Highly selective sigma receptor ligands elevate inositol
1,4,5-trisphosphate production in rat cardiac myocytes.

J 1998

Highly selective sigma receptor ligands elevate inositol 1,4,5-trisphosphate production in rat cardiac myocytes.

NOVÁKOVÁ, Marie, Catherine ELA, Wayne D. BOWEN, Yonathan HASIN, Yael EILAM et. al.

Basic information

Original name

Highly selective sigma receptor ligands elevate inositol 1,4,5-trisphosphate production in rat cardiac myocytes.

Name in Czech

Vysoce selektivní ligandy sigma receptorů zvyšují produkci 1,4,5-trisfosfátu u srdečních myocytů potkana

Authors

NOVÁKOVÁ, Marie (203 Czech Republic, guarantor), Catherine ELA (376 Israel), Wayne D. BOWEN (840 United States of America), Yonathan HASIN (376 Israel) and Yael EILAM (376 Israel)

Edition

European Journal of Pharmacology, Elsevier, 1998, 0014-2999

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

30105 Physiology

Country of publisher

Netherlands

Confidentiality degree

není předmětem státního či obchodního tajemství

Impact factor

Impact factor: 1.992

Organization unit

Faculty of Medicine

UT WoS

000075335800019

Keywords in English

sigma receptors; cardiac myocytes; contractility; Ca2+ cytosolic; inositol 1;4;5-trisphosphate; phospholipase C

Abstract

ORIG CZ

V originále

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.

In Czech

Vysoce specifické ligandy sigma receptorů zvyšují sílu stahu komorových kardiomyocytů poté, co se ze sarkoplazmatického retikula vylije vápník. Otevření retikula je zprostředkováno zvýšenou produkcí inositol-tris-fosfátu.

Citovat

NOVÁKOVÁ, Marie, Catherine ELA, Wayne D. BOWEN, Yonathan HASIN and Yael EILAM. Highly selective sigma receptor ligands elevate inositol 1,4,5-trisphosphate production in rat cardiac myocytes. European Journal of Pharmacology. Elsevier, 1998, vol. 353, 2-3, p. 315-327. ISSN 0014-2999.

@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 and 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, vol.~353, 2-3, p.~315-327. ISSN~0014-2999.

Detailed Information on Publication Record