Abstract：
:A major challenge in translational research is to reduce the currently high proportion of new candidate treatment agents for neuroinflammatory disease, which fail to reproduce promising effects observed in animal models when tested in patients. This disturbing situation has raised criticism against the currently used animal models in preclinical research and calls for improvement of these models. This seems a difficult task as the cause of failure is often not known. Here we propose a potentially useful strategy for investigating why a promising strategy fails as a guidance for improving the validity of the animal model(s).
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
't Hart BAdoi
10.1016/j.ejphar.2015.03.030subject
Has Abstractpub_date
2015-07-15 00:00:00pages
14-8eissn
0014-2999issn
1879-0712pii
S0014-2999(15)00245-9journal_volume
759pub_type
杂志文章,评审abstract：:The effect of high helium pressure on inhibitory synaptic transmission was studied in rat hippocampal slices with extracellular recordings. Both feed-forward and recurrent GABAergic inhibition were tested in the CA1 region with paired-pulse stimulation paradigms. The efficiency of both types of inhibition decreased un...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90606-1
更新日期：1988-08-24 00:00:00
abstract：:In chloralose-anaesthesized cats, clonidine, an alpha 2-adrenoceptor agonist with an imidazole ring, depressed pudendal nerve reflex activity. Clonidine's inhibitory action on this compound action potential response was mimicked by guanabenz, a non-imidazole alpha 2-adrenoceptor agonist, and was reversed by SK & F 864...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90551-z
更新日期：1991-03-26 00:00:00
abstract：:The repeated administration of N-methyl-beta-carboline-3-carboxamide (FG 7142) to mice leads to 'chemical kindling', i.e. the development of seizures in response to doses which were initially insufficient to produce convulsive activity. To determine if chemical kindling produced changes in the GABAA receptor/chloride ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90658-4
更新日期：1989-01-24 00:00:00
abstract：:Metastasis in breast cancer is a leading cause of mortality among women in many countries. This study investigated the anti-cancer role of benzoimidazoquinazoline and benzimidazotriazin; two novel compounds that were designed, synthesized, structurally elucidated, and biologically evaluated as potent anti-angiogenic a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173747
更新日期：2021-02-05 00:00:00
abstract：:Kinin B1 receptors on rabbit aorta smooth muscle cells in culture were investigated. [3H]Des-Arg10-kallidin labeled a single site in cells at early passage with an equilibrium dissociation constant of 258 pM and a maximal binding density of approximately 680 sites/cell. Treatment of the same cells for 18 h with epider...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90137-6
更新日期：1994-02-15 00:00:00
abstract：:Levcromakalim was more potent at relaxing rat small mesenteric arteries with endothelium (EC50, 84+/-10 nM) than denuded vessels (EC50, 779+/-101 nM). The cannabinoid receptor antagonist SR 141716A (N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-me thyl-1H-pyrazole-3-carboxamide hydrochloride; 1 microM...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01397-6
更新日期：1997-11-27 00:00:00
abstract：:Crocetin, an aglycone of crocin, is found both in the saffron crocus (Crocus starus L.) and in gardenia fruit (Gardenia jasminoides Ellis). We evaluated the protective effects of crocetin against the retinal ischemia induced by 5h unilateral ligation of both the pterygopalatine artery (PPA) and the external carotid ar...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.02.007
更新日期：2013-03-05 00:00:00
abstract：:Anandamide is an endogenous ligand at both the inhibitory cannabinoid CB(1) receptor and the excitatory vanilloid receptor 1 (VR1). The CB(1) receptor and vanilloid VR1 receptor are expressed in about 50% and 40% of dorsal root ganglion neurons, respectively. While all vanilloid VR1 receptor-expressing cells belong to...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(01)01309-7
更新日期：2001-10-19 00:00:00
abstract：:It has been shown that α(2)-adrenoceptors mediate vasopressor responses in pithed rats. However, the corresponding α(2)-adrenoceptor subtypes have not been pharmacologically identified. Thus, this study set out to identify the specific subtypes (α(2A), α(2B) and α(2C)) mediating the vasopressor responses to the α(2)-a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.06.011
