Naunyn-Schmiedeberg's Archives of Pharmacology
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Protective effect of verbascoside in activated C6 glioma cells: possible molecular mechanisms
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Abstract The glycosylated phenylpropanoid verbascoside (VB), isolated from cultured cells of the medicinal plant Syringa vulgaris (Oleaceae), has previously been characterized as an effective scavenger of biologically active free radicals and an inhibitor
of lipid peroxidation. The aim of the present study was to evaluate in a rat glioma cell line (C6) the effect of VB biotechnologically
produced by S. vulgaris plant cell cultures in the regulation of the inflammatory response. We used a model of central nervous system inflammation
induced by bacterial endotoxin/cytokine (lipopolysaccharide (LPS)/interferon (...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - November 10, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Apoptosis induction by doxazosin and other quinazoline α1-adrenoceptor antagonists: a new mechanism for cancer treatment?
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Abstract Doxazosin and related, quinazoline-based α1-adrenoceptor antagonists can induce apoptosis in prostate and various other normal, benign, smooth muscle, endothelial and
malignant cells. Such apoptosis-inducing effects occur independently of α1-adrenoceptor antagonism and typically require much high concentrations than those required for receptor occupancy. Several
studies have invested efforts towards the elucidation of the molecular mechanisms underlying doxazosin-induced apoptosis.
These include various tumor cells, cardiomyocytes, endothelial cells and bladder smooth muscle cells. While the high c...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - November 10, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Opposite effects of milnacipran, a serotonin norepinephrine reuptake inhibitor, on the levels of nitric oxide and brain-derived neurotrophic factor in mouse brain cortex
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We report here the effects of subchronic
treatment of mice with milnacipran, a serotonin norepinephrine reuptake inhibitor, on the levels of NO and BDNF in mice. In
vivo administration of milnacipran (10 mg/kg) for 14 days caused a significant decrease in nitrate and nitrite concentrations
in the cerebral cortex and hippocampus, but not in the midbrain. Milnacipran (10 mg/kg, 14 days) also decreased the activity
of NO synthase in the cerebral cortex. On the other hand, milnacipran (10 mg/kg, 14 days) increased the levels of BDNF protein
and mRNA in the cerebral cortex. These findings sugg...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - November 5, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Nitric oxide and potassium channels mediate GM1 ganglioside-induced vasorelaxation
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In this study, we demonstrate that GM1 (10, 30, 100, 300 µM, 1 and 3 mM) induces vascular relaxation determined by isometric
tension studies in rat mesenteric artery rings contracted with 1 µM phenylephrine. The vasorelaxation induced by GM1 was abolished
by endothelium removal, by incubation with l-NAME (1 µM), and partially inhibited by the blockade of potassium channels by 1 mM tetraethylammonium, 10 µM glibenclamide,
by the soluble guanylate cyclase inhibitor 1H-[1,2,4]oxadiazolo[4,3-alpha]quinoxalin-1-one (10 µM), and by 50 nM charybdotoxin,
a blocker of large and inter...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - November 5, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Inhibitors of TRP channels reveal stimulus-dependent differential activation of Ca2+ influx pathways in human neutrophil granulocytes
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Abstract A pharmacological characterization of Ca2+ influx pathways in neutrophil granulocytes is problematic because of the lack of specific inhibitors. The activation of transient
receptor potential cation channel, subfamily M, member 2 (TRPM2) channels by intracellular adenosine diphosphate ribose (ADPR),
well characterized in neutrophils, is reportedly inhibited by 8-bromo-ADPR (8Br-ADPR). TRPM2 is blocked by N-(p-amylcinnamoyl)anthranilic acid (ACA) interfering with the pore, but ACA is as well effective on other transient receptor
potential channels, especially transient receptor potential canonical (TR...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - November 5, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Vasodilator effects of Diocleinae lectins from the Canavalia genus
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This study investigated and compared vascular actions of leguminous lectins obtained from the Canavalia genus (Canavalia brasiliensis, Canavalia gladiata, and Canavalia maritima) in the rat models of paw edema and isolated aorta. Paw edema was induced by subcutaneous injection of lectins (0.01–1 mg/kg)
in animals pre-treated or not with indomethacin or L-NAME. In isolated aorta, cumulative concentration curves of C. gladiata or C. brasiliensis (1–100 µg/ml) were performed at the contraction plateau induced by phenylephrine or at tissue basal tonus. The mechanism
of the lectin relaxant action was investigat...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - October 23, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Interference of the noradrenergic neurotoxin DSP4 with neuronal and nonneuronal monoamine transporters
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Abstract The haloalkylamine DSP4 (N[-2-chloroethyl]-N-ethyl-2-bromobenzylamine) is a noradrenergic neurotoxin, which is used for the chemical denervation of noradrenergic neurons,
and it has been proposed to be a selective substrate for the neuronal, Na+- and Cl−-dependent noradrenaline transporter (NAT). In the present study, we investigated whether DSP4 not only interacts with the
human NAT (hNAT) but also with other neuronal monoamine transporters such as the transporters for dopamine (hDAT) and serotonin
