Abstract：
:Cetiedil is a potent blocker of acetylcholine and choline fluxes. Several analogs of this compound have been synthesized and their effect on acetylcholine (ACh) and choline fluxes in synaptosomes and on ACh uptake in synaptic vesicles have been studied. The effects of these analogs were compared to those of other drugs acting on cholinergic functions. All these compounds were also studied in relation to the ACh translocating properties of the mediatophore, a protein recently purified from cholinergic nerve membranes and probably involved in the final step of release. We thus obtained a pattern of drug action for the three functions under study. The patterns of drug action on ACh release from synaptosomes or proteoliposomes were similar and clearly different from those for either synaptosomal choline transport or vesicular ACh uptake. In addition, the main outlines of the structure-function relationship for each of the functions studied, are described for cetiedil analogs.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Gaudry-Talarmain YM,Diebler MF,Robba M,Lancelot JC,Lesbats B,Israël Mdoi
10.1016/0014-2999(89)90355-5subject
Has Abstractpub_date
1989-08-03 00:00:00pages
427-33issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(89)90355-5journal_volume
166pub_type
杂志文章abstract：:The main purpose of this study was to compare in vitro pharmacological properties of human αCGRP (CGRP) and a recently discovered metabolically stable CGRP analogue, SAX, in isolated rat and human artery segments. In rat, CGRP and SAX induced similar vasodilatory responses in isolated mesenteric artery with the potenc...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.04.007
更新日期：2018-06-15 00:00:00
abstract：:We have studied the pharmacological effects of (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and the enantiomers of (RS)-2-amino-3-(3-hydroxy-1,2, 5-thiadiazol-4-yl)propionic acid (TDPA) on cloned human excitatory amino acid transporter subtypes 1, 2 and 3 (EAAT1-3) expressed in Cos-7 cells. Wh...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00625-7
更新日期：2000-10-06 00:00:00
abstract：:Removal of the epithelium increased the responsiveness of isolated guinea-pig trachea to the contractile effects of endothelin. This phenomenon was observed in the presence of indomethacin (5 microM), captopril (10 microM), bacitracin (20 micrograms/ml) or leupeptin (50 microM), but was inhibited by phosphoramidon (10...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90114-3
更新日期：1989-11-21 00:00:00
abstract：:Infusion of α,β-methylene ATP (α,β-meATP) into murine neck muscle facilitates brainstem nociception. This animal experimental model is suggested to be appropriate for investigating pathophysiological mechanisms in tension-type headache. It was hypothesized that d-lysine acetylsalicylic acid (ASA, aspirin®) reverses th...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.10.008
更新日期：2011-12-30 00:00:00
abstract：:The aims were to test whether 2 weeks treatment with the beta2-adrenoceptor agonist, salbutamol, or the alpha1-adrenoceptor antagonist, doxazosin, could correct nerve blood flow and conduction velocity deficits in 8 week streptozotocin-diabetic rats and to examine neurovascular mechanisms using co-treatment with the n...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01533-1
更新日期：1998-02-19 00:00:00
abstract：:Induction of inducible nitric oxide synthase (iNOS) expression and nitric oxide (NO) production is thought to have beneficial immunomodulatory effects in acute and chronic inflammatory disorders. In Raw 264.7 cells stimulated with lipopolysaccharide (LPS) to mimic inflammation, withaferin A inhibited LPS-induced expre...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.09.017
更新日期：2008-12-03 00:00:00
abstract：:Nonalcoholic steatohepatitis (NASH) is one of the most common liver diseases involving chronic accumulation of fat and inflammation, often leading to advanced fibrosis, cirrhosis and carcinoma. However, the pathological mechanism for this is unknown. GPR120/FFAR4 has been recognized as a functional fatty acid receptor...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.11.046
更新日期：2018-02-05 00:00:00
abstract：:N-Phthaloyl gamma-aminobutyric acid, a new gamma-aminobutyric acid derivative synthesized in this laboratory, has been found to possess anticonvulsant, antinociceptive and antistress activities. Effects of this derivative on gastric lesions induced by aspirin and ethanol were studied in rats. N-Phthaloyl gamma-aminobu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90298-i