更新日期：2012-09-15 00:00:00
abstract：:The association between cocaine administration and induction of oxidative stress in different brain regions suggests that oxidative damage is an important factor participating in cocaine disruption of normal central nervous system functions. In order to deal with this topic, brain penetrating exogenous antioxidants we...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.10.024
更新日期：2011-01-10 00:00:00
abstract：:In the presence of thiorphan an 'enkephalinase' inhibitor, bestatin an aminopeptidase inhibitor of bacterial origin potently inhibited the hydrolysis of [3H][Leu5]enkephalin by slices from rat striatum with an IC50 value of about 0.2 microM whereas puromycin was approximately 1000 times less potent on this preparation...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90181-4
更新日期：1983-01-21 00:00:00
abstract：:The mouse and tissues from this species are increasingly used as experimental models because of the wide variety of gene deletions and overexpressions available in this species. Yet, very little is known about normal vascular responses in the mouse. We investigated the vasorelaxant responses on thoracic aortic rings f...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01418-2
更新日期：2001-11-16 00:00:00
abstract：:The effects of propranolol alone or associated with atrial pacing were studied on regional myocardial blood flows (RMBF) and regional contractility (sonocardiometry) in non-ischemic, moderately and severely ischemic areas of the canine myocardium. In non-ischemic areas, propranolol reduced both epicardial and endocard...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90284-4
更新日期：1983-09-02 00:00:00
abstract：:The biological activity of two galanin (GAL) fragments, GAL-(1-16) and GAL-(17-29), was tested in vivo by using a spinal nociceptive flexor reflex model in the rat. Intrathecal (i.t.) GAL-(1-16) had a similar biphasic effect on the flexor reflex, with facilitation at lower doses and facilitation followed by depression...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90502-w
更新日期：1990-06-21 00:00:00
abstract：:Recent studies have suggested that hydrogen sulfide (H2S), an important endogenous signaling gaseous molecule, participates in relaxation of smooth muscle. Nevertheless, the mechanism of this relaxation effect on respiratory system is still unclear. The present study aims to investigate the physiological function as w...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.07.004
更新日期：2014-10-15 00:00:00
abstract：:Intracellular accumulation of calcium is thought to play an integral role in the progression of ischemic injury and cell death. We infused the calcium entry blocker, nitrendipine (1.5 micrograms/kg per min), into cats in order to investigate the importance of extracellular Ca2+ influx during hemorrhagic shock. Nitrend...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90510-7
更新日期：1984-01-13 00:00:00
abstract：:The effects of 1 mM L-cysteine on sodium nitrite-, 3-morpholinosydnonimine (SIN-1)- and acetylcholine-induced relaxation and cyclic GMP accumulation were studied in isolated noradrenaline-precontracted rat mesenteric arterial rings. L-Cysteine augmented the relaxation and cyclic GMP increase induced by sodium nitrate ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90133-o
更新日期：1992-04-22 00:00:00
abstract：:Peripheral electrical stimulation of the rat produced a "dose-dependent" analgesia both in intact and in spinal animals. Naloxone, a narcotic antagonist, almost completely reversed this analgesia. It is felt that peripheral electroanalgesia acts via the release of endogenous narcotic-like substances, the enkephalins, ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90016-4
更新日期：1977-10-01 00:00:00
abstract：:We have previously demonstrated that (+)-morphine and (-)-morphine given spinally stereoselectively attenuate the spinally-administered (-)-morphine-produced tail-flick inhibition in the mouse. The phenomenon has been defined as antianalgesia. Present studies were then undertaken to determine if the systemic administr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.06.012
更新日期：2007-10-01 00:00:00
