Abstract:
:The potency and site of action of Ro5-3663 as a GABA antagonist were investigated in the rat cuneate slice in vitro. A Schild plot for Ro5-3663 was clearly non-linear but enabled a pA2 value of 3.97 to be calculated. Combination studies using the 'classical' GABA antagonists bicuculline and picrotoxin indicated that Ro5-3663 acted at a separate site from bicuculline, but may share a common site with picrotoxin.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Harrison NL,Simmonds MAdoi
10.1016/0014-2999(83)90064-xsubject
Has Abstractpub_date
1983-01-28 00:00:00pages
155-8issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(83)90064-Xjournal_volume
87pub_type
杂志文章abstract::Low doses of BHT 920, LY 171555 and (+)3PPP, three dopamine agonists selective for D-2 receptors, induced yawning in rats. This effect was reduced by the selective D-1 antagonist SCH 23390 but the antagonism did not exceed a 50% reduction from the control values. In contrast, the selective D-2 antagonist (-)sulpiride ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90162-2
更新日期:1987-02-10 00:00:00
abstract::1,8-Cineole (also known as eucalyptol) is a monoterpene that occurs naturally in many aromatic plants, 1,8-cineole has been reported to ameliorate dysfunction of endothelial cells. However, the mechanism of action of 1,8-cineole is incompletely understood. We investigated the protective effect of 1,8-cineole on lipopo...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2016.07.039
更新日期:2016-10-15 00:00:00
abstract::Chronic Obstructive Pulmonary Disease (COPD) is a major incurable global health burden and is the 4th leading cause of death worldwide. It is believed that an exaggerated inflammatory response to cigarette smoke causes progressive airflow limitation. This inflammation, where macrophages, neutrophils and T lymphocytes ...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2015.03.029
更新日期:2015-07-15 00:00:00
abstract::A major limitation of cancer treatment is the ability of cancer cells to develop resistance to chemotherapeutic drugs, by the establishment of multidrug resistance. Here, we characterize MC70 as ABC transporters inhibitor and anticancer agent, alone or with chemotherapy. MC70 was analyzed for its interaction with ABCB...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.08.025
更新日期:2011-11-16 00:00:00
abstract::Sodium nitroprusside produced a dose-dependent increase in extracellular levels of cGMP in the cerebellar cortex in vivo. This was independent of nitric oxide synthase activity. The metalloporphyrins zinc-protoporphyrin-IX, tin-protoporphyrin-IX and zinc-deuteroporphyrin-IX,2,4-bis glycol prevented the increase in cGM...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(94)90149-x
更新日期:1994-05-17 00:00:00
abstract::Neuropathic pain is among the most common and difficult-to-treat types of chronic pain and is associated with sodium channel malfunction. The sodium channel blocker ralfinamide has exhibited potent analgesic effects in several preclinical pain models and in patients with mixed neuropathic pain syndromes (Phase II tria...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2018.01.041
更新日期:2018-03-15 00:00:00
abstract::We investigated the influence of inhibition of nitric oxide (NO) synthase, using NG-nitro-L-arginine (L-NNA) or NG-mono-methyl-L-arginine (L-NMMA), and the effects of exogenous donor of NO, such as glyceryl trinitrate (GTN), on the healing of chronic gastric ulcers induced by acetic acid, on gastric blood flow around ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90997-v
更新日期:1993-08-03 00:00:00
abstract::A very strong epidemiological link exists between obesity, the metabolic syndrome, diabetes and diabetes-associated cardiovascular pathologies. For this reason the peripheral effects of the centrally-acting satiety adipokines, adiponectin and leptin, and of non-adipose-derived hormones with similar effects, like ghrel...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.11.052
更新日期:2007-03-08 00:00:00
abstract::Plasma concentrations of unchanged dihydroergotamine (DHE) were measured in beagle dogs on days 1 and 7 of a 1 week treatment with daily oral doses of DHE. Responses to both 5-HT and noradrenaline were monitored isometrically on spiral strips from saphenous arteries and femoral veins removed 24 and 72 h after the last...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90601-5
