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.

Základní údaje

Originální název

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

Název česky

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

Autoři

NOVÁKOVÁ, Marie (203 Česká republika, garant), Catherine ELA (376 Izrael), Wayne D. BOWEN (840 Spojené státy), Yonathan HASIN (376 Izrael) a Yael EILAM (376 Izrael)

Vydání

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

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

30105 Physiology

Stát vydavatele

Nizozemské království

Utajení

není předmětem státního či obchodního tajemství

Impakt faktor

Impact factor: 1.992

Organizační jednotka

Lékařská fakulta

UT WoS

000075335800019

Klíčová slova anglicky

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

Štítky

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

Příznaky

Mezinárodní význam, Recenzováno

Změněno: 25. 6. 2009 20:53, prof. MUDr. Marie Nováková, Ph.D.

Anotace

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.

Česky

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 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.

@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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