(hSERT) or with nonneuronal (Na+-independent) monoamine transporters also known as organic cation tr...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - October 16, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Pharmacological modulation of transmitter release by inhibition of pressure-dependent potassium currents in vestibular hair cells
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Abstract Vestibular vertigo may be induced by increases in the endolymphatic pressure that activate pressure-dependent K+ currents (IK,p) in vestibular hair cells. IK,p have been demonstrated to modulate transmitter release and are inhibited by low concentrations of cinnarizine. Beneficial
effects against vestibular vertigo of cinnarizine have been attributed to its inhibition of calcium currents. Our aim was
to determine the extent by which the inhibition of IK,p by cinnarizine may alter the voltage response to stimulating currents and to analyze whether such alterations may be sufficient
to modulate the act...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - October 14, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Pharmacological profile of intrathecal fadolmidine, a α2-adrenoceptor agonist, in rodent models
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Abstract The present experiments compared the peripheral and central pharmacological effects of three α2-adrenoceptor agonists: fadolmidine, clonidine, and dexmedetomidine after single intrathecal bolus injections at analgesic
dose level in rats. Effects on mydriasis and cardiovascular functions were studied in anaesthetised rats, the effects on sedation/motor
performance, body temperature, and gastrointestinal motility were evaluated in conscious rats, and also the effects on brain
biogenic amines were studied. All compounds caused dose-dependent mydriasis, a decrease in blood pressure and heart rate,
seda...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - October 13, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Mechanisms of the inhibition of endplate acetylcholine receptors by antiseptic chlorhexidine (experiments and models)
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Abstract Mechanisms of the inhibition of evoked multiquantal endplate currents (EPC) by chlorhexidine (CHX) were studied in electrophysiological
experiments and by mathematical modeling to discriminate between possible channel, receptor, and non-receptor effects of this
common antiseptic drug. Experiments were carried out on the isolated neuromuscular preparation of the cut m. sartorius of
the frog Rana ridibunda. The nerve-stimulation-evoked endplate currents were measured by standard double microelectrode technique. For the mathematical
simulation, a method based on the solution of a system of ordinary dif...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - October 6, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Synthesis and characterisation of NS13558: a new important tool for addressing KCa1.1 channel function ex vivo
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Abstract Pharmacological activation of the large-conductance Ca2+-activated K+ channel (KCa1.1) in the cardiac inner mitochondrial membrane has been found to protect the heart against ischemia reperfusion
injuries. However, there are concerns about the selectivity of the pharmacological tools used to modulate the channel. Here,
we address this issue by synthesising a methylated analogue of the tool KCa1.1 channel activator NS11021. The compound (NS13558)
is designed as a structurally closely related and biologically inactive analogue of NS11021. NS13558 did not elicit any significant
opening of cloned human ...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - October 1, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Atrial Ca2+ signaling in atrial fibrillation as an antiarrhythmic drug target
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This article reviews the
molecular mechanisms of altered Ca2+ signaling in AF and discusses the potential value of novel approaches targeting atrial Ca2+-handling abnormalities.
Content Type Journal ArticleCategory REVIEWDOI 10.1007/s00210-009-0457-1Authors
Dobromir Dobrev, Dresden University of Technology Department of Pharmacology and Toxicology Dresden Germany
Journal Naunyn-Schmiedeberg's Archives of PharmacologyOnline ISSN 1432-1912Print ISSN 0028-1298 (Source: Naunyn-Schmiedeberg's Archives of Pharmacology)
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 28, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
The human cardiac K2P3.1 (TASK-1) potassium leak channel is a molecular target for the class III antiarrhythmic drug amiodarone
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The objective
of this study was to investigate acute effects of the class III antiarrhythmic drug amiodarone on human K2P3.1 channels. Potassium currents were recorded from Xenopus oocytes using the two-microelectrode voltage clamp technique. Amiodarone produced concentration-dependent inhibition of hK2P3.1 currents (IC50 = 0.40 µM) with maximum current reduction of 58.1%. Open rectification properties that are characteristic to hK2P3.1 currents were not altered by amiodarone. Channels were blocked in open and closed states in reverse frequency-dependent
manner. hK2P3.1 channel inhibition was voltage-independen...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 24, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Tunicamycin induces resistance to camptothecin and etoposide in human hepatocellular carcinoma cells: role of cell-cycle arrest and GRP78
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In conclusion,
the data suggest that tunicamycin induces the resistance to topoisomerase inhibitors through GRP78 up-regulation and G1 arrest
of the cell cycle. The findings also prompt the deliberation that the resistance can be caused during combined administration
of chemotherapeutic drugs and Chinese herbal medicines, which induce endoplasmic reticulum stress and/or cell-cycle arrest
in cancer cells.
