Disease relevance of Praxilene

• Daily treatment with three doses of naftidrofuryl (10, 15, and 22.5 mg/kg i.m.) modified some enzyme activities affected or unaffected by intermittent hypoxia and, particularly, decreased acetylcholinesterase activity [1].
• Papaverine and its derivatives (naftidrofuryl, viquidil, YC-93) decreased respiratory control, an effect that might correlate with their capacity to effect a vasodilatation of the cerebral vessels and their inefficacy in models of acute cerebral infarction [2].
• Effects of naftidrofuryl on breathlessness and exercise tolerance in chronic bronchitis [3].
• By maintaining an intact endothelium in vivo during ischemia, naftidrofuryl could prevent the further damage induced by leukocyte recruitment and activation [4].
• Twenty-four patients wth peripheral vascular disease unsuitable for surgery and suffering from ischaemic rest pain were treated equally with 14 days of bed rest and intravenous naftidrofuryl and their pain analogue scores and personality structures were analysed [5].

Psychiatry related information on Praxilene

• The efficacy of naftidrofuryl in patients with vascular or mixed dementia [6].
• After a wash-out period of four weeks 51 patients with mild to moderate senile dementia were treated with either 600 mg naftidrofuryl (n = 23) daily per os or placebo (n = 28) over an eight-week period [7].
• In the total study group, the naftidrofuryl group showed a significantly better improvement in the results of the psychometric test battery, which was the primary variable during treatment [7].
• Naftidrofuryl in the treatment of vascular dementia [8].
• This may be due to a correctional effect of naftidrofuryl on hemispatial neglect [9].

High impact information on Praxilene

• Indeed, naftidrofuryl potently inhibited the TNF-alpha-triggered increase of intercellular adhesion molecule-1 (ICAM-1) expression as well as stress fiber formation in human umbilical vein endothelial cells (HUVEC) [10].
• Importantly, it also highlights a novel NOS II-dependent mechanism of action for naftidrofuryl [10].
• Naftidrofuryl-driven regulation of endothelial ICAM-1 involves nitric oxide [10].
• Naftidrofuryl is a selective inhibitor of the 5-HT2 receptor expressed on human endothelial cells [10].
• Naftidrofuryl (20 mg/kg) exerted no effect on cerebral energy metabolism, but considerably reduced postischemic blood pressure (possibly thereby masking its ameliorative action) [11].

Chemical compound and disease context of Praxilene

• The present study was designed to determine whether naftidrofuryl oxalate (Naftidrofuryl) may exert a beneficial effect on the cerebral mitochondria after microsphere-induced embolism assessed under in vitro conditions [12].
• Effects of naftidrofuryl oxalate (naftidrofuryl) on neurotransmitter, acetylcholine, and amino acid content of brain regions following microsphere-induced cerebral embolism were examined to elucidate its possible therapeutic effects on ischemic brain [13].
• Pretreatment with naftidrofuryl or ketanserin prevented hippocampal CA1 neuronal loss after 5 min of transient ischemia [14].
• Serotonin, 5-HT2 receptors, and their blockade by naftidrofuryl: a targeted therapy of vascular diseases [15].
• Cost effectiveness of cilostazol compared with naftidrofuryl and pentoxifylline in the treatment of intermittent claudication in the UK [16].

Biological context of Praxilene

• Naftidrofuryl at the concentration of 3 microM elicited slight but significant restoration of the oxidative phosphorylation ability of the mildly injured mitochondria isolated from rats after the cerebral embolism, but not of the severely injured mitochondria [12].
• Treatment of naftidrofuryl resulted in an appreciable reverse of the brain glucose and glycogen levels and a substantial recovery of altered enzyme activities to normal levels in the Embden-Meyerhof pathway and tricarboxylic acid cycle.(ABSTRACT TRUNCATED AT 250 WORDS)[17]
• Bioanalyses and pharmacokinetics of nafronyl in the dog [18].
• Improved specific and sensitive reverse-phase HPLC assays of nafronyl (I) and its acidic metabolite and hydrolysis product (II) in biological fluids were developed with sensitivities of 3-6 ng/mL using fluorometric detection with 225 nm excitation and 330 nm emission wavelengths [18].
• A memory assessment technique for use in geriatric psychopharmacology: drug efficacy trial with naftidrofuryl [19].