更新日期:1983-04-22 00:00:00
abstract::The present study was undertaken to evaluate the effects of 5-hydroxytryptamine on pulmonary vascular resistances and vascular permeability with respect to the 5-hydroxytryptamine receptor subtypes. Left lower lobe of lungs isolated from the dog was perfused with constant heights of arterial and venous blood reservoir...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90232-x
更新日期:1989-05-02 00:00:00
abstract::Parkinson's disease is a neuropathological disorder involving the degeneration of dopamine neurons in the substantia nigra, with the resultant loss of their terminals in the striatum. This dopamine loss causes most of the motor disturbances associated with the disease. One animal model of Parkinson's disease involves ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)01260-2
更新日期:2001-10-05 00:00:00
abstract::The interference of azelastine with pleurisy induced by antigen was investigated in actively sensitized rats. The antigenic challenge (ovalbumin, 12 micrograms/cavity) caused early plasma leakage, which peaked within 4 h, accompanied by intense neutrophil infiltration. Pleural exudate decayed 24 h after antigen provoc...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90522-r
更新日期:1991-05-17 00:00:00
abstract::Precipitated withdrawal in rats chronically exposed to delta 9-tetrahydrocannabinol, the major psychoactive principle of the marijuana plant, was unequivocally demonstrated for the first time using a selective antagonist, SR 141716A (N-(piperidin-1-yl)-5-(4-chlorophenyl)-1(2,4- dichloro-phenyl)-4-methyl-1H-pyrazole ca...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00447-s
更新日期:1995-08-25 00:00:00
abstract::The myocardial effects of g-strophanthin and the partial beta 1-adrenoceptor agonist xamoterol were compared to the effects of isoprenaline in the isolated spontaneously beating rabbit heart. Xamoterol and g-strophanthin both produced a distinct maximum increase in contractility as shown by the increase in isotonic co...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90792-2
更新日期:1986-06-24 00:00:00
abstract::Corticotropin-releasing factor (CRF) plays a major role at the level of the hypothalamus and pituitary to control the body's response mechanisms to stressful stimuli. The recent discovery of CRF outside the central nervous system suggests that CRF may well play a similar role in peripheral tissues, most likely in a pa...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/s0014-2999(97)00057-5
更新日期:1997-03-26 00:00:00
abstract::The present study was aimed to evaluate the behavioral and biochemical effects of macranthol, a triphenyl lignan isolated from Illicium dunnianum. To this aim, mice were treated with macranthol (10, 20 and 40 mg/kg) and then subjected to the forced swimming test, tail suspension test and chronic unpredictable mild str...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.03.010
更新日期:2013-05-05 00:00:00
abstract::Administration of ovalbumin by aerosol to sensitised rats produced a rapid (15 min) protein exudation in different airway tissues, as determined by Evans blue staining. This was associated with marked mast cell degranulation determined by histological examination, with there being no difference between mucosal and con...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)01093-7
更新日期:2001-08-24 00:00:00
abstract::In utero exposure of rodents to valproic acid (VPA) has been proposed to induce an adult phenotype with behavioural characteristics reminiscent of those observed in autism spectrum disorder (ASD). Our previous studies have demonstrated the social cognition deficits observed in this model, a major core symptom of ASD, ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.01.050
更新日期:2014-03-15 00:00:00
abstract::Co-dergocrine (Hydergine), an ergot preparation composed of four dihydrogenated peptide ergot alkaloids (dihydroergocornine, dihydroergocristine, dihydro-alpha-ergokryptine, dihydro-beta-ergokryptine, 3:3:2:1), has been reported to exert in vivo effects suggesting an interaction with dopaminergic systems. The present ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90312-0
更新日期:1982-12-24 00:00:00
