Abstract:
:Synthesis of the vasoconstrictor peptide endothelin-1 by endothelial and epithelial cells is strongly induced by tumor necrosis factor alpha (TNF-alpha). The actions of TNF-alpha are mediated by two transmembrane receptors of approximately 55 (p55, CD120a) and 75 kDa (p75, CD120b). Reagents activating selectively these receptor subtypes have been used to identify which TNF receptor mediates the induction of endothelin-1 synthesis. Stimulation of bovine aortic endothelial cells or human HEp-2 epithelial cells with a p55-selective mutant of human TNF-alpha (R32W-S86T) induced significant and concentration-dependent increases in endothelin-1 release. A p75 receptor-selective TNF-alpha mutant (D143N-A145R) was ineffective alone or in combination with the p55-selective mutant. Competitive binding experiments with [125I]TNF-alpha showed the p55-selective mutant, but not the p75-selective mutant, to inhibit the binding of [125I]TNF-alpha to endothelial and HEp-2 cells. Similar results were obtained with the p55 agonist antibody htr1 in both cell lines. These results establish the p55 TNF receptor as the main receptor involved in the induction of endothelin-1 synthesis by TNF-alpha.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Lees DM,Pallikaros Z,Corder Rdoi
10.1016/s0014-2999(00)00022-4keywords:
subject
Has Abstractpub_date
2000-02-25 00:00:00pages
89-94issue
1-2eissn
0014-2999issn
1879-0712pii
S0014-2999(00)00022-4journal_volume
390pub_type
杂志文章abstract::LK 204-545 ((+/-)-1-(2-(3-(2-cyano-4-(2-cyclopropyl-methoxy-ethoxy)phenoxy)-2-hydro xy-propyl-amino)-ethyl)-3-(4-hydrxy-phenyl) urea), an antagonist that possesses high beta1-/beta2-selectivity in the rat, and a range of cardio-selective and non-selective beta-adrenoceptor antagonists were examined to compare their ra...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00019-9
更新日期:1999-02-19 00:00:00
abstract::Acetylcholine is not only a neurotransmitter, but is found in a variety of non-neuronal cells. For example, the enzyme choline acetyltransferase (ChAT), catalyzing acetylcholine synthesis, is expressed by the colonic epithelium of different species. These cells release acetylcholine across the basolateral membrane aft...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.03.036
更新日期:2014-06-15 00:00:00
abstract::This study determined the in vitro functional profile of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3,4-dihydro-2-quinolinone monomethanesulfonate (OPC-14523) at rat and human serotonin (5-HT) 5-HT1A receptors and binding affinity of OPC-14523 at human frontocortical 5-HT1A receptors. OPC-14523 (1 microM...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2005.05.035
更新日期:2005-07-11 00:00:00
abstract::We investigated the acute and chronic effects of alpha 2-adrenoceptor and muscarinic receptor agonists on dihydropyridine-sensitive voltage-dependent Ca2+ channels in spinal cord-dorsal root ganglion cocultures. Clonidine and oxotremorine inhibited the voltage-dependent Ca2+ influx (42 +/- 2% and 35 +/- 6% with 100 mi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(93)90060-m
更新日期:1993-01-04 00:00:00
abstract::Experiments were conducted to explore the effects of Neuropeptide FF acting at spinal and supraspinal sites in models of chronic inflammatory or neuropathic pain and of acute pain. Neuropeptide FF was administered intrathecally (i.t.; 10.0, 25.0 and 50.0 nmol) or intracerebroventricularly (i.c.v.; 10.0, 12.5 and 15.0 ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00668-3
更新日期:2000-11-03 00:00:00
abstract::The influence of endothelin-1 on nociception induced by capsaicin was assessed in the mouse hindpaw. Local endothelin-1 injection (1 to 20 pmol/paw) 30 min prior to ipsilateral injection of capsaicin (0.1 microg/paw) increased, in a graded fashion, the time spent licking the injected paw. Maximal hyperalgesia was obta...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00281-7
更新日期:1998-06-12 00:00:00
abstract::Oxidative stress plays an important role in the pathogenesis of chronic obstructive pulmonary disease (COPD) and in the induction of corticosteroid (CS) insensitivity. Chronic ozone exposure leads to a model of COPD with lung inflammation and emphysema. Mitogen-activated protein kinase phosphatase-1 (MKP-1) may underl...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.10.003
更新日期:2014-12-05 00:00:00
abstract::Angiogenesis is critical for re-establishing blood supply to the ischemic myocardium after acute myocardial infarction (AMI). This study aimed to investigate the effects of morroniside on angiogenesis after AMI and explored associated proangiogenic mechanisms. A rat model of AMI was established by ligation of the left...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2020.172954
