Abstract：
:Substituted benzamides such as metoclopramide, cisapride, zacopride, renzapride or BRL 20627, stimulate intestinal motility in various species. As they are antagonists at 5-HT3 and agonists at 5-HT4 receptors and as both mechanisms could potentially contribute to their gastrointestinal prokinetic effect, the underlying mechanism is unclear. To clarify this, the effect of some substituted benzamides on gut motility was investigated in the isolated guinea pig ileum using the Trendelenburg technique, in which pressure-induced peristaltic contractions are measured. All benzamides stimulated the peristaltic reflex with the rank order of potency: renzapride greater than cisapride greater than BRL 20627 greater than (+/-)-zacopride greater than metoclopramide. ICS 205-930, granisetron and 2-methyl-5-HT did not change the peristaltic response. 5-HT and 5-methoxytryptamine potently mimicked the effect of the benzamides. The effect of 5-HT was not blocked by ICS 205-930 (10(-7) M). These results indicate that the Trendelenburg preparation is suitable for the investigation of intestinal prokinetic effects of the substituted benzamides. Furthermore, the results suggest that the intestinal effect of benzamides results from activation of 5-HT4 receptors rather than from blockade of 5-HT3 receptors.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Buchheit KH,Buhl Tdoi
10.1016/0014-2999(91)90821-7subject
Has Abstractpub_date
1991-11-26 00:00:00pages
203-8issue
2eissn
0014-2999issn
1879-0712pii
0014-2999(91)90821-7journal_volume
205pub_type
杂志文章abstract：:We determined the role of high-grade inflammation on endothelial function and its association with biomarkers of endothelial dysfunction in collagen-induced arthritis. Sprague-Dawley rats were divided into a control (n = 12) or collagen-induced arthritis (CIA; n = 21) group. To induce arthritis, Bovine-type-II collage...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172786
更新日期：2019-12-15 00:00:00
abstract：:Cutaneous arteries are known to constrict in response to cooling via α2C-adrenoceptors. The involvement of α1-adrenoceptors in the cooling response has also recently been suggested by in vivo studies in mice. The present study was thus aimed to confirm it in the isolated mouse cutaneous plantar artery. Changes in vess...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.08.014
更新日期：2014-11-05 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：:The influence of (+/-)-tamsulosin, a selective alpha 1A-adrenoceptor antagonist, on the positive inotropic effect and the accumulation of inositol phosphates that are induced via alpha 1-adrenoceptors was studied in comparison with that of another alpha 1A-adrenoceptor ligand oxymetazoline in the rabbit ventricular my...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00442-6
更新日期：1996-10-03 00:00:00
abstract：:Painless myocardial infarction is a serious complication of diabetes. The present study examined whether cardiac nociception was altered in the streptozotocin-induced diabetic rat model by assessing intrapericardial capsaicin-evoked electromyography (EMG) responses in the spinotrapezius muscle. Somatic sensitivities t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.10.073
更新日期：2011-01-25 00:00:00
abstract：:Amphetamine elicits its locomotor-activating and drug-reinforcing effects by releasing the catecholamines dopamine and norepinephrine into the synapse. Amphetamine is a substrate of the plasmalemmal transporters for both dopamine and norepinephrine. As such, it binds to the transporters in conjunction with Na+ and Cl-...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2003.08.059
更新日期：2003-10-31 00:00:00
abstract：:The actions of a purified Helicobacter pylori lipopolysaccharide (3 mg x kg(-1), i.v.) on rat gastric antral and duodenal microvascular integrity (determined as radiolabelled albumin leakage) and the expression of the inducible nitric oxide (NO) synthase (iNOS; assessed by the citrulline assay) were investigated 4 h a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01008-1
更新日期：2001-05-25 00:00:00
abstract：:Increasing stimulation frequency and monensin were utilized in attempts to enhance Na+ influx and thereby elicit the maximum rate of ouabain-sensitive 86Rb+ uptake in rat atrial muscle. Increasing stimulation frequency between 0 and 9 Hz enhanced the rate of ouabain-sensitive 86Rb+ uptake, whereas the uptake rate appe...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90338-9
