Search results for "Verapamil"
showing 10 items of 68 documents
Evidence for the neuronal origin of immunoreactive interleukin-1 beta released by rat hypothalamic explants.
1996
In this study, we have investigated the release of immunoreactive interleukin-1 beta (irIL-1 beta) from the rat hypothalamus in vitro. It was found that (1) tissue explants release sizable amounts of irIL-1 beta (ranging from 0.43 to 0.52 pg/mg of wet tissue) in 20 min incubations; (2) basal release in significantly increased by depolarization induced with 56 mM KCl; (3) K(+)-induced irIL-1 beta release is inhibited by the specific blocker of N-type calcium channels, omega-conotoxin, and by verapamil, but not by nifedipine; (4) K(+)-induced release is also inhibited by the Na+ channel blockers tetrodotoxin and lidocaine; (5) irIL-1 beta release is significantly increased by noradrenalin; su…
The effects of phorbol 12,13-diacetate on responses of guinea-pig isolated trachea to methylxanthines, isoprenaline and ryanodine
1994
1. Using guinea-pig isolated trachea, we have studied how phorbol 12,13-diacetate (PDA) modulates mechanical responses of the tissue to methylxanthines, isoprenaline and ryanodine. 2. Caffeine (10 microM-5 mM), theophylline (10 microM-5 mM) and isoprenaline (1 nM-1 microM), each inhibited the spontaneous tone of the trachea. Pretreatment with PDA (0.1-10 microM) converted relaxant responses to high concentrations of the methylxanthines into contractions. PDA produced no equivalent effect against isoprenaline. Pretreatment with verapamil (1 or 10 microM), nifedipine (0.1 microM) or incubation with Ca(2+)-free, EGTA (0.1 mM)-containing physiological salt solution (PSS) suppressed the contract…
Differential effects of calcium channel antagonists (omega-conotoxin GVIA, nifedipine, verapamil) on the electrically-evoked release of [3H]acetylcho…
1990
Electrically-evoked release of [3H]acetylcholine from autonomic neurons (myenteric plexus), motoneurons (phrenic nerve) and the central nervous system (neocortex) was investigated in the presence and absence of the calcium channel antagonists omega-conotoxin GVIA, nifedipine and verapamil, whereby the same species (rat) was used in all experiments. Release of [3H]acetylcholine was measured after incubation of the tissue with [3H]choline. omega-Conotoxin GVIA markedly reduced (70%) the evoked release of [3H]acetylcholine from the myenteric plexus of the small intestine (IC50: 0.7 nmol/l) with a similar potency at 3 and 10 Hz stimulation. An increase in the extracellular calcium concentration…
EFFECTS OF VANADATE ON RESPONSES OF GUINEA-PIG ISOLATED TRACHEA TO SPASMOGENS
1993
Abstract The effects of vanadate on the contractility of the guinea-pig isolated trachea was examined. Vanadate (0·1 Mm) produced a sustained contraction that was abolished in Ca2+-free EGTA (0·1 Mm)-containing physiological salt solution but was resistant to verapamil (1 μm). Vanadate (0·1 Mm) depressed tracheal responses to CaCl2 (in Ca2+-free depolarizing solution), KCl, acetylcholine, histamine and 5-hydroxytryptamine. For vanadate (10 μm), the inhibition of spasmogenic responses only reached statistical significance for histamine and 5-hydroxytryptamine. Caffeine (1 Mm)-induced spasm (trachea at 20°C in the presence of indomethacin (2·8 μm)) was not affected by vanadate (10 μm-0·1 Mm).…
EFFECTS OF PHORBOL 12,13-DIACETATE AND ITS INFLUENCE ON SPASMOGENIC RESPONSES IN NORMAL AND SENSITIZED GUINEA-PIG TRACHEA
1995