Content Type Journal ArticleCategory ORIGINAL ARTICLEDOI 10.1007/s00210-009-0453-5Authors
Jui-Ling Hsu, National Taiwan University School of Pharmacy No. 1, Section 1, Jen-Ai Road Taipei TaiwanPo-Cheng Chiang, Na...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 24, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Inhibitory effects of cigarette smoke extract on neural crest migration occur through suppression of R-spondin1 expression via aryl hydrocarbon receptor
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Abstract Although it is known that smoking during pregnancy induces fetal malformations, few basic studies at the molecular level are
currently available. Since it is known that neural crest cells (NCC) play an important role in tissue development and differentiation,
we investigated the influence of cigarette smoke extract (CSE) on NCC migration. CSE treatment reduced the migration index
of NCC in dose- and tar-content-dependent manners without induction of apoptosis or decrease in proliferation of NCC. alpha-Naphthoflavone,
an antagonist of aryl hydrocarbon receptor (AhR), prevented the reduction in NCC mi...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 18, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Es kann die Spur von unseren Erdetagen—on pharmacologists and pharmacology
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Abstract
Es kann die Spur von unseren Erdetagen is a slightly modified line from Goethe’s tragedy Faust and together with the following line can be translated as “The vestiges of our path on earth/Through aeons cannot fade away”.
The author’s festival speech at the 50th Spring Meeting of the German Pharmacological Society this year in Mainz was given under that title and is presented here in abridged form. Twelve examples are given showing that
indeed our, the pharmacologists’, professional vestiges cannot disappear. Many pharmacologists may share this view of their
profession.
Content Type Jou...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 17, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Inhibition of IK,ACh current may contribute to clinical efficacy of class I and class III antiarrhythmic drugs in patients with atrial fibrillation
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Abstract Inward rectifier potassium currents IK1 and acetylcholine activated IK,ACh are implicated in atrial fibrillation (AF) pathophysiology. In chronic AF (cAF), IK,ACh develops a receptor-independent, constitutively active component that together with increased IK1 is considered to support maintenance of AF. Here, we tested whether class I (propafenone, flecainide) and class III (dofetilide,
AVE0118) antiarrhythmic drugs inhibit atrial IK1 and IK,ACh in patients with and without cAF. IK1 and IK,ACh were measured with voltage clamp technique in atrial myocytes from 58 sinus rhythm (SR) and 35 cAF patients. T...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 17, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Peripheral nerve injury up-regulates expression of interactor protein for cytohesin exchange factor 1 (IPCEF1) mRNA in rat dorsal root ganglion
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Abstract Interaction protein for cytohesin exchange factors 1 (IPCEF1) is a recently identified protein that binds to cytohesin 2 and
might participate in membrane receptor trafficking by enhancing the activity of cytohesin 2 in cultured cells. However, whether
IPCEF1 is involved in this process in vivo is unknown. Here, we report that IPCEF1 messenger RNA (mRNA) is expressed in the
dorsal root ganglions (DRGs) of adult rats. Moreover, peripheral nerve injury induced by fifth spinal nerve ligation and transection
or sciatic nerve transection significantly up-regulated expression of IPCEF1 mRNA in the injured...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 15, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Inhibitory effect of reinioside C on monocyte–endothelial cell adhesion induced by oxidized low-density lipoprotein via inhibiting NADPH oxidase/ROS/NF-κB pathway
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Abstract Monocyte adhesion to activated vascular endothelial cells is the critical event in the initiation of atherosclerosis. Adhesion
molecules are inflammatory markers, which are upregulated by oxidized low-density lipoprotein (ox-LDL) and play a pivotal
role in atherogenesis. In present study, the effect of reinioside C, a major compound of Polygala fallax Hemsl., on adhesion of monocytes to endothelial cells induced by ox-LDL was investigated. The results showed that incubation
of endothelial cells with ox-LDL (100 µg/mL) for 24 h markedly increased the expression of ICAM-1 and P-selectin and enh...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 15, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Transforming growth factor-β type I receptor/ALK5 contributes to doxazosin-induced apoptosis in H9C2 cells
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In conclusion, our results demonstrated that TβRI/ALK5-p38 MAPK phosphorylation signaling pathway could contribute
to doxazosin-induced cell apoptosis, which could be further enhanced by TGF-β1 in association with attenuating Smad3 phosphorylation
in H9C2 cells.