更新日期:2020-04-05 00:00:00
abstract::Acute treatment of rats with morphine (10 mg/kg) resulted in a marked reduction of motor response to inescapable electric footshock (EFS). Nalorphine (2mg/kg) antagonized this action of morphine. Pretreatment with synthetic ACTH 1-24 (10 IU) 60 min prior to testing also inhibited this morphine-induced reduction, where...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(75)90143-0
更新日期:1975-08-01 00:00:00
abstract::The influence of degradation by peptidases on concentration-response relationships for peptide agonists of the tachykinin and bombesin-like families was investigated. The combined presence of three peptidase inhibitors, phosphoramidon (1 microM), captopril (1 microM) and bestatin (100 microM), had no significant effec...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90520-g
更新日期:1990-02-06 00:00:00
abstract::Isolated rat diaphragms were treated with the oxime HI-6, 25 min after the start of soman exposure for 5, 15, 20 or 25 min. Recovery of neuromuscular transmission (NMT) was smaller and the subsequent spontaneous failure of NMT greater when soman exposure was longer. Diaphragms taken from anaesthetized atropinized soma...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90504-6
更新日期:1983-05-06 00:00:00
abstract::The regulation of acetylcholine (ACh) lifetime by acetylcholinesterase (AChE, EC 3.1.1.7) and butyrylcholinesterase (BuChE, EC 3.1.1.8) was evaluated in vitro in canine tracheal smooth muscle preparations. Selective inhibition of AChE by low concentrations of 1,5-bis(N-allyl-N,N-dimethyl-4-ammoniumphenyl)-pentane-3-on...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90772-i
更新日期:1991-11-19 00:00:00
abstract::The spinal cord dorsal horn contains neural mechanisms which can greatly facilitate pain. It is well established that excitatory amino acids, aspartate and glutamate, are involved in the spinal transmission of nociceptive information and in the development of hyperalgesia. In the present study, intrathecal (i.t.) admi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(96)00145-8
更新日期:1996-06-03 00:00:00
abstract::Grooming behaviour in mice was dose dependently increased by SK&F 38393 (1.87-30 mg/kg), whereas it was dose dependently decreased by RU 24926 (2.5-10 mg/kg) or LY 171555 (0.4-1.6 mg/kg) alone or combined with SK&F 38393 or apomorphine (0.39-6 mg/kg). The inhibitory effect of 0.75 mg/kg apomorphine on grooming behavio...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90141-0
更新日期:1988-10-26 00:00:00
abstract::Cats, sedated and paralyzed, showed a significant increase in body temperature after intravenous injection of morphine while animals with additional spinal blockade (C3) from injection of 2% lidocaine solution, did not. The results suggest that motor activity is not necessary for morphine-induced hyperthermia in the c...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(78)90113-9
更新日期:1978-06-01 00:00:00
abstract::The pharmacological profile of a new CCKA receptor antagonist, T-0632 [sodium (S)-1-(2-fluorophenyl)-2,3-dihydro-3-[(3-isoquinolinylcarbonyl) amino]-6-methoxy-2-oxo-1H-indole-3-propanoate], was examined in in vivo studies and compared with those of L-364, 718 [3S(-)-N-(2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1, 4-benzo...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(96)00473-6
更新日期:1996-09-26 00:00:00
abstract::Inhaled corticosteroids (ICS) are recommended treatments for all degrees of asthma severity and in combination with bronchodilators are indicated for COPD patients with a history of frequent exacerbations. However, the long-term side effects of glucocorticoids (GCs) may include increased risk of respiratory infections...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2020.173839
更新日期:2021-02-15 00:00:00
abstract::7-Nitroindazole (a selective neuronal nitric oxide (NO) synthase inhibitor) at 25 and 50 mg/kg, 30 min before the test, did not influence the electroconvulsive threshold. However, at 50 mg/kg, it enhanced the anticonvulsive activity of phenobarbital against maximal electroshock and did not affect that of carbamazepine...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01034-0
更新日期:1997-07-23 00:00:00
abstract::Nitric oxide (NO) is present in the exhaled breath of humans and other mammalian species. It is generated in the lower airways by enzymes of the nitric oxide synthase (NOS) family, although nonenzymatic synthesis and consumptive processes may also influence levels of NO in exhaled breath. The biological properties of ...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2005.12.069