abstract::The mechanisms underlying the capsaicin-induced relaxation of the acetylcholine- as well as KCl-contraction were studied by measuring isometric force and phosphorylation of 20-kDa regulatory light chain subunit of myosin (MLC(20)) in ileal longitudinal smooth muscles of rats. Capsaicin relaxed acetylcholine- and KCl-s...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.01.014
更新日期:2004-03-08 00:00:00
abstract::We studied the interaction of S-methylisothiourea (a selective inducible nitric oxide synthase inhibitor) with rofecoxib (a selective cyclooxygenase-2 inhibitor) and mefenamic acid (a non-selective cyclooxygenase inhibitor) in adjuvant-induced arthritis in female albino Wistar rats, applying the isobolographic analysi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.10.047
更新日期:2007-02-05 00:00:00
abstract::Cannabinoid CB(2) receptor is reported to be expressed in varying amounts in different human immune subpopulations. To examine the expression pattern of CB(2) in the mouse, immune cell subpopulations were purified and studied by semiquantitative Reverse Transcription-Polymerase Chain Reaction (RT-PCR). CB(2) mRNA was ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)01122-0
更新日期:2001-07-06 00:00:00
abstract::The new antisecretory drug, telenzepine (4,9-dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)acetyl]-10H-thieno-[3,4 - b][1,5]benzodiazepin-10-one), was investigated for its inhibition of functionally intact muscarinic receptors involved in gastric acid secretion in rabbit fundic glands, perfused mouse stomach in vitro, p...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90498-4
更新日期:1985-06-07 00:00:00
abstract::Intake of nicotine has been related in many cases to acute or chronic hypertension. Using the patch-clamp technique the effect of nicotine on voltage-dependent K+ channel currents in rat tail artery smooth muscle cells was studied. Nicotine at concentrations of 1-100 microM or 0.3-3 mM increased or decreased, respecti...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00833-4
更新日期:1999-01-08 00:00:00
abstract::Peroxisome proliferator-activated receptor gamma (PPARgamma) is a ligand-activated transcription factor belonging to the nuclear hormone receptor superfamily. PPARgamma regulates several metabolic pathways by binding to sequence-specific PPAR response elements in the promoter region of target genes, including lipid bi...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2005.12.048
更新日期:2006-03-08 00:00:00
abstract::Recent studies have shown that many organophosphates can bind competitively and noncompetitively to membrane muscarinic receptors. The present study investigated the responses of the rat aortic rings to diisopropyl-flurophosphate (DFP), an organophsophorus cholinesterase inhibitor, and the possible involvement of musc...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00629-4
更新日期:2000-09-22 00:00:00
abstract::A close relationship between the renin-angiotensin system and the pathophysiology of diabetic retinopathy has been suggested, several angiotensin II type 1 receptor (angiotensin AT1 receptor) antagonists being effective in animal models. Therefore, we examined the efficacy of an angiotensin AT1 receptor antagonist, ol...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2005.02.047
更新日期:2005-04-11 00:00:00
abstract::The bisquaternary compound dequalinium has been tested for its ability to inhibit the loss of K+ which angiotensin II causes in guinea-pig hepatocytes and which occurs through apamin-sensitive Ca(2+)-activated K+ (SKCa) channels. Dequalinium blocked angiotensin II-evoked K+ loss with an IC50 of 1.5 +/- 0.1 microM and ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90590-e
更新日期:1993-05-19 00:00:00
abstract::Endogenous hydrogen sulfide is produced by cystathionine-γ-lyase and cystathionine-β-synthase in a variety of tissues and has recently been implicated in the regulation of cardiac functions. Acceleration of the heart rate in response to catecholamines is impaired in patients with cirrhosis. The present study was aimed...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.09.039
更新日期:2012-12-05 00:00:00
abstract::More recently, arsenic trioxide (ATO), was integrated into acute promyelocytic leukemia (APL) treatment, showing high efficacy and tolerability in patients with both ATRA-sensitive and ATRA-resistant APL. ATO could induce apoptosis at relatively high concentrations (0.5 to 2.0 micromol/L) and partial differentiation a...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.04.040
更新日期:2014-08-05 00:00:00