abstract：:We have characterized the tachykinin NK(2) receptor-mediated contraction and vectorial ion transport responses in the muscularis mucosae and mucosa of the rat isolated distal colon, respectively. The tachykinin NK(2) receptor-selective antagonist nepadutant (c([(beta-D-GlcNAc)Asn-Asp-Trp-Phe-Dpr-Leu]c(2beta-5beta))) p...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)00836-6
更新日期：2001-03-01 00:00:00
abstract：:Angiotensin II increased the inositol phosphates production (EC50 = 3.4+/-0.7 nM) in Chinese hamster ovary (CHO) cells expressing the cloned human angiotensin AT1 receptor (CHO-AT1 cells). Coincubation with angiotensin AT1 receptor antagonists produced parallel rightward shifts of the concentration-response curve with...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00205-8
更新日期：1999-05-14 00:00:00
abstract：:We investigated the effect of probucol, a lipid-lowering agent with antioxidant properties, on HCl plus ethanol-induced gastric mucosal injury and on the healing of acetic acid-induced gastric ulcers in rats. When the free radical-scavenging activity of probucol was measured by an electron spin resonance technique, th...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00448-8
更新日期：1998-08-07 00:00:00
abstract：:Vascular hypertrophy occurs during chronic hypertension and contributes to the elevation of peripheral vascular resistance in hypertension. In this study, we examined whether acute pressure overloading of the vascular wall produces activation of mitogen-activated protein (MAP) kinases, enzymes believed to be involved ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00072-8
更新日期：2000-03-17 00:00:00
abstract：:The effects of Ca2+ channel antagonists on the capsaicin-induced cough reflex in guinea pigs were studied. Intraperitoneal injection of nifedipine, verapamil and flunarizine in doses that ranged from 0.3 to 3.0 mg/kg decreased the number of coughs in a dose-dependent manner. These Ca2+ channel antagonists exhibited an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90072-c
更新日期：1992-02-25 00:00:00
abstract：:Effects of protein kinase C inhibitors, staurosporine and 1-(5-isoquinolinylsulfonyl)-2-methylpiperazine dihydrochloride and protein tyrosine kinase inhibitors, genistein, tyrphostin and 2,5-dimethylcinnamate on the neutrophil responses stimulated by immunoglobulin G (IgG), complement C5a or platelet-activating factor...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00097-0
更新日期：1996-06-13 00:00:00
abstract：:Primary cultures of rat cerebellar granule cells are shown to possess a high density (283 +/- 48 fmol/mg of protein) of muscarinic receptor sites, defined using N-[3H]methylscopolamine [( 3H]NMS), with a KD of 0.18 +/- 0.01 nM measured after culture in vitro for 7 days. Displacement of specific [3H]NMS binding demonst...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0922-4106(05)80017-3
更新日期：1991-03-25 00:00:00
abstract：:Dermenkephalin (Tyr-D-Met-Phe-His-Leu-Met-AspNH2) is a highly potent and selective delta-opioid peptide isolated from frog skin. It was recently recognized that the C-terminus His4-Leu5-Met6-Asp7NH2 of dermenkephalin was responsible for the addressing of the peptide towards the delta-opioid receptor. In order to inves...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90107-4
更新日期：1994-01-15 00:00:00
abstract：:In mature spontaneously hypertensive (SHR) and Wistar-Kyoto (WKY) rats, acetylcholine, the calcium ionophore A 23187 and ATP release endothelium-derived contracting factor (EDCF), cyclooxygenase (COX) derivatives that activate thromboxane-endoperoxide (TP) receptors on vascular smooth muscle. The EDCFs released by ace...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.10.050
更新日期：2007-02-05 00:00:00
abstract：:Bronchial and alveolar epithelial cell apoptosis is a vital step in smoke-induced lung injury. We investigated whether and how microRNA (miRNA) Let-7f-1-3p would regulate smoke-induced apoptosis in bronchial and alveolar epithelial cells. Human small airway epithelial cells (HSAEC) and human pulmonary alveolar epithel...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172531
更新日期：2019-11-05 00:00:00
abstract：:Diabetes is a major health problem and a predisposition factor for further degenerative complications and, therefore, novel therapies are urgently needed. Currently, cannabinoid receptor 1 (CB1 receptor) antagonists have been considered as promissory entities for metabolic disorders treatment. Accordingly, the purpose...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.03.036
更新日期：2017-05-15 00:00:00