Content Type Journal ArticleCategory ORIGINAL ARTICLEDOI 10.1007/s00210-009-0449-1Authors
Yi-Fan Yang, National Taiwan University Institute of Pharmacology, College of Medicine No. 1, Sec. 1, Jen-Ai Rd Taipei 100 TaiwanChau-Chung Wu, National Taiwan University Hospital Department of Internal Medicine Taipei TaiwanWen-Pin Chen, National Taiwan University I...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 3, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Potentiation of excitatory serotonergic responses by MK-801 in the medial prefrontal cortex
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Abstract New atypical antipsychotics show a greater affinity to serotonergic rather than to dopamine receptors, suggesting that serotonin
(5-HT) has a major role in the pathophysiology and treatment of schizophrenia. The goal of this study was to characterise
the response of pyramidal neurons in the medial prefrontal cortex (mPFC) to 5-HT and NMDA before and after administration
of the NMDA receptor antagonist, MK-801 (dizocilpine), a well-validated pharmacological model of psychosis. mPFC pyramidal
(glutamatergic) neurons were recorded in urethane-anaesthetised rats. The responses to NMDA and 5-HT were asse...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - September 3, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Interaction of androsterone and progesterone with inhibitory ligand-gated ion channels: a patch clamp study
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In conclusion, different molecular mechanisms of interaction between neuroactive steroids and GABA as
well as glycine receptors could be identified and quantitatively described. Our data clarify the role of steroid compounds
in the modulation of inhibitory receptor channel function.
Content Type Journal ArticleCategory ORIGINAL ARTICLEDOI 10.1007/s00210-009-0440-xAuthors
Elke Ziegler, Medical University Hannover Department of Neurology Carl-Neuberg-Str. 1 30625 Hanover GermanyM. Bodusch, Medical University Hannover Department of Neurology Carl-Neuberg-Str. 1 30625 Hanover GermanyY. Song, Medical University Hannover ...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - August 24, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Antinociceptive activity and toxicology of the lectin from Canavalia boliviana seeds in mice
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Abstract The aim of the present study was to evaluate the potential antinociceptive and toxicity of Canavalia boliviana lectin (CboL) using different methods in mice. The role of carbohydrate-binding sites was also investigated. CboL given to
mice daily for 14 days at doses of 5 mg/kg did not cause any observable toxicity. CboL (1, 5, and 10 mg/kg) administered to
mice intravenously inhibited abdominal constrictions induced by acetic acid and the two phases of the formalin test. In the
hot plate and tail immersion tests, the same treatment of CboL induced significant increase in the latency per...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - August 24, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Magnesium modifies fentanyl-induced local antinociception and hyperalgesia
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Abstract Fentanyl-induced hyperalgesia and antinociception after systemic administration has been shown in previous clinical and experimental
studies. However, there is very little evidence regarding the local possible effects of fentanyl. The purpose of this study
was to assess whether local (intraplantar) fentanyl administration can produce antinociception and hyperalgesia. In addition,
we examined the effects of magnesium, N-methyl-D-aspartate receptor antagonist, on possible changes produced by fentanyl. The paw withdrawal latencies to radiant heat stimuli
were measured to assess the thermal nociceptive ...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - August 21, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Phosphodiesterases do not limit β1-adrenoceptor-mediated sinoatrial tachycardia: evidence with PDE3 and PDE4 in rabbits and PDE1–5 in rats
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Abstract The mammalian heart expresses at least five phosphodiesterases (PDE1–5). Catecholamines produce surges of inotropically relevant
cAMP through β1-adrenoceptor stimulation. cAMP is mainly hydrolysed by PDE3 and/or PDE4 thereby blunting contractility. Basal sinoatrial
beating rate in mouse, rat, piglet and rabbit sinoatrial cells is reduced by PDE3 and/or PDE4 through hydrolysis of cAMP.