更新日期：1992-08-25 00:00:00
abstract：:Plasma adrenaline mainly originated from adrenaline-containing cells in the adrenal medulla, while plasma noradrenaline reflects the release from sympathetic nerves in addition to the secretion from noradrenaline-containing cells in the adrenal medulla. The present study was undertaken to characterize the source of pl...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.02.069
更新日期：2008-05-31 00:00:00
abstract：:Curcumin, main compound obtained from rizhoma of Curcuma longa, shows antitumoral, antioxidant, anticarcinogenic and gastric protective properties. Recently, it has been demonstrated that curcumin exerts its gastric protective action due to an increase in gastric nitric oxide (NO) levels. However, it is unknown whethe...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.02.030
更新日期：2014-05-05 00:00:00
abstract：:Langendorff preparations of Sprague-Dawley rat hearts were perfused with calcium-free Krebs solution of pH 7.48 (control), 7.26 (acidosis) or 7.69 (alkalosis) containing either adrenaline or potassium. The responses of the force of contraction, coronary perfusion pressure and heart rate to graded doses of calcium prec...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90411-i
更新日期：1991-04-10 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00129-9
更新日期：1995-06-12 00:00:00
abstract：:We have previously proposed that pro-inflammatory cytokines and nitric oxide (NO) contributed to reversible myocardial depression in patients with sepsis and congestive heart failure. Sepsis and heart failure are also associated with refractoriness to beta-adrenoceptor agonists. Therefore, the chronotropic effects of ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00912-0
更新日期：1997-02-12 00:00:00
abstract：:Taurine influx in the perfused rat heart was characterized and the effect of isoproterenol on this process determined. Hearts were perfused by the Langendorff technique with [3H]-taurine in a non-recirculating system. The rate of taurine influx was constant for at least 20 min and the process was saturable. A Km of 45...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90163-2
更新日期：1978-04-15 00:00:00
abstract：:Adenosine added to isolated electrically driven preparations of human ventricular heart muscle antagonized the positive inotropic effect of isoprenaline (mean EC50 19 mumol 1(-1), n = 9). Similar effects were observed with the adenosine receptor agonist (-)-N6-phenylisopropyladenosine (mean EC50 0.5 mumol 1(-1), n = 7...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90170-0
更新日期：1985-10-22 00:00:00
abstract：:The ligand preferences of recombinant NR1 homomeric and NR1-NR2 heteromeric NMDA receptors were examined by homogenate binding assay. The binding affinities for most ligands were similar to those reported for native NMDA receptors. The order of affinity for [3H]glutamate was NR1-NR2B > NR1-NR2A approximately NR1-NR2D ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90058-2
更新日期：1994-08-16 00:00:00
abstract：:Using microdialysis in rat prefrontal cortex, we found that 1 mg/kg of the stimulant methylphenidate and the non-stimulant atomoxetine, two widely used treatments for Attention Deficit/Hyperactivity Disorder (ADHD), produce robust increases in the extracellular levels of histamine, which plays a key role in attention,...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.11.048
更新日期：2007-03-08 00:00:00
abstract：:Previous investigations in our laboratory revealed subsensitivity of right ventricular tissue, isolated from one month STZ-diabetic rats, to the inotropic effects of isoproterenol. The present study was concerned with the characterization of this subsensitivity phenomenon. Observations of supersensitivity to methoxami...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90311-6
更新日期：1987-04-29 00:00:00
abstract：:The present study was designed to investigate the antinociception of spirocyclopiperazinium salt compound LXM-10-M (2,4-dimethyl-9-β-m-hydroxyphenylethyl-3-oxo-6, 9-diazaspiro [5.5] undecane chloride) in thermal and chemical pain models, and further to explore the molecular target and potential signal pathway. We asse...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.11.056
更新日期：2016-01-05 00:00:00
