromboxane A2 receptor antagonist the action of TG is identical to that observed with tBuBHQ. Generally, inhibition of calcium sequestration does not automatically result in platelet activation. In contrast to a receptor mediated activation Ca(2+)-ATPase inhibitors require the self-amplification mechanism of endogenously formed thromboxane A2 to cause a similar response. We conclude that the calcium store sensitive to Ca(2+)-ATPase inhibitors is a subset of the receptor sensitive calcium pool. FAU - Brune, B AU - Brune B AD - Faculty of Biology, University of Konstanz, Germany. FAU - Ullrich, V AU - Ullrich V LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - England TA - FEBS Lett JT - FEBS letters JID - 0155157 RN - 0 (Arachidonic Acids) RN - 0 (Hydroquinones) RN - 0 (Receptors, Cell Surface) RN - 0 (Terpenes) RN - 26XK13B61B (2,5-di-tert-butylhydroquinone) RN - 67526-95-8 (Thapsigargin) RN - EC 3.4.21.5 (Thrombin) RN - EC 7.2.2.10 (Calcium-Transporting ATPases) RN - SY7Q814VUP (Calcium) SB - IM MH - Arachidonic Acids/metabolism MH - Blood Platelets/*metabolism MH - Calcium/*blood MH - Calcium-Transporting ATPases/*antagonists & inhibitors MH - Cytosol/metabolism MH - Endoplasmic Reticulum/enzymology MH - Humans MH - Hydroquinones/*pharmacology MH - Platelet Aggregation MH - Receptors, Cell Surface/metabolism MH - Terpenes/*pharmacology MH - Thapsigargin MH - Thrombin/pharmacology EDAT- 1991/06/17 00:00 MHDA- 1991/06/17 00:01 CRDT- 1991/06/17 00:00 PHST- 1991/06/17 00:00 [pubmed] PHST- 1991/06/17 00:01 [medline] PHST- 1991/06/17 00:00 [entrez] AID - 0014-5793(91)80747-Q [pii] AID - 10.1016/0014-5793(91)80747-q [doi] PST - ppublish SO - FEBS Lett. 1991 Jun 17;284(1):1-4. doi: 10.1016/0014-5793(91)80747-q.