However, in rodents, the tachycardia elicited by catecholamines through production of cAMP by β-adrenoceptor activation is
not controlled by PDE3 and PDE4, despite a blunting effect of PDE3 or/and PDE4 on basal sin...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - August 19, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
The effects of the TRPV1 receptor antagonist SB-705498 on trigeminovascular sensitisation and neurotransmission
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This report examines the effect of the transient receptor potential vanilloid 1 receptor antagonist SB-705498 on neurotransmission
and inflammation-induced sensitisation in the trigeminovascular sensory system. A single-neuron electrophysiological animal
model for neurovascular head pain was used to evaluate dural and facial noxious inputs and the effects of SB-705498 administered
by intravenous (i.v.) injection. Electrical and mechanical stimulation of the dura mater and the facial skin activated second-order
neurons in the trigeminal nucleus caudalis of cats, with A-δ latencies. Intravenous injection of SB-705498 (2...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - August 19, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Effect of carvedilol on behavioral, mitochondrial dysfunction, and oxidative damage against d-galactose induced senescence in mice
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In conclusion, present studies
highlight the protective effects of CAR against d-galactose-induced behavioral, biochemical, and mitochondrial dysfunction in mice. The study further provides a hope that
CAR could be used in the management of cognitive dysfunction and related symptoms during aging.
Content Type Journal ArticleCategory ORIGINAL ARTICLEDOI 10.1007/s00210-009-0442-8Authors
Anil Kumar, Panjab University Pharmacology Division, University Institute of Pharmaceutical Sciences, UGC Centre for Advance Studies Chandigarh 160014 IndiaSamrita Dogra, Panjab University Pharmacology Division, University Institute of...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - August 14, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Reciprocal regulation between M3 muscarinic acetylcholine receptor and protein kinase C-ε in ventricular myocytes during myocardial ischemia in rats
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Abstract We have studied the association between M3 muscarinic acetylcholine receptors (M3-mAChR) and protein kinase C-ε (PKC-ε) during ischemic myocardial injury using Western blot analysis and immunoprecipitation
technique. Myocardial ischemia (MI) induced PKC-ε translocation from cytosolic to membrane fractions. This translocation participated
in the phosphorylation of M3-mAChR in membrane fractions, which could be abolished by the inhibitor of PKC, chelerythrine chloride. On the other hand,
M3-mAChR could also regulate the expression of PKC-ε in ischemic myocardium. Choline (choline chloride, an M3 re...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - August 14, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Desensitisation of native and recombinant human urotensin-II receptors
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Abstract Human urotensin-II (U-II) is an 11-amino-acid cyclic peptide that activates a Gq-coupled receptor named UT. Little is known about the desensitisation profile of this receptor as peptide binding is essentially
irreversible. In the present study, we have examined the effects of U-II and carbachol on Ca2+ signalling in SJCRH30 rhabdomyosarcoma (receptor density, Bmax ~0.1 pmol/mg protein) and human embroynic kidney (HEK)hUT (B
max ~1.4 pmol/mg protein) cells expressing native and recombinant UT, respectively. In SJCRH30, HEKhUT and human peripheral blood mononuclear cells induced to express nat...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - August 12, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Inotropic effects of l-lysine in the mammalian heart
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Abstract We studied the effects of l-lysine in cardiac preparations of mice and men. Of note, l-lysine increased force of contraction in a concentration- and time-dependent manner in isolated electrically paced left atrium
of mouse and in human right atrium. It further increased heart rate and left ventricular pressure in the isolated perfused
mouse heart. In isolated adult mouse cardiomyocytes, the contractility as assessed by edge detection was increased as well
as the Ca2+ transients after electrically pacing by field stimulation. However, using the patch clamp technique, no effect of l-lysine on action po...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - August 7, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
The peripheral administration of a nitric oxide donor potentiates the local antinociceptive effects of a DOR agonist during chronic inflammatory pain in mice
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Abstract Several works reveal that nitric oxide could enhance the peripheral antinociception induced by opioids during acute inflammation.
