Search results for "RAPA"
showing 10 items of 471 documents
Effect of verapamil and diltiazem on isolated gastro-oesophageal sphincter of the rat
1985
Abstract The effect of verapamil and diltiazem on the contraction induced by agonists on the rat lower oesophageal sphincter in-vitro has been studied. Both calcium entry blockers inhibited the contractile response to acetylcholine, carbachol and KCl. The potency of the inhibitory action was diltiazem > verapamil. The results give substance to the use of calcium entry blockers in the treatment of oesophageal spasm.
Effects of Ca2+ channel antagonists in guinea-pig normal and skinned gall bladder.
1993
CaCl2 (0.01-50 mM, in K(+)-depolarized tissues), KCl (0.1-100 mM) and acetylcholine (1 nM-10 mM) produced concentration-dependent contractions of guinea-pig isolated gall bladder. Nifedipine (1-100 microM), verapamil (1-100 microM), diltiazem (1-100 microM), cinnarizine (1-100 microM), and flunarizine (1-100 microM) each produced a concentration-related inhibition of the log concentration-effect curve for CaCl2. The rank order of potencies of these antagonists, measured as the IC50 against Ca2+ (50 mM)-induced contraction of depolarized gall bladder, was diltiazem (0.25 microM)or = verapamil (0.8 microM) approximately nifedipine (1.2 microM)cinnarizine (25 microM) approximately flunarizine …
Calcium dependence of the contraction produced by endothelin (ET-1) in isolated guinea-pig trachea.
1990
Endothelin (ET-1, 1 pM to 0.1 microM) produced a concentration-dependent contraction of isolated guinea-pig trachea. BAY K 8644 (1 microM) did not significantly alter the concentration-response curve for ET-1. Incubation with nicardipine (10 microM) partly inhibited responses to low concentrations (10 pM to 1 nM) of ET-1 while verapamil (10 microM) and diltiazem (10 microM) were ineffective. La3+ (10 microM) and Cd2+ (10 microM) preferentially depressed the responses evoked by high concentrations (30 nM-0.1 microM) of ET-1 without affecting the responses evoked by low concentrations of the peptide. Incubation in Ca2(+)-free (with EDTA, 1 mM) medium resulted in suppression of the responses e…
The influence of active secretion processes on intestinal absorption of salbutamol in the rat.
2001
Abstract Salbutamol was perfused in the small intestine of rat using a standard rat gut ‘in situ’ preparation: (1) in inhibitor-free solution at seven different concentrations (0.15, 0.29, 1.20, 5.0, 9.0, 13.0 and 18.0 mM); (2) at a 0.29 mM concentration – thought to be close to the allometric dose in man – in the presence of a non-specific enzyme inhibitor, sodium azide (0.3, 3.0 and 6.0 mM); and (3) at 0.29 mM in the presence of a selective secretion inhibitor, verapamil (10.0 and 20.0 mM). In free solution, the mixed-order rate constants, k ′ a , of salbutamol increase as the solute concentration increases until an apparent asymptotic value is reached. This could be due to the saturation…
Effects of calcium channel blockers on gastric emptying and acid secretion of the rat in vivo.
1986
Abstract Experiments were designed to evaluate the effects of three calcium channel blockers (verapamil, diltiazem and cinnarizine) on gastric emptying and secretion in the rat. Pretreatment with the calcium blockers delayed gastric emptying of phenol red in a dose-dependent manner. Verapamil was the most effective of the agents tested. Verapamil and diltiazem inhibited gastric acid secretion in the pylorus-ligated rat without affecting pepsin output. Cinnarizine was ineffective in this model. When the perfused lumen of the anaesthetized rat was used, verapamil was found to inhibit responses to carbachol or histamine more than those to pentagastrin. Further, we found a greater sensitivity t…
Differential Effects of Verapamil on Various Gastric Lesions in Rats
1988
Verapamil (3, 10, 20 mg/kg-1) increases the necrotizing effects of oral 25% NaCl or 100% ethanol. Damage by 0.6 N HCl was not equally affected since 1 mg/kg-1 of verapamil decreased the ulcer index whereas the higher doses augmented it. Pharmacologically induced gastric lesions were also differently affected by verapamil, ulcers produced by histamine being greatly enhanced and those of reserpine inhibited. Neither indomethacin nor compound 48/80 ulcers were modified. These results suggest that verapamil modifies the susceptibility of the gastric mucosa to damage.
Effects of low temperature and pharmacological interventions on the responses of the isolated guinea-pig trachea
1992
Cooling the guinea-pig isolated trachea from 37°C to 20°C virtually abolished the response to CaCl2 (in K+-depolarized tissues) and depressed that to histamine (about 75% reduction), KCl and 5-hydroxytryptamine (around 50% inhibition) while the response to acetylcholine remained unaffected. A further cooling to 10°C was necessary to inhibit acetylcholine-induced contractions. Hyporesponsiveness to spasmogens by cooling was not associated with subsensitivity (increased EC50) except for 5-hydroxytryptamine. Contractile responses to KCl (50 mmol/l), histamine (1 mmol/l) and 5-hydroxytryptamine (0.1 mmol/l) in a Ca2+-free EGTA (0.1 mmol/l)-containing solution were inhibited by cooling to 20°C b…
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…