Anatomical context of Praxilene

• In cases of vascular insufficiency within the inner ear, vasodilators such as carbon dioxide, papaverine, buphenine (nylidrin), naftidrofuryl (nafronyl) and thymoxamine have been recommended, but their true efficacy is questionable [20].
• Rat cortex synaptic and nonsynaptic mitochondria: enzymatic characterization and pharmacological effects of naftidrofuryl [21].
• The present study was designed to elucidate the possible beneficial effects of naftidrofuryl on ischemia-induced endothelium damage [4].
• Experiments were designed to determine the effects of the vasoactive drug naftidrofuryl on vascular smooth muscle, endothelial cells and adrenergic nerves in isolated canine blood vessels [22].
• Nine hundred microspheres (48 microns in diameter) were injected into the right internal carotid artery of rats, and changes in their behavior and energy metabolism of the cortex, striatum and hippocampus of both hemispheres were determined with and without naftidrofuryl treatment [23].

Associations of Praxilene with other chemical compounds

• Serotonin-induced contractility in human saphenous vein is inhibited by naftidrofuryl [24].
• Exposure of these mitochondria to 0.1 to 1 microM Naftidrofuryl significantly restored the succinate dehydrogenase activity [12].
• We investigated the effects of age and nafidrofuryl oxalate (Naftidrofuryl), a 5-HT2 antagonist, on neurotransmission and transduction systems in the gerbil hippocampus using quantitative autoradiography [25].
• Specific, sensitive, reversed-phase high-pressure liquid chromatographic assays of nafronyl (I) and its acidic metabolite and hydrolysis product (II) were developed in aqueous solutions and in biological fluids with sensitivities of 100 ng/ml using butacaine as the internal standard and spectrophotometric detection of 224 nm [26].
• The effects of naftidrofuryl (Praxilene) on exercise-induced tissue ischaemia was objectively assessed by continuously measuring the tcpO2 in 30 patients during three treadmill tests over a 3-month period in a randomized double-blind, placebo controlled, parallel group study [27].

Gene context of Praxilene

• Effect of endothelin-1 on human platelet shape change: reversal of activation by naftidrofuryl [28].
• On the other hand, the 5-HT2 antagonist naftidrofuryl failed to protect the brain tissue significantly against ischemic brain damage [29].
• Although no influence of naftidrofuryl on the rate of growth of neurites was observed, the drug enhanced the relative amount of the high molecular weight neurofilament subunit without affecting the concentration of a microtubule-associated protein, MAP2 [30].
• Recently, an additional mode of action of naftidrofuryl (i.e., mixed endothelin receptor antagonism) has been suggested [31].
• Naftidrofuryl significantly improved the physiological function of the liver cells as reflected by indocyanine green (ICG) clearance by the liver (t = 2.61; p less than or equal to 0.02) and also caused a larger fall in raised serum levels of gamma glutamyl transpeptidase (GGT) than did the placebo injections [32].

Analytical, diagnostic and therapeutic context of Praxilene

• 5. The results suggested that treatment with nafronyl improves or attenuates changes in monoamine neurotransmitter metabolism of the brain regions impaired by microsphere embolism [33].
• METHODS: This multicenter, randomized, double-blind study compared naftidrofuryl 600 mg/d with placebo for 1 year in patients with vascular or mixed dementia [34].
• When results of subgroups were analyzed according to the etiopathogenetic background of patients with SDAT, it was possible to show that naftidrofuryl affected psychopathometry and EEG-parameters while patients with MID responded to naftidrofuryl with changes in AGP score and EEG variables [7].
• In vivo effect of naftidrofuryl on 5-hydroxytryptamine-mediated constriction in rat peripheral microcirculation [35].
• Determination of naftidrofuryl in the plasma of humans by high-performance liquid chromatography [36].

References