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At least 19 recordsLinked to original sources

The effect of trifluperidol on the contractile response of guinea-pig taenia coli to acetylcholine, histamine, potassium and calcium.

In guinea-pig taenia coli, trifluperidol antagonized the contraction induced by all agonists tested in a non-competitive manner. pA2 values for trifluperidol calculated for acetylcholine, histamine and calcium were not different. pD'2 values for trifluperidol calculated for acetylcholine, histamine and potassium did not differ, while the pD'2 for acetylcholine and calcium were significantly different. pD'2 values for trifluperidol calculated for calcium varied with the concentration of the antagonist. Trifluperidol has been considered a non-specific blocking agent in guinea-pig taenia coli. This inhibitory activity has been considered very similar to that of local anaesthetic agents, although calcium was blocked in a non-competitive manner by trifluperidol, differently from anaesthetic agents that block calcium in a competitive way.

Acetylcholine↗

Effects of beta adrenergic blocking drugs and trifluperidol on intestinal motility and splanchnic nerve activity in cats.

In cats anaesthetized with chloralose and urethane we studied the effect of the selective beta 1 adrenergic blocking practolol and the non-selective beta 1-2 adrenergic blocking pindolol on the intestinal motility, the efferent sympathetic activity, arterial blood pressure and heart-rate. We compared the effects of trifluperidol on the intestinal tone, the intestinal motility and its duration with those of trifluperidol and practolol combined. It was found that 1-, 2-, and 3 mg/kg of practolol given intravenously had no influence on the spontaneous electric activity of postganglionic fibres of the splanchnic or hypogastric nerves, thus it had no central effect. Accordingly, its site of effect proved to be peripheric. Its administration was associated with a slight decrease of the arterial blood pressure and heart rate. The intestinal tone was instantly increased depending on the does in every case. In two-thirds of our experiments the intestinal motility was restored 1 to 3 minutes following administration depending on the dose. Combined with trifluperidol, practolol produces a further increase in the enhancing activity of trifluperidol on the intestinal tone and motility. It considerably extends the duration of the action of trifluperidol on the intestinal motility. Pindolol increases the intestinal tone and motility dose-dependently in every case, reduces the efferent sympathetic activity, which is inversely proportional to the dose. The action is most pronounced on administration of 0.125 micrograms/kg of pindolol intravenously but it cannot be observed with a dose of 0.5 mg/kg. No significant changes were observed in blood pressure but there was a reduction in heart rate. The action of pindolol is supposed to be both central and peripheral in nature.

Animals↗

Flupentixol and trifluperidol reduce secretion of tumor necrosis factor-alpha and nitric oxide by rat microglial cells.

Tumor necrosis factor-alpha (TNF-alpha) and nitric oxide (NO), both of which are produced by activated microglial cells, are involved in the neuropathogenesis of many diseases affecting the central nervous system (CNS). There is a need to develop drugs that inhibit neurotoxic processes in neurodegenerative diseases. The aim of this study was to evaluate the effect of two neuroleptics, flupentixol and trifluperidol, on the release of pro-apoptotic TNF-alpha and NO by LPS-activated rat microglial cells. Flupentixol and trifluperidol reduced the TNF-alpha and NO release by cultured microglia exposed to LPS for 6 and 24h. The results suggest that flupentixol and trifluperidol, which are well-known antipsychotic drugs, may be used in the treatment of CNS diseases associated with excessive TNF-alpha and NO release.

Animals↗

Characterization of haloperidol and trifluperidol as subtype-selective N-methyl-D-aspartate (NMDA) receptor antagonists using [3H]TCP and [3H]ifenprodil binding in rat brain membranes.

[3H]TCP and [3H]ifenprodil binding to N-methyl-D-aspartate (NMDA) receptors in rat forebrain membranes was used to compare the inhibition of haloperidol and trifluperidol with that of ifenprodil and eliprodil. In the [3H]TCP binding assay, inhibition curves of ifenprodil, eliprodil, haloperidol and trifluperidol revealed two affinity states in the presence of glutamate, glycine and spermidine. The potency of these agents to inhibit the high-affinity fraction of the binding agreed with the results of other studies investigating their potency to block glutamate-induced current at recombinant NR1a/NR2B NMDA receptors expressed in Xenopus oocytes. These agents also inhibited [3H]ifenprodil binding in a biphasic manner, whether in the absence or the presence of either the sigma site ligand GBR-12909 or spermidine. Spermidine reduced the fraction of high-affinity sites labeled with [3H]ifenprodil. The only alteration in the affinity was a decrease in the IC50 value of haloperidol to inhibit the high-affinity fraction of [3H]ifenprodil binding. GBR-12909 also reduced the fraction of [3H]ifenprodil sites inhibited by these compounds with high affinity, with no change in the affinity for either fraction. These data suggest that spermidine is neither a competitive antagonist at the fraction of the binding inhibited by these agents with high affinity, nor is this fraction of the binding to sigma sites. Haloperidol and trifluperidol represent a new class of agent that interacts at a site that is labeled by [3H]ifenprodil as well as [3H]TCP in rat brain membranes and that closely reflects ifenprodil's voltage-independent site on the recombinant NR1a/NR2B subtype of the NMDA receptor.

Animals↗

Persistent cerebellar deterioration in a patient with lobar pneumonia under lithium, carbamazepine, and trifluperidol treatment.

We report on a patient with schizoaffective disorder who was on combination therapy of lithium, carbamazepine, and the neuroleptic trifluperidol. He experienced a lobar pneumonia and developed an acute and persistent cerebellar deterioration which was most likely due to lithium toxicity, while the serum lithium level was within the therapeutic range. The combination of lithium, carbamazepine, and neuroleptics is common, and is generally considered to be safe. The reported case suggests that this regimen might increase the risk of intoxication with potentially disabling side-effects.

Anti-Bacterial Agents↗

Effects of the hypocholesteremic agent trifluperidol on the sterol, steryl ester, and fatty acid metabolism of Saccharomyces cerevisiae.

Trifluperidol (TFP), at a concentration of 100 muM, inhibited the 24-h growth of Saccharomyces cerevisiae by about 30%. Effects on lipid metabolism were investigated by monitoring the incorporation of [1-14C]sodium acetate into various lipid fractions after 4 and 24 h of growth in the presence of several concentrations of TFP. Although little effect was noted on the amount of free sterols, 24-h incorporation of label into steryl esters was increased two- to fourfold by 100 muM TFP. Major sterol components of the steryl ester fraction isolated from an untreated culture were zymosterol (48%) and ergosterol (24%), whereas from the TFP-treated culture delta8,24(28)-ergostadienol (66.6%) and delta8-ergostenol (14.7%) were most abundant. Free sterols present in the highest concentration in the untreated culture were ergosterol (78.2%) and lanosterol (13%); whereas delta8,22-ergostadienol (38.5%), delta8-ergostenol (35.4%), and delta8,24(28)-ergostadienol (25.4%) were the most abundant free sterols obtained from the TFP-treated culture. Thus, the major block in the sterol biosynthetic pathway in yeast appears to be delta8 leads to delta7 isomerization. In these same cultures the relative amounts of C12 and C14 acids isolated from both steryl ester and miscellaneous lipid fractions were increased more than threefold over controls.

Anticholesteremic Agents↗

Neuroleptic malignant syndrome with trifluperidol.

In a case of NMS subsequent to administration of trifluperidol to a young man, the patient responded remarkably quickly to bromocriptine. The authors point out the deficiencies in the diagnostic criteria, which need further refinement for a better understanding of the syndrome.

Adult↗