更新日期:2006-03-08 00:00:00
abstract::Multidrug resistance phenotype in mammalian cells is often correlated with overexpression of P-glycoprotein or Multidrug Resistance-Associated protein (MRP(1)). Both proteins are energy-dependent drug efflux pumps that efficiently reduce the intracellular accumulation and hence the cytotoxicity of many natural cytotox...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00047-9
更新日期:2000-03-17 00:00:00
abstract::The behavioural and electrocortical power spectrum effects of tryptoline and the 5-hydroxy and 5-methoxy derivatives were studied after microinjection of the drugs into the third cerebral ventricle in freely moving rats. The three compounds produced a dose-dependent desynchronication in electrocortical activity with a...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90660-1
更新日期:1987-10-06 00:00:00
abstract::Long-term treatment with sodium barbital did not alter significantly the responsiveness of the isolated rat vas deferens to noradrenaline. However, three days after barbital withdrawal there was a 4.5-fold increase in the sensitivity and an enhanced maximum response to the neurotransmitter. Pharmacological analysis of...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90550-7
更新日期:1982-08-13 00:00:00
abstract::The present study was an attempt to answer the question whether the local anesthetic [3H]tetracaine labels sodium channels in mouse brain synaptosomes. Binding of [3H]tetracaine had a Kd of 0.19 microM and a Bmax ranging from 3.7 to 5.2 pmol/mg of protein. Local anesthetics other than tetracaine and cocaine-related co...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90530-9
更新日期:1987-11-10 00:00:00
abstract::Socially reared and isolation-reared rats treated chronically since weaning with alpha-flupenthixol showed elevated levels of spontaneous locomotor activity compared with control treated rats. However, chronic apomorphine treatment had no effect on spontaneous locomotor activity. Chronic alpha-flupenthixol treatment e...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(76)90019-4
更新日期:1976-05-01 00:00:00
abstract::Pyrrolidine dithiocarbamate (PDTC) can form a complex with metal ions and then act as a proteasome inhibitor, which leads to tumor cell apoptosis, and could therefore be developed as an anticancer agent. In our efforts to find factors that induce PDTC-mediated apoptosis of tumor cells, the effect of serum concentratio...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.09.048
更新日期:2010-12-15 00:00:00
abstract::Deprenyl, used clinically in Parkinson's disease, has multiple pharmacological effects which make it a good candidate to treat neurotoxicity. Thus, we investigated deprenyl's ability to attenuate methamphetamine-induced dopamine neurotoxicity. We also examined deprenyl's effect in changing markers associated with psyc...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.06.046
更新日期:2007-11-14 00:00:00
abstract::Nonalcoholic fatty liver disease (NAFLD) is the most common liver disease in the world. Despite the impact of this pathology in the population, nowadays there is no specific treatment for this disease, focusing its treatment on risks factors. However, it is imperative the existence of a specific treatment, due to this...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2019.172699
更新日期:2019-11-15 00:00:00
abstract::The present work is aimed at evaluating the protective effect of eugenol against in vitro nicotine-induced toxicity in murine peritoneal macrophages, compared with N-acetylcysteine. Eugenol was isolated from Ocimum gratissimum and characterized by HPLC, FTIR, (1)H NMR. To establish most effective protective support, w...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.09.019
更新日期:2009-11-25 00:00:00
abstract::The mechanisms of ryanodine-induced contractions were studied in strips of femoral arteries from spontaneously hypertensive rats (SHR) and normotensive Wistar-Kyoto rats (WKY). Ryanodine (30 nM to 30 microM) alone contracted arterial strips in a dose-dependent manner. The maximum contraction in SHR was about 5 times g...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90383-2
更新日期:1994-03-11 00:00:00
abstract::In vitro effects of d,l-methadone and morphine on [3H]serotonin (3H-5-HT) uptake in rat periaqueductal gray (PAG) slices were investigated. Only methadone had a significant inhibitory effect on 3H-5-HT uptake which was significantly enhanced by naloxone. The systemic administration of methadone did not affect 3H-5-HT ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(79)90030-x
更新日期:1979-10-26 00:00:00