更新日期：1986-09-23 00:00:00
abstract：:Loss of body weight was proved to be a convenient and reliable way to predict the degree of reserpine-induced amine depletion after i.p. injections of reserpine (2.5, 5 and 10 mg/kg) and it thus helps reduce variability. Two populations of animals were sharply distinguished lying on either side of the 5% cutoff point ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90327-1
更新日期：1975-05-01 00:00:00
abstract：:The present study aims to investigate whether azithromycin reverses P-glycoprotein-dependent anticancer drug resistance in vitro and modifies the hepatobiliary excretion of doxorubicin, a substrate for P-glycoprotein in vivo. Azithromycin increased dose-dependently the intracellular accumulation of doxorubicin in adri...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.11.035
更新日期：2004-01-26 00:00:00
abstract：:Natural purines like ATP, ADP and adenosine have crucial roles in platelet physiology. This knowledge has been significant in drug development and today ADP receptor antagonists are widely used for prevention of thrombotic events following myocardial infarction and ischaemic stroke. Recent studies have shown that a pu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172428
更新日期：2019-08-15 00:00:00
abstract：:Guinea pig neurotensin differs from other mammalian neurotensin by the substitution of proline by serine at position 7. [Ser7]neurotensin produced a concentration-dependent contraction of the guinea pig oesophagus and rat fundus, a biphasic effect (initial relaxation followed by more sustained contraction) on the guin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90293-7
更新日期：1987-08-21 00:00:00
abstract：:Although hypoxia induces adrenomedullin gene expression in cultured rat cardiac myocytes, it is still unknown whether oxidative stress is involved in the hypoxia-induced adrenomedullin production. We investigated whether oxidative stress might participate in hypoxia-induced adrenomedullin secretion and whether adrenom...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01462-5
更新日期：2002-02-01 00:00:00
abstract：:Choline displaced [3H]QNB binding from rat brain muscarinic receptors competitively, (Ki = 460 microM) but it was only 1/1000th as potent as ACh. Deanol was an extremely weak displacer of [3H]QNB binding while hemicholinium-3 was 50 times more potent than choline. Although brain levels of choline are well below its Ki...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90012-8
更新日期：1979-09-15 00:00:00
abstract：:The effect of omega-conotoxin on opiate analgesia and withdrawal syndrome was investigated in rats. omega-Conotoxin given i.c.v. and i.p. caused weak analgesia in the tail-flick test. When the toxin (20 ng/rat) was given i.c.v. immediately before morphine (1.5 micrograms/rat i.c.v.) the resultant analgesic effect was ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90149-x
更新日期：1992-07-21 00:00:00
abstract：:Calcitonin gene-related peptide (CGRP), a 37-amino acid neuropeptide, is found in the central nervous system as well as in the heart. CGRP shows high sequence homology with amylin, salmon calcitonin, and adrenomedullin. This study aimed to investigate the effect of CGRP on atrial hemodynamics and atrial natriuretic pe...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.10.020
更新日期：2004-01-12 00:00:00
abstract：:To determine if an Ag(+)-induced contracture is associated with the Ca(2+)-induced Ca2+ release mechanism in the sarcoplasmic reticulum, effects of Ca(2+)-induced Ca2+ release modulators on the Ag(+)-induced contracture were studied with single fibers of frog toe skeletal muscle. The fiber treated with 1 mM caffeine c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(95)90036-5
更新日期：1995-03-16 00:00:00
abstract：:The aim of the research was to characterize muscarinic receptors of bovine ciliary muscle and to investigate the desensitization process. The role of protein kinase C was analyzed. The results show that muscarinic receptors of bovine ciliary muscle have the pharmacological characteristics of the M3 subtype. Acute expo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)10122-4
