Search results for "Isoprenaline"
showing 10 items of 48 documents
The relaxant effects of cromakalim (BRL 34915) on human isolated airway smooth muscle
1992
Cromakalim (BRL 34915) is a potassium channel opener with therapeutic potential as a bronchodilator in asthma. Cromakalim (0.1–30 μmol/l) inhibited the spontaneous tone of human isolated bronchi n a concentration-related manner being nearly as effective as isoprenaline or theophylline. The order of relaxant potencies (expressed as -log10 IC50 mol/l; mean ±SEM) was isoprenaline (7.29 ± 0.27; n = 8) > cromakalim (5.89 ± 0.12; n = 7) > theophylline (4.07 ±0.13; n = 10). In human bronchi where tone had been raised by addition of histamine (0.1 mmol/l), acetylcholine (0.1 mmol/l) or leukotriene D4 (LTD4, 0.1 μmol/l), the relaxant effect of cromakalim was substantially reduced. Cromakalim suppres…
Electrophysiologic and inotropic effects of alpha-adrenoceptor stimulation in human isolated atrial heart muscle.
1992
The effects of α-adrenoceptor stimulation on force of contraction were investigated in human atrial heart muscle and compared with those of β-adrenoceptor stimulation. The maximal positive inotropic effect produced by stimulation of α-adrenoceptors with phenylephrine (in the presence of atenolol 10 μmol/l) was significantly smaller than that seen in response to β-adrenoceptor stimulation with isoprenaline. The maximal effect of phenylephrine (25% of the maximal effect of isoprenaline) required far higher concentrations (1 mmol/l) than isoprenaline (100 nmol/l); the EC50 values amounted to 33.1 μmol/l and 3.3 nmol/l, respectively. In the presence of the α-adrenoceptor blocking agent phentola…
Adrenoceptor-mediated changes of action potential and force of contraction in human isolated ventricular heart muscle.
1988
Abstract 1. The effects of alpha-adrenoceptor stimulation on the action potential and force of contraction were investigated in human isolated ventricular heart muscle and compared with those of beta-adrenoceptor stimulation. 2. The maximal stimulation by isoprenaline of beta-adrenoceptors produced large changes in the force of contraction, which were accompanied by moderate increases in the height of the action potential. The maximal inotropic effect produced by stimulation of alpha-adrenoceptors with phenylephrine, in the presence of propranolol (1 mumol 1(-1)) was much smaller (about 10% of that seen in response to beta-adrenoceptor stimulation), and no significant changes of the action …
Opposite effects of beta-adrenoceptor stimulation and 8-bromo-cyclic AMP on potassium efflux in mammalian heart muscle.
1980
beta-adrenoceptor stimulation by isoprenaline increases the potassium efflux in beating guinea-pig atria. This effect is not mimicked by 8-bromo-cyclic AMP, a cyclic AMP analogue which exerts a positive inotropic effect in this preparation.
Electrical and mechanical activity of mammalian heart muscle fibres treated with papaverine
1977
The action of papaverine on electrical and mechanical activity was investigated in ventricular and atrial heart muscle fibres from guinea-pigs and cats. 1. Papaverine (10−5 M–5×10−5M) had positive, negative or no inotropic effects in ventricular preparations; positive inotropic effects were not observed after pretreatment of the animals with reserpine. In atrial preparations, papaverine (2×10−5M) had a positive inotropic effect that was independent of endogenously stored catecholamines. 2. The effects of isoprenaline and dibutyryl cyclic AMP were potentiated by papaverine (10−5 M–2×10−5M). 3. The action potential duration was always prolonged by papaverine in ventricular as well as in atria…
The response to isoproterenol of synaptic ribbon numbers in the rat pineal gland changes during postnatal development
1995
Abstract In the mammalian pineal gland synaptic ribbons (SRs) are dynamic organelles of pinealocytes undergoing a day/night rhythm, with small numbers during daytime and significantly higher numbers at night, similar to the formation of the pineal hormone melatonin. Whereas the day/night rhythm of melatonin synthesis is adrenergically regulated, data on the adrenergic regulation of SR numbers in the rat pineal gland are at variance. While some authors have demonstrated that isoproterenol (ISO) stimulates SR numbers, others could not find any effect. To clarify the issue, we carried out identical experiments in two age groups. It was found that in male Sprague-Dawley rats, administration of …
STIMULATION OF ?1-ADRENOCEPTORS ENHANCES ELECTRICALLY EVOKED [3H]-ACETYLCHOLINE RELEASE FROM RAT PHRENIC NERVE
1990
1. The effects of isoprenaline, noradrenaline and fenoterol on the electrically evoked release of [3H]-acetylcholine from the rat phrenic nerve were investigated. 2. Isoprenaline (0.1 mumol/L) and noradrenaline (1 mumol/L) enhanced evoked [3H]-acetylcholine release by about 90%, an effect which was abolished by CGP 20712A (0.1 mumol/L), a specific antagonist at beta 1-adrenoceptors. Noradrenaline still enhanced [3H]-acetylcholine release in the presence of phentolamine (1 mumol/L). 3. The enhancing effect of both isoprenaline and noradrenaline decreased at prolonged exposure times (24-32 min). A pre-exposure of the tissue to a low concentration (0.01 mumol/L) of isoprenaline prevented the e…
Functional role of cholinoceptors and purinoceptors in human isolated atrial and ventricular heart muscle
1989
1. The effects of cholinergic and purinergic stimulation on action potential, force of contraction and 86Rb efflux were investigated in human atrial and ventricular heart muscle. 2. In atrial heart muscle, carbachol and (-)-N6-(R-phenyl-isopropyl)-adenosine (R-PIA) and 5'-(N-ethyl)-carboxamido-adenosine (NECA) evoked transient decreases of action potential duration and force of contraction; the steady-state effects on force of contraction were virtually identical to control values. In the presence of propranolol, steady-state values after carbachol, R-PIA or NECA amounted to about 50% of control values. 3. In ventricular heart muscle, carbachol, NECA and R-PIA did not significantly affect t…
The nicardipine-isoprenaline interaction in human and guinea-pig isolated airways
1994
Summary— The effects of the dihydropyridine calcium antagonist nicardipine on the concentration-response curves of relaxant compounds acting through the adenylate-cyclase/cAMP system (isoprenaline, forskolin, adenosine and theophylline) or by the cGMP pathway (sodium nitroprusside) were studied on human isolated bronchus and guinea-pig isolated trachea. These effects were compared with those of nifedipine (a dihydropyridine derivative) and theophylline (a non-selective phosphodiesterase inhibitor). Nicardipine, in the range of 0.01 to 1 μM, significantly potentiated the relaxant effects of isoprenaline, forskolin, adenosine and theophylline, whereas the effects of sodium nitroprusside were …
Adrenergic modulation of the release of 5-hydroxytryptamine from the vascularly perfused ileum of the guinea-pig
1988
1. Isolated segments of the guinea-pig ileum were vascularly perfused and the release of 5-hydroxytryptamine (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) into the portal venous effluent was determined by h.p.l.c. with electrochemical detection. Test substances were applied via the arterial perfusion medium. 2. Isoprenaline (0.1 microM) increased the outflow of 5-HT and 5-HIAA maximally by about 75% and this was antagonized by propranolol (0.1 microM). Forskolin (1-10 microM) increased the outflow of 5-HT by approximately 105% and that of 5-HIAA by approximately 55%. The phosphodiesterase inhibitor AH 21-132 (0.1-1 microM) increased the outflow of 5-HT and 5-HIAA by about 70%. Isoprenaline…