abstract：:Baicalein was a major bioactive flavonoid derived from Radix Scutellariae in Xiao-Chai-Hu-Tang which was commonly used to treat chronic hepatitis and liver fibrosis in China. The aim of this study was to assess whether chronic baicalein administration could prevent liver fibrosis induced by carbon tetrachloride (CCl(4...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.01.002
更新日期：2010-04-10 00:00:00
abstract：:We reported previously that 18 compounds varying in general anesthetic potency by up to 66 000-fold inhibited, at anesthetic concentrations, the metabolism of arachidonic acid and aminopyrine by cytochrome P450 monooxygenases in rat liver microsomes. Now, we report that P450-mediated para-hydroxylation of aniline is m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(95)00022-4
更新日期：1995-10-06 00:00:00
abstract：:Sprague-Dawley rats received oral doses of enalapril maleate (5 mg/kg), a potent, nonsulfhydryl, angiotensin converting enzyme inhibitor, or saline. Sixty min later, morphine sulfate, 5 mg/kg, or saline was injected subcutaneously. Response to a thermal stimulus was monitored before and up to 5 h ter morphine injectio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90607-1
更新日期：1984-02-17 00:00:00
abstract：:Angiotensin AT1 receptor antagonists represent a novel class of cardiovascular drugs. In conscious, normotensive rats, irbesartan ((2-n-butyl-3-[(2'-(1H-tetrazol-5-yl)-biphenyl-4-yl) methyl]-1,3-diaza-spiro[4,4]non) and losartan ((2 n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl -4-yl) methyl] imid...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00983-2
更新日期：1999-02-19 00:00:00
abstract：:We previously reported that both nitric oxide (NO) generated from NO synthase by bombesin and NO generated from SIN-1 (NO donor) activate the brain cyclooxygenase (COX) (COX-1 for bombesin), thereby eliciting the secretion of both catecholamines (CA) from the adrenal medulla by brain thromboxane A(2)-mediated mechanis...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.01.005
更新日期：2012-03-15 00:00:00
abstract：:This study evaluated the contribution of supraspinal opioid receptors to the production of antinociception, in the rat. I.c.v. administration of a selective mu- (DAMGO) and a selective delta- (DPDPE), but not a selective kappa- (U50,488H) opioid receptor agonist, produced significant dose-dependent increase in mechani...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90905-6
更新日期：1991-12-03 00:00:00
abstract：:Mouse gastric fundus strips were relaxed by ultraviolet light (UV) irradiation, exogenous nitric oxide (NO), isoproterenol, S-nitrosoglutathione, S-nitroso-L-cysteine and S-nitroso-N-acetyl-penicillamine. Glutathione did not affect relaxations in response to UV irradiation, exogenous NO and isoproterenol while inhibit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02098-8
更新日期：2002-08-30 00:00:00
abstract：:We now describe the preparation and characterization of a novel radioligand, 2-[125I]iodo-5-methoxy-carbonylamino-N-acetyltryptamine (2-[125I]MCA-NAT), with high affinity and pharmacological selectivity for melatonin ML2 receptor sites. 2-[125I]MCA-NAT was prepared by introducing an [125I]iodine molecule on carbon 2 o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00870-5
更新日期：1996-04-22 00:00:00
abstract：:Vancomycin (VCM) is a first-line antibiotic for serious infections caused by methicillin-resistant Staphylococcus aureus. However, nephrotoxicity is one of the most complaint in VCM therapy. We previously reported that VCM induced apoptosis in a porcine proximal tubular epithelial cell line (LLC-PK1), in which mitocho...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.02.025
更新日期：2017-04-05 00:00:00
abstract：:Effects of nicotine, and nicotine+vitamin E on glutathione reductase (Glutathione: NADP(+) oxidoreductase, EC 1.8.1.7) activity in the muscle, heart, lungs, testicles, kidney, stomach, brain and liver tissues were investigated in vivo and also in vitro. The groups were: nicotine [0.5 mg/kg/day, intraperitoneal (i.p.)]...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.10.008
更新日期：2007-01-12 00:00:00
abstract：:Morphine is known to produce mydriasis in mice. We have found that enkephalins caused a similar effect. Morphine was twice as active as D-Ala-D-Leu-enkephalin (BW-180C), 5 times as active as Met-enkephalin and 7 times as active as Leu-enkephalin. The time course of the effect was shortest for the enkephalins ( t 1/2 =...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90402-1
更新日期：1980-07-25 00:00:00