Nonetheless, the role of nitric oxide in the local antinociceptive effects of δ-opioid receptor (DOR) agonists during chronic
peripheral inflammation is not known. The aim of this study is to evaluate whether nitric oxide would enhance the local antinociceptive
effects of a DOR agonist during chronic inflammatory pain in mice. Chronic inflammatory pain was induced by the subplantar
administration of complete Freund’s adjuvant (CFA; 30 µl) and thermal hyperalgesia as...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - July 27, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Role of sphingosine-1-phosphate (S1P) and the S1P2 receptor in allergen-induced, mast cell-dependent contraction of rat lung parenchymal strips
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Abstract Lung parenchymal strips isolated from ovalbumin-sensitized rats manifest a mast cell-dependent, biphasic contraction when
challenged with allergen. The first phase is mediated by the release of preformed 5-HT while the second phase is dependent
on de novo synthesis of leukotrienes. Sphingosine 1-phosphate (S1P) is a sphingolipid metabolite which is readily generated
in mast cells and has been demonstrated to be an important regulator of allergen-induced mast cell activation. We have used
the parenchymal strip to explore the role of sphingosine 1-phosphate and the S1P2 receptor in the two components ...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - July 27, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
TRPA1 agonists delay gastric emptying in rats through serotonergic pathways
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Abstract Our recent study found that TRPA1 is highly expressed in enterochromaffin cells and that stimulation of these cells with TRPA1
agonists enhances 5-hydroxytryptamine (5-HT) secretion in vitro. Here, to demonstrate the 5-HT-releasing effect of TRPA1 agonists
in vivo, we examined the effect of TRPA1 agonists on gastric emptying in rats. The results showed that TRPA1 agonists dose-dependently
delayed gastric emptying. Further, the effects of TRPA1 agonists on this delay were abolished in rats treated with a TRPA1
antagonist, an inhibitor of tryptophan hydroxylase, or a 5-HT3 receptor antagonist. Taken t...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - July 25, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
The guinea pig ileum lacks the direct, high-potency, M2-muscarinic, contractile mechanism characteristic of the mouse ileum
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Abstract We explored whether the M2 muscarinic receptor in the guinea pig ileum elicits a highly potent, direct-contractile response, like that from the M3 muscarinic receptor knockout mouse. First, we characterized the irreversible receptor-blocking activity of 4-DAMP mustard
in ileum from muscarinic receptor knockout mice to verify its M3 selectivity. Then, we used 4-DAMP mustard to inactivate M3 responses in the guinea pig ileum to attempt to reveal direct, M2 receptor-mediated contractions. The muscarinic agonist, oxotremorine-M, elicited potent contractions in ileum from wild-type,
M2 receptor knockout, a...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - July 7, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Antinociceptive effects of (O-methyl)-N-benzoyl tyramine (riparin I) from Aniba riparia (Nees) Mez (Lauraceae) in mice
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Abstract The present study examined the antinociceptive effects of (O-methyl) N-benzoyl-tyramine (riparin I, ripI) isolated from the unripe fruit of Aniba riparia in chemical and thermal behavioral models of pain, such as acetic acid-induced abdominal writhing, formalin, and hot-plate
tests in mice. Moreover, the involvement of the nitric oxide pathway as well as the opioid system in the antinociceptive action
of ripI in the formalin test was investigated. RipI was administered both orally and intraperitoneally to male mice at single
doses of 25 and 50 mg/kg. In the acetic acid-induced abdominal writhing...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - June 26, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Determinants for the cAMP-binding site at the S-adenosylhomocysteine-hydrolase
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In conclusion, our data show
that the cAMP-binding site at the AdoHcy-hydrolase is independent of the NAD+/NADH ratio of the enzyme and is identical with the high affinity-binding site of Ado. Moreover, cAMP did not interact with
the catalytic site of AdoHcy-hydrolase and did not act as an allosteric effector for the AdoHcy-hydrolase.
Content Type Journal ArticleCategory ORIGINAL ARTICLEDOI 10.1007/s00210-009-0432-xAuthors
Doris Kloor, University of Tübingen Department of Experimental and Clinical Pharmacology and Toxicology, Faculty of Medicine Wilhelmstraße 56 72074 Tübingen GermanyMarina Hermes, University of ...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - June 23, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Abstracts from the 7th International Meeting of the Sphingolipid Club held in Leiden, The Netherlands, 14.-16.11.2008
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Content Type Journal ArticleCategory ABSTRACTSDOI 10.1007/s00210-009-0430-z
Journal Naunyn-Schmiedeberg's Archives of PharmacologyOnline ISSN 1432-1912Print ISSN 0028-1298 (Source: Naunyn-Schmiedeberg's Archives of Pharmacology)
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - June 19, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Abstracts of the FIGON Dutch Medicine Days in Lunteren on 6-8 October 2008
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Content Type Journal ArticleCategory ABSTRACTSDOI 10.1007/s00210-009-0422-z
Journal Naunyn-Schmiedeberg's Archives of PharmacologyOnline ISSN 1432-1912Print ISSN 0028-1298 (Source: Naunyn-Schmiedeberg's Archives of Pharmacology)
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - June 16, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Coupling factor 6 as a novel vasoactive and proatherogenic peptide in vascular endothelial cells
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Abstract Coupling factor 6 (CF6) is composed of 76 amino acids and is present in the peripheral stalk of mitochondrial ATP synthase.