Abstract We have studied the effects of phorbol 12,13-diacetate (PDA) and its influence on a variety of spasmogenic responses in trachea isolated in from normal and sensitized guinea-pigs. Tracheal preparations were denuded of epithelium, treated with indomethacin (2·8 μm), and cooled to 20°C. In these experimental conditions, tracheal strips contracted to PDA (0·1 nm-1 μm). Contractions to PDA (1 μm) were greater in sensitized tissues. In normal trachea, contractions to PDA (0·1 μm) were depressed by H-7, 1-(5-isoquinolinyl-sulphonyl)-2-methylpiperazine, (50 μm), amiloride (10 μm), verapamil (10 μm) and Ca2+-free exposure. Similar effects were obtained in sensitized trachea except that PDA…
COMPARATIVE STUDY ON THE ELECTROPHYSIOLOGICAL EFFECTS OF MONENSIN ON ATRIAL AND VENTRICULAR MUSCLE PREPARATIONS OF GUINEA-PIG HEART
1995
The effects of monensin (10 µmol/L) alone and in presence of verapamil (3 µmol/L) or ouabuin (1 µmol/L) or glibenclamide (10 µmol/L) or BaCl2 separately were studied on the electrophysiological properties represented by force of contraction, duration of action potential, and membrane resting potential of isolated atrial and ventricular muscle of guinea –pig heart. Monensin induced a transient increase in the force of contraction of atrial and ventricular muscles. It caused a decrease in action potential duration of papillary muscle, this effect was reversed by glibenclamide. Monensin increased the action potential duration of atrial muscle in absence or presence of glibenclamide. In presenc…
Specific suppression of pentylenetetrazol-induced epileptiform discharges in CA3 neurons (hippocampal slice, guinea pig) by the organic calcium antag…
1989
Antiepileptic actions of the organic calcium antagonists flunarizine (cinnarizine derivate) and verapamil (papaverin derivat) on pentylenetetrazol-induced epileptic bioelectric activity were tested in CA3 neurones of hippocampal slices. In all experiments both calcium antagonists reduced the amplitudes and/or durations of paroxysmal depolarizations as well as their rate of occurrence, when the bath concentrations of flunarizine or verapamil exceeded 20 mumol/l. When they were added to the bath solution before pentylenetetrazol application, recordings of the resting membrane potential, of the membrane resistance, of action potentials and of spontaneous as well as of evoked excitatory and inh…
Cytotoxicity of Novel Sulfanilamides Towards Sensitive and Multidrugresistant Leukemia Cells
2014
Novel sulfa Schiff bases were synthesized and characterized by a reaction between aromatic sulfonamides and aromatic aldehydes or heterocyclic ketones in equimolar ratios. Their cytotoxicity was evaluated by the resazurin assay towards human sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemia cells. Three of the tested compounds viz., 4-(anthracen-9-ylmethyleneamino)-N-(pyrimidin-2-yl)benzenesulfonamide (4), 4-(anthracen-9- ylmethyleneamino)benzenesulfonamide, (5) and 4-((3-phenylallylidene)amino)benzene-sulfonamide, (6) were cytotoxic (IC 50 values: 5.38-19.96 µM). CEM/ADR5000 cells were not cross-resistant to these compounds, indicating activity against otherwise drug-resistan…
Effects of Ca2+ entry blockers on CaCl2-, KCl- and noradrenaline-induced contractions of goat cerebral arteries
1990
Abstract The effects of three Ca 2+ entry blockers, nicardipine, nimodipine and verapamil, on CaCl 2 -, KCl- and noradrenaline-induced contractions were examined in isolated goat middle cerebral artery. The relationship between the effects of Ca 2+ entry blockers and the extracellular Ca 2+ dependence of the contractions was also examined. In ‘nominally’ Ca 2+ -free medium, addition of CaCl 2 induced concentration-dependent contractions of previously depolarized arteries. Withdrawal of Ca 2+ from the extracellular medium caused strong inhibition of the KCl- and noradrenaline-induced arterial contractions. Addition of EGTA to the Ca 2+ -free medium almost abolished the noradrenaline-response…