Abstract:
:Trigeminal stimulation of C-fibers increased c-fos expression within the trigeminal nucleus caudalis (NtV) and thalamic neuronal activity which both reflect the transmission of a nociceptive message. We examined the effects on both these phenomena of the selective NK1 and NK2 receptor antagonists, SR140333 and SR48968. SR140333 (0.3, 1 and 3 micrograms/kg intravenously [i.v.]) dose-dependently, reversibly and stereoselectively antagonized the increase of contralateral thalamic activity. This compound, when given i.v. (30 micrograms/kg) or orally (10 mg/kg), also reduced the number of Fos-like immunoreactive cells particularly at the medial and caudal level of the NtV. In contrast, SR48968 did not exert any antagonistic effect either on thalamic activity or on Fos-like immunoreactivity. The data strongly suggest a preferential involvement of NK1 vs NK2 receptors in nociceptive transmission following trigeminal ganglion stimulation. Taken together, our results indicate that SR140333 could provide a potent drug for the relief of pain occurring under excessive activity of sensory trigeminal fibers.
journal_name
Fundam Clin Pharmacoljournal_title
Fundamental & clinical pharmacologyauthors
Michaud JC,Alonso R,Gueudet C,Fournier M,Calassi R,Brelière JC,Le Fur G,Soubrié Pdoi
10.1111/j.1472-8206.1998.tb00929.xsubject
Has Abstractpub_date
1998-01-01 00:00:00pages
88-94issue
1eissn
0767-3981issn
1472-8206pii
S0767398198802338journal_volume
12pub_type
杂志文章abstract::HMG CoA reductase inhibitors (statins) have an established place in the treatment of coronary artery disease. However, their role in the treatment of heart failure (HF), including HF due to coronary artery disease, has been controversial since beneficial as well as possible harmful effects may occur. Several recent st...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.2007.00538.x
更新日期:2007-11-01 00:00:00
abstract::The effects of cooling (to 28 degrees C) and warming (to 41 degrees C) on the vasoconstrictions induced by 5-hydroxytryptamine (5-HT) and acetylcholine (ACh) and the role of nitric oxide in these effects were analyzed in human umbilical artery and vein. 5-HT (10(-9)-10(-4) M) and ACh (10(-9)-10(-4) M) induced concentr...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2007.00562.x
更新日期:2008-02-01 00:00:00
abstract::ATP-Binding Cassette transporters such as ABCG2 confer resistance to various anticancer drugs including irinotecan and its active metabolite, SN38. Early quantitative evaluation of efflux transporter inhibitors-cytotoxic combination requires quantitative drug-disease models. A proof-of-concept study has been carried o...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12005
更新日期:2014-04-01 00:00:00
abstract::Free radical species have been implicated as important agents involved in myocardial ischemic and reperfusion injuries. Superoxide is capable of mobilizing iron from ferritin and the released iron can cause hydroxyl formation from H2O2. The aim of this study was to evaluate the time-dependent increase in lipid peroxid...
journal_title:Fundamental & clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1111/j.1472-8206.1998.tb00947.x
更新日期:1998-01-01 00:00:00
abstract::Cicletanine, a racemic furopyridine derivative synthesized as racemate, is used as an antihypertensive agent. Its two enantiomers are involved in the pharmacological effects of the drug. Cicletanine is metabolized by conjugation enzyme systems (phase II) into sulfoconjugated or glucuroconjugated enantiomers. As oxazep...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1999.tb00363.x
更新日期:1999-01-01 00:00:00
abstract::We have studied the effects of neurotensin (NT) on the release of [3H]dopamine ([3H]DA) evoked by terminal depolarization with either K+, veratridine or 4-aminopyridine (4-AP). NT (1-1000 nM) induced a net potentiation (up to 170%) of the K+ (25 mM)-evoked release of [3H]DA. The capacity of NT to potentiate the effect...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1993.tb00224.x
更新日期:1993-01-01 00:00:00
abstract::Although nisoxetine has been shown to elicit cutaneous (peripheral) anesthesia, spinal (central) anesthesia with nisoxetine was not exposed. The aim of this study was to examine spinal anesthesia of nisoxetine and its influence on the antinociceptive action of mepivacaine. We compared nisoxetine with an established lo...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2012.01070.x
更新日期:2014-02-01 00:00:00
abstract::Cyclo-oxygenase (COX) has been reported to play a significant role in neurodegeneration and other brain-related disorders. Recent studies have reported that COX plays a significant role in the pathophysiology of brain-related disorders and COX-2 inhibitors could be useful drug therapy in neurodegenerative disorders. T...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2006.00398.x
更新日期:2006-06-01 00:00:00