The generation of CF6 is positively regulated by tumor necrosis factor α and shear stress via nuclear factor κB, and by high
glucose via protein kinase C and p38 mitogen-activated protein kinase. CF6 is released outside of the cells from vascular
endothelial cells, and binds to the β-subunit of the plasma membrane-bound ATP synthase in vascular endothelial cells and
leads to intracellular acidosis. CF6 produces vasoconstriction, and the biological active site resides at the ...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - June 2, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Adenosine A2A receptor deficient mice are partially resistant to limbic seizures
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Abstract The neuromodulator adenosine, acting through activation of four defined metabotropic receptors called A1, A2A, A2B and A3, has been proposed as an endogenous anticonvulsant. Here, the consequences of deleting the adenosine A2A receptor have been examined in different experimental models of epilepsy. A2AR KO mice were not protected against seizures originating from brainstem structures, namely electroshock-induced seizures.
The intensities of seizures induced by pentylenetetrazol or pilocarpine, as well as the percentages of convulsing mice, were
significantly reduced in A2A receptor knockout (A2AR KO)...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - June 2, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Gastroprotective activity of isopulegol on experimentally induced gastric lesions in mice: investigation of possible mechanisms of action
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Abstract The present study investigated whether isopulegol, a monoterpene present in essential oils of several aromatic plants, would
be able to promote some gastroprotective effect and also verified the possible mechanisms involved in this action. For this
study, ethanol- and indomethacin-induced gastric ulcer models in mice and histopathological assessment were used. The roles
of NO, sulfhydryls (glutathione, GSH), ATP-sensitive K+ channels (KATP channels), and prostaglandins were also investigated. Isopulegol exhibited a dose-related gastroprotective effect against
ethanol-induced lesions, while the pretr...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 29, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Novel selective ligands for free fatty acid receptors GPR120 and GPR40
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Abstract GPR120 and GPR40 are G-protein-coupled receptors whose endogenous ligands are medium- and long-chain free fatty acids, and
they are thought to play an important physiological role in insulin release. Despite recent progress in understanding their
roles, much still remains unclear about their pharmacology, and few specific ligands for GPR120 and GPR40 besides medium-
to long-chain fatty acids have been reported so far. To identify new selective ligands for these receptors, more than 80 natural
compounds were screened, together with a reference compound MEDICA16, which is known to activate GPR40, by m...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 27, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Signaling properties of human α1D-adrenoceptors lacking the carboxyl terminus: intrinsic activity, agonist-mediated activation, and desensitization
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Abstract α1-Adrenoceptors are differentially regulated by protein kinase C-mediated phosphorylation. The most sensitive member of this
family is the α1D-subtype, which is also characterized by a constitutive activity and a reduced expression at the plasma membrane controlled
by the amino terminus. Information on the structural domains that determine the function and regulation of this receptor subtype
is scarce. Therefore, the function and phosphorylation of amino terminus-truncated (Δ1–79, (ΔN)) α1D-adrenoceptors were studied and compared with those of α1D-adrenoceptors truncated both at the amino an...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 21, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Suppressive effect of CTB glycoprotein (75 kDa) on IL-4 expression in primary-cultured lymphocytes treated with di(2-ethylhexyl) phthalate
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Abstract The purpose of this study is to determine the inhibitory effect of a glycoprotein isolated from Cudrania tricuspidata Bureau (CTB glycoprotein, 75 kDa) on di(2-ethylhexyl) phthalate (DEHP)-induced differentiation of T helper (Th) type 2 cells
in T lymphocytes separated from mice. This experiment evaluated the activities of protein kinase C (PKC), mitogen-activated
protein kinase (MAPK), transcription factors [signal transducer and activator of transcription (STAT)-6 and GATA-binding protein
3 (GATA3)], and Th2 cell-related cytokine [interleukin-4 (IL-4)] using immunoblotting and reverse transcri...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 14, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Effects of a single postnatal methamphetamine administration on NMDA-induced seizures are sex- and prenatal exposure-specific
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Abstract The aim of our study was to reveal whether acute methamphetamine (MA) administration changes the sensitivity to seizures induced
by N-methyl-d-aspartate (NMDA) in prenatally MA-exposed adult rats. Adult rats with respect to sex and female estrous cycle (prenatally
MA-exposed, prenatally saline-exposed, and controls) were divided into groups with acute MA (1 mg/kg) or without acute drug
administration (saline injection). Intraperitoneal administration of 250 mg/kg of NMDA was used as a seizure model. The present
study demonstrated that both prenatal MA and prenatal saline exposure decreased...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 14, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Effect of antipsychotic drug perphenazine on fast sodium current and transient outward potassium current in rat ventricular myocytes
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Abstract Antipsychotic drug perphenazine belongs to the phenothiazine group commonly reported to induce ECG changes and tachyarrhythmias.
