Abstract：
:The effects of the new 3,4-disubstituted furoxan, CHF 2206, on vascular tone, platelet aggregation and platelet cyclic 3',5'-guanosine monophosphate (cGMP) levels were investigated. The compound was a potent inhibitor of rabbit aortic ring contraction induced by norepinephrine, the stable prostaglandin F2 alpha analogue, U-46619, and KCl; this activity was independent of endothelium integrity. When pre-incubated with platelet-rich plasma, CHF 2206 potently reduced in a dose-dependent manner the aggregation induced by the threshold aggregating concentration of collagen, ADP or platelet activating factor (PAF). In the same experimental conditions, the test compound increased the platelet cGMP levels and this rise was clearly associated with the inhibition of platelet aggregation. Moreover, 3-isobutyl-1-methyl-xanthine (IBMX) 5 microM potentiated the antiaggregating activity of CHF 2206. These results indicate that the increase in cGMP plays a key role in the CHF 2206-elicited responses. Oxyhemoglobin reduced all the pharmacological actions of the test compound. This evidence, along with the capacity of CHF 2206 to cause inorganic nitrite production in the presence of platelet-rich plasma, strongly suggests that nitric oxide (NO) may be a common reactive intermediate responsible for the effects induced by the drug. In conclusion, the furoxan derivative CHF 2206 exerts a potent antiaggregating and vasodilating activity with a pharmacological profile similar to the one described for NO-donating pro-drugs.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Civelli M,Caruso P,Giossi M,Bergamaschi M,Razzetti R,Bongrani S,Gasco Adoi
10.1016/0014-2999(94)90077-9subject
Has Abstractpub_date
1994-04-01 00:00:00pages
17-24issue
1-3eissn
0014-2999issn
1879-0712pii
0014-2999(94)