| NOVÁKOVÁ, Marie, Catherine ELA, Wayne D. BOWEN, Yonathan HASIN a Yael EILAM. Highly selective sigma receptor ligands elevate inositol 1,4,5-trisphosphate production in rat cardiac myocytes. European Journal of Pharmacology. Elsevier, 1998, roč. 353, 2-3, s. 315-327. ISSN 0014-2999. |
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@article{199500,
author = {Nováková, Marie and Ela, Catherine and Bowen, Wayne D. and Hasin, Yonathan and Eilam, Yael},
article_number = {2-3},
keywords = {sigma receptors; cardiac myocytes; contractility; Ca2+ cytosolic; inositol 1;4;5-trisphosphate; phospholipase C},
language = {eng},
issn = {0014-2999},
journal = {European Journal of Pharmacology},
title = {Highly selective sigma receptor ligands elevate inositol 1,4,5-trisphosphate production in rat cardiac myocytes.},
volume = {353},
year = {1998}
}
TY - JOUR
ID - 199500
AU - Nováková, Marie - Ela, Catherine - Bowen, Wayne D. - Hasin, Yonathan - Eilam, Yael
PY - 1998
TI - Highly selective sigma receptor ligands elevate inositol 1,4,5-trisphosphate production in rat cardiac myocytes.
JF - European Journal of Pharmacology
VL - 353
IS - 2-3
SP - 315
EP - 315
PB - Elsevier
SN - 00142999
KW - sigma receptors
KW - cardiac myocytes
KW - contractility
KW - Ca2+ cytosolic
KW - inositol 1;4;5-trisphosphate
KW - phospholipase C
N2 - Exposure of cardiac myocytes from adult rat ventricles to the highly selective, high affinity sigma receptor ligands BD-737 (0.1-100 nM) and BD-1047 (0.01-10 nM) caused potentiation of electrically-evoked amplitudes of contraction and Ca2q transients, while exposure to 100 nM BD-1047 caused attenuation of these amplitudes. In addition, BD-737 (1-100 nM) and BD-1047 (10-100 nM) caused an increase in the incidence of spontaneous twitches. These effects were inhibited when the incubation with BD-737 was done in the presence of the phospholipase C inhibitor, neomycin, or after pre-incubation with thapsigargin or caffeine which deplete the sarcoplasmic reticulum Ca2q stores. Inositol 1,4,5-trisphosphate (IP3) production in cardiac myocytes was determined by the IP3 binding protein assay. Both substances caused an increase in the intracellular concentration of IP3. BD-737 caused a rapid transient increase to 3.2-fold in 1 min and stabilization at 2.1-fold of control thereafter. BD-1047 caused a gradual increase reaching 4.4-fold after 5 min. The results suggest that the effects of these sigma receptor ligands on contractility and spontaneous contractions are mediated by activation of phospholipase C and elevation of intracellular IP3 level.
ER -
NOVÁKOVÁ, Marie, Catherine ELA, Wayne D. BOWEN, Yonathan HASIN a Yael EILAM. Highly selective sigma receptor ligands elevate inositol 1,4,5-trisphosphate production in rat cardiac myocytes. \textit{European Journal of Pharmacology}. Elsevier, 1998, roč.~353, 2-3, s.~315-327. ISSN~0014-2999.
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