abstract::Ivermectin, a parasiticide that long ago proved its worth in veterinary medicine, became one of the most effective tools for control programs against human filarial diseases in the 1980s. It is provided at no cost, is effective against microfilariae (blocking their transmission) and can be administered annually as a s...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1046/j.1472-8206.2003.00170.x
更新日期:2003-04-01 00:00:00
abstract::Interferon (IFN)-γ is known to downregulate expression of drug detoxifying proteins such as cytochromes P-450 (CYPs) in human hepatocytes. The present study was designed to determine whether IFN-γ may also impair expression of influx and efflux drug transporters, which constitute important determinants of the liver de...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2010.00822.x
更新日期:2011-02-01 00:00:00
abstract::The poor outcomes in advanced non-small-cell lung cancer (NSCLC) necessitate new treatments. Recent studies emphasize anisomycin as a promising anti-cancer drug candidate. In this work, we systematically investigated the efficacy of anisomycin alone and its combination with the standard-of-care drugs in NSCLC. We show...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12641
更新日期:2020-12-18 00:00:00
abstract::A meta-analysis was performed on the results of clinical trials of buflomedil in intermittent claudication. The analysis used results from 744 patients enrolled in ten studies, conducted at 42 centers in seven countries. All studies were randomized, double-blind, placebo-controlled trials which measured improvement in...
journal_title:Fundamental & clinical pharmacology
pub_type: 临床试验,杂志文章,meta分析
doi:10.1111/j.1472-8206.1995.tb00515.x
更新日期:1995-01-01 00:00:00
abstract::The hypotensive and negative chronotropic effects of 5 calcium entry blockers (verapamil 200 micrograms/kg IV; diltiazem 300 micrograms/kg IV; nifedipine 5 micrograms/kg IV; nicardipine 50 micrograms/kg IV; and bepridil 5 mg/kg IV) were compared in control normotensive and acute neurogenic hypertensive anaesthetized d...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1987.tb00548.x
更新日期:1987-01-01 00:00:00
abstract::Amitriptyline significantly inhibited alcohol, aspirin, indomethacin and cold-restraint stress-induced ulceration. Secretory studies conducted in pyloric-ligated rats revealed that the drug, at the doses employed, significantly reduced total acidity and protein content. However, significant reductions of the gastric v...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1046/j.1472-8206.2002.00092.x
更新日期:2002-08-01 00:00:00
abstract::Quercetin is a flavonol polyphenol widely found in many vegetables, grains, and fruits. Quercetin has been shown to inhibit proliferation and invasion of various glioma cells and is regarded as a potential anticancer agent against glioma. However, whether and how this drug could affect brain blood vessels and endothel...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12514
更新日期:2020-04-01 00:00:00
abstract::Pyroglutamic acid (PCA) was compared with placebo in a randomized, double blind trial for assessing its efficacy in treating memory deficits in 40 aged subjects. Twenty subjects were treated with PCA and 20 with placebo over a period of 60 d. Memory functions were evaluated at baseline and after 60 d of treatment by m...
journal_title:Fundamental & clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1111/j.1472-8206.1990.tb00485.x
更新日期:1990-01-01 00:00:00
abstract::Overdose cardiac effects of imipramine are due to fast Na channel blockade and are clinically reversed by administration of sodium lactate which induces alkalosis (about pH 7.50) and hypernatremia (about 8 mM). The mechanisms of this beneficial effect of Na lactate were explored in vitro on guinea-pig ventricular myoc...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1992.tb00102.x
更新日期:1992-01-01 00:00:00
abstract::The aim of this review is to comment the results described in the literature concerning the possible pharmacodynamic mechanisms involved in the improvement of quality of life of angiotensin converting enzyme inhibitors that is just a working hypothesis. These drugs, widely used in the treatment of hypertension, preven...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.1996.tb00592.x
更新日期:1996-01-01 00:00:00
abstract::Over the past 10 years, more than 40 potentially oncogenic genes, termed protooncogenes, have been identified in the human genome. Little is known of the physiological role of the proteins encoded by these genes, but they seem to be involved in the reception and transmission of hormonal and other environmental informa...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.1990.tb00694.x
更新日期:1990-01-01 00:00:00
abstract::Dapsone-induced agranulocytosis is a rare but potentially fatal adverse drug reaction (ADR). A 45-year-old male Caucasian patient developed agranulocytosis caused by dapsone (diamino-diphenyl sulfone), which he was prescribed for leukocytoclastic vasculitis. Patient's treatment consisted of termination of dapsone, ant...