更新日期：1997-07-09 00:00:00
abstract：:The effects of 3-(3-iodo-4-aminobenzyl)-8-(4-oxyacetate)-1-propylxanthine (I-ABOPX; BW-A522), which has nanomolar affinity for the recently cloned human and sheep adenosine A3 receptor, on the putative A3 receptor mediated hypotensive response to N6-2-(4-aminophenyl)ethyl adenosine (APNEA) in the rat have been investi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90604-1
更新日期：1994-02-03 00:00:00
abstract：:The role of pertussis toxin-sensitive G proteins on the alpha 2-adrenoceptor and mu-opioid receptor-mediated inhibition of the efferent function of capsaicin-sensitive neurones was investigated in guinea-pig atria pretreated with guanethidine. In the presence of atropine, CGP 20712A (2-hydroxy-5-(2-[hydroxy-3-(4-[(1-m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90444-9
更新日期：1992-06-17 00:00:00
abstract：:The suppressing effect of acamprosate (calcium-acetyl homotaurinate) on alcohol drinking is well established; however, little is known about its effects upon the alcohol-induced withdrawal syndrome. Male Wistar rats received as a sole drinking fluid a 20% (v/v) alcohol solution for one week. Animals consumed on averag...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00175-6
更新日期：1996-06-03 00:00:00
abstract：:Naloxone, a competitive antagonist of opioid receptors, and placebo (dextrose 5% in water (D5W) were administered on separate days to healthy normotensive (NT) male volunteers and to male patients with essential hypertension (HT). A single-blind, placebo-controlled, cross-over design was employed. Increasing doses of ...
journal_title：European journal of pharmacology
pub_type： 临床试验,杂志文章
doi：10.1016/0014-2999(86)90048-8
更新日期：1986-07-31 00:00:00
abstract：:We have studied the effects of benextramine on the U46619 (11 alpha,9 alpha-epoxymethano-15S-hydroxy-prosta-5Z,13E-dienoic acid)-mediated contraction of the rat isolated small mesenteric artery. U46619 (10 nM-10 microM) produced a concentration-dependent contraction of the small mesenteric artery. The selective prosta...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00040-4
更新日期：1996-04-11 00:00:00
abstract：:The pharmacological activity of N-methyl-actinodaphnine, isolated from Illigera luzonensis, was determined by functional and binding experiments with peripheral tissues. In a functional study, N-methyl-actinodaphnine was a simple competitive antagonist of contractions elicited by phenylephrine (pA2 = 7.11) in rat thor...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00135-8
更新日期：1995-06-06 00:00:00
abstract：:The effects of acute treatment with sibutramine on the peripheral sympathetic neurotransmission in vas deferens of young rats were still not evaluated. Therefore, we carried out this study in order to verify the effects of acute sibutramine treatment on the neuronal- and exogenous agonist-induced contractions of the y...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.05.035
更新日期：2014-09-05 00:00:00
abstract：:The effects of dopamine (DA) and of two selective DA DA1 agonists (SKF 38393 and SKF 82526) on adenylate cyclase activity were studied with human kidney cortex membrane preparations. DA elicited a dose-related stimulation of adenylate cyclase activity with an EC50 of 60 microM. The selective DA DA1 antagonist SCH 2339...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90667-x
更新日期：1988-05-10 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：: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：:Microinjections of substance P (SP, 100 pmol) into the dorsal raphe nucleus (DRN) in conscious rats increased blood pressure and heart rate for 30-40 min. Concomitantly, the extracellular levels of 5-hydroxytryptamine (5-HT) in the ventral hippocampus, monitored by microdialysis, increased by 30% for 20 min compared w...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90194-9
更新日期：1992-08-06 00:00:00
abstract：:Glucocorticoids inhibit inducible-type NO synthase activity in a variety of cell types. We report here that proteins recovered from the medium of dexamethasone-treated J774 macrophages (1, 10, 100 microg/ml) inhibited lipopolysaccharide-stimulated nitrite generation by 10.0 +/- 3.0%, 32.3 +/- 5.3% and 55.0 +/- 6.0%, r...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01361-7
更新日期：1997-11-19 00:00:00
