Search results for "Calcium"
showing 10 items of 1740 documents
5-Oxo-1,4-dihydroindenopyridines: Calcium modulators with partial calcium agonistic activity
1990
The title compounds 4a-g were prepared by Knoevenagel reactions of 1,3-indandione (1) with the aromatic aldehydes 2a-g followed by cyclizing Michael addition of the products thus obtained with methyl β-aminocrotonate (3). The structures of products 4 were characterized by spectal data. Positive inotropic activities were observed on electrically stimulated, left atria of giunea pigs and these effects could be attributed to calcium agonism. On the other hand, barium chloride-induced contractions of guinea pig ileum were inhibited in a dose-dependent manner.
ChemInform Abstract: 5-Oxo-1,4-dihydroindenopyridines: Calcium Modulators with Partial Calcium Agonistic Activity.
1990
The title compounds 4a-g were prepared by Knoevenagel reactions of 1,3-indandione (1) with the aromatic aldehydes 2a-g followed by cyclizing Michael addition of the products thus obtained with methyl β-aminocrotonate (3). The structures of products 4 were characterized by spectal data. Positive inotropic activities were observed on electrically stimulated, left atria of giunea pigs and these effects could be attributed to calcium agonism. On the other hand, barium chloride-induced contractions of guinea pig ileum were inhibited in a dose-dependent manner.
ChemInform Abstract: Vinylogous and Coupled Hexahydroquinolinones and Dihydropyridines with Calcium-Modulating Effects.
1990
The vinylogous, anellated and non-anellated dihydropyridines 4 and their coupled analogues 5 are accessible through Hantzsch-type cyclization reactions. IR, 1H-NMR, and mass spectral data are in agreement with the postulated structures. Pharmacological investigations on electrically-stimulated left atria of guinea pigs with some of the compounds gave rise to positive inotropic activities whereas BaCl2-induced contractions of the ileum were inhibited in a dose-dependent manner by some of the products.
Dissociation of theophylline uptake and inotropic effect in myocardial tissue: influence of temperature, pH and calcium.
1975
1. The myocardial uptake and the positive inotropic effect of theophylline (100 mug/ml; 0.56 mM) were studied in isolated electrically driven guinea-pig hearts perfused by the Langendorff technique under various extracellular conditions. [3H]-theophylline was used. 2. Variations in temperature, hydrogen ion and calcium ion concentrations of the perfusion media changed the time course and magnitude of the effect of theophylline on myocardial twitch tension but did not affect the time course and amount of theophylline uptake. 3. Under all conditions, the build-up of the positive inotropic effect of theophylline was about three times faster than the uptake of the drug into the heart. 4. Since …
Does cyclic GMP mediate the negative inotropic effect of acetylcholine in the heart?
1977
DURING vagal stimulation the pacemaker activity of the heart is diminished. The reduction in heart rate is due to a release of acetylcholine (ACh) from the parasympathetic nerve terminals that increases the permeability of the myocardial cell membrane for potassium ions (for review see ref. 1). This is accompanied by a shortening of the action potential duration in atrial muscle and a diminished calcium uptake2, which in turn results in a negative inotropic effect. Voltage clamp experiments in mammalian atrial muscle have shown that with higher concentrations of ACh not only is the potassium current augmented but also the slow inward current of calcium is reduced3. It is not clear how the c…
Functional characterization of two human olfactory receptors expressed in the baculovirus Sf9 insect cell system
2005
Olfactory receptors (ORs) are the largest member of the G-protein-coupled receptors which mediate early olfactory perception in discriminating among thousands of odorant molecules. Assigning odorous ligands to ORs is a prerequisite to gaining an understanding of the mechanisms of odorant recognition. The functional expression of ORs represents a critical step in addressing this issue. Due to limitations in heterologous expression, very few mammal ORs have been characterized, and so far only one is from human origin. Consequently, OR function still remains poorly understood, especially in humans, whose genome encodes a restricted chemosensory repertoire compared with most mammal species. In …
Integrin alpha 2 beta 1 promotes activation of protein phosphatase 2A and dephosphorylation of Akt and glycogen synthase kinase 3 beta.
2002
The integrins are a large family of heterodimeric transmembrane receptors composed of α and β subunits (22). In addition to mediating cell-matrix interactions, integrins have been shown to activate intracellular signaling pathways which, in collaboration with growth factor-induced signals, regulate cellular functions (46). Some integrin signaling cascades are activated via the β subunit cytoplasmic domain, and they are therefore triggered by several integrin heterodimers. These signals include the activation of protein tyrosine kinases of the Src and focal adhesion kinase (FAK) families (9, 47). More-recent studies have revealed signaling events that are activated specifically by an α subun…
β1D Integrin Inhibits Cell Cycle Progression in Normal Myoblasts and Fibroblasts
1998
Integrins are alphabeta heterodimeric transmembrane receptors involved in the regulation of cell growth and differentiation. The beta1 integrin subunit is widely expressed in vivo and is represented by four alternatively spliced cytoplasmic domain isoforms. beta1D is a muscle-specific variant of beta1 integrin and a predominant beta1 isoform in striated muscles. In the present study we showed that expression of the exogenous beta1D integrin in C2C12 myoblasts and NIH 3T3 or REF 52 fibroblasts inhibited cell proliferation. Unlike the case of the common beta1A isoform, adhesion of beta1D-transfected C2C12 myoblasts specifically via the expressed integrin did not activate mitogen-activated pro…
Increased gene expression of a cytokine-related molecule and profilin after activation of Suberites domuncula cells with xenogeneic sponge molecule(s)
2000
Porifera (sponges) constitute the lowest metazoan phylum, Experiments examined whether sponges can recognize self/nonself molecules. Cells from the marine sponge Suberites domuncula were incubated with membranes from either S. domuncula or another marine sponge, Geodia cydonium, as well as with recombinant alpha-integrin from G. cydonium. The cells responded immediately with a rise of intracellular Ca2+ ([Ca-i(2+)]) if they were treated with membranes from G. cydonium but not after treatment by those from S. domuncula. This change of [Ca-i(2+)] was also recorded with G. cydonium alpha-integrin. In parallel, the expression of two genes was strongly upregulated; one codes for a cytokine-relat…
Endothelial Nitric Oxide Synthase Regulates T Cell Receptor Signaling at the Immunological Synapse
2006
The role of nitric oxide (NO) in T cells remains controversial, and the origin and localization of endogenous NO and whether it regulates lymphocyte activation are unclear. We show here that, within minutes of binding to antigen, T cells produce NO via endothelial nitric oxide synthase (eNOS). This process required increased intracellular Ca2+ and phosphoinositide3-kinase activity. By using an eNOS-green fluorescent fusion protein and fluorescent probes to detect NO, we show that eNOS translocates with the Golgi apparatus to the immune synapse of T helper cells engaged with antigen-presenting cells (APC), where it was fully activated. Overexpression of eNOS prevented the central coalescence…