journal_title:Fundamental & clinical pharmacology
pub_type:
doi:10.1111/fcp.12287
更新日期:2017-10-01 00:00:00
abstract::In addition to their direct effects on cardiac contractility, a number of positive inotropic agents also induce, through direct peripheral vasodilation, a reduction in afterload which is of major importance in their beneficial effects in the treatment of congestive heart failure. However, the induced increase in cardi...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1991.tb00759.x
更新日期:1991-01-01 00:00:00
abstract::A number of antiplatelet drugs, principally aspirin alone or in combination, have been evaluated in randomized trials of survivors of prior occlusive vascular disease events or of individuals at high risk because of multiple cardiovascular risk factors. In this meta-analysis we compare single and dual antiplatelet reg...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,meta分析
doi:10.1111/j.1472-8206.2008.00582.x
更新日期:2008-06-01 00:00:00
abstract::The effects of CGP 37849 [DL-(E)-2-amino-4-methyl-5-phosphono-3-pentenoate] and its ethylester CGP 39551 on whole-cell currents evoked by the endogenous excitatory amino acids, L-glutamate and L-aspartate, were studied in cultured mouse spinal cord neurones. Although CGP 37849 was the more potent compound, both antago...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1999.tb00322.x
更新日期:1999-01-01 00:00:00
abstract::Ponsinomycin is a new macrolide antibiotic. Its effect on DHE pharmacokinetics was investigated in this study. Twelve young healthy volunteers received a single 9 mg oral dose of DHE before and on the 8th day of treatment (800 mg twice daily) with ponsinomycin. DHE was assayed in plasma by RIA. Because of low plasma l...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1991.tb00700.x
更新日期:1991-01-01 00:00:00
abstract::Since patients may report spontaneously adverse events associated with their medications, such notifications are constantly on the rise. In 2017, an unexpected rise of notifications associated with the marketing of a new formula of Levothyrox, differing from the 30-year-old drug only by minor elements, occurred in Fra...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12446
更新日期:2019-08-01 00:00:00
abstract::Drug-drug interactions (DDIs) between antihypertensive drugs and non-steroidal anti-inflammatory drugs (NSAIDs) can lead to adverse drug reactions (ADRs). Guidelines are available to help prescribers deal with these drug associations, but their implementation is not well evaluated. The aims of this study were to asses...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12014
更新日期:2014-04-01 00:00:00
abstract::This paper reviews state-of-art statistical designs for dose-escalation procedures in first-into-man studies. The main focus will be on studies in oncology, as most statistical procedures for phase I trials have been proposed in this context. Extensions to situations such as the observation of bivariate outcomes and h...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.2004.00226.x
更新日期:2004-06-01 00:00:00
abstract::The blood-brain barrier (BBB) is responsible for the control of solutes' concentration in the brain. Tight junctions and multiple ATP-binding cassette (ABC) and SoLute Carrier (SLC) efflux transporters protect brain cells from xenobiotics, therefore reducing brain exposure to intentionally administered drugs. In epile...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12175
更新日期:2016-04-01 00:00:00
abstract::Endocannabinoid system has attracted the researchers to investigate into its ever fascinating roles governing many of the physiological functions in the human body. The prime endogenous cannabinoids are arachidonoylethanolamide also called anandamide and 2-arachidonoylglycerol. Recent pharmacological advances point ou...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.2006.00454.x
更新日期:2007-02-01 00:00:00
abstract::The aim of our study was to analyse the protective effects of different alpha-tocopherol analogues 1) against fibrillations induced by an ischemia-reperfusion sequence, and 2) to further investigate in vitro the radical scavenging properties of these analogues by two sensitive methods. Concerning 1: isolated rat heart...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1998.tb00937.x
更新日期:1998-01-01 00:00:00