Data about its effect on ionic membrane currents in cardiomyocytes are missing. We analyzed the effect of perphenazine (0.1–100 µM)
on fast sodium current I
Na and transient outward potassium current I
to in enzymatically isolated rat right ventricular myocytes by the whole-cell patch-clamp technique at room temperature. Perphenazine
reversibly blocked I
Na (reducing its amplitude; IC50 = 1.24 ± 0.10 µM) and I
to (accelerating its apparent inactiv...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 9, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Blockade of HERG K+ channel by isoquinoline alkaloid neferine in the stable transfected HEK293 cells
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Abstract We studied the effects of isoquinoline alkaloid neferine (Nef) extracted from the seed embryo of Nelumbo nucifera Gaertn on Human ether-à-go-go-related gene (HERG) channels stably expressed in human embryonic kidney (HEK293) cells using
whole-cell patch clamp technique, western blot analysis and immunofluorescence experiment. Nef induced a concentration-dependent
decrease in current amplitude according to the voltage steps and tail currents of HERG with an IC50 of 7.419 μM (n
H −0.5563). Nef shifted the activation curve in a significantly negative direction and accelerated recovery from inac...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 8, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Inhaled corticosteroids and long-acting beta-agonists in adult asthma: a winning combination in all?
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Content Type Journal ArticleCategory Retraction NoteDOI 10.1007/s00210-009-0418-8Authors
Dirkje S. Postma, University Medical Center, University of Groningen Department of Pulmonology Hanzeplein 1 9713 GZ Groningen The NetherlandsHuib A. M. Kerstjens, University Medical Center, University of Groningen Department of Pulmonology Hanzeplein 1 9713 GZ Groningen The NetherlandsNick H. T. ten Hacken, University Medical Center, University of Groningen Department of Pulmonology Hanzeplein 1 9713 GZ Groningen The Netherlands
Journal Naunyn-Schmiedeberg's Archives of PharmacologyOnline ISSN 1432-1912Print ISSN 0028-1298 (...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 8, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
Safflor yellow B suppresses pheochromocytoma cell (PC12) injury induced by oxidative stress via antioxidant systemand Bcl-2 /Bax pathway
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Abstract Our previous study demonstrates that SYB produces a neuroprotective effect in vivo. In the present study, we investigated
the protective effect of safflor yellow B (SYB) on the acute oxidative injury induced by H2O2 and mechanisms in PC12 cells. H2O2 was used to mimic in vitro model of the oxidative injury and to induce apoptosis in PC12 cells. The cells were pretreated
with the different concentrations of SYB. The cell viability, lactate dehydrogenase (LDH) release, malondialdehyde (MDA),
and superoxide anion levels, superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities were meas...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 8, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
NF-κB induces PGE2-synthesizing enzymes in neurons
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Abstract The transcription factor NF-κB is activated in neurons and promotes neuronal death in cerebral ischemia. Its target genes
include cytosolic phospholipase A-2 (cPLA-2), cyclooxygenase-2 (COX-2), and microsomal prostaglandin E2 synthase-1 (mPGES-1), three genes that are involved in the synthesis of prostaglandin E2 (PGE2). In our study, oxygen glucose deprivation (OGD), an in vitro model of cerebral ischemia, activated NF-κB activity in primary
cortical neurons. Furthermore, OGD and the NF-κB activator tumor necrosis factor stimulated the expression of cPLA-2, cyclooxygenase-2
(COX-2), and mPGES-1 a...
Source: Naunyn-Schmiedeberg's Archives of Pharmacology - May 5, 2009 Category: Drugs & Pharmacology Tags: Naunyn-Schmiedeberg's Archives of Pharmacology Source Type: journals
