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.
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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
Original language English
Type of outcome Article in a journal
Field of Study 30105 Physiology
Country of publisher Netherlands
Confidentiality degree is not subject to a state or trade secret
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
Tags 4, 5-trisphosphate, Ca2+ cytosolic, cardiac myocytes, contractility, inositol 1, phospholipase C, sigma receptors
Tags International impact, Reviewed
Changed by Changed by: prof. MUDr. Marie Nováková, Ph.D., učo 1188. Changed: 25/6/2009 20:53.
Abstract
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.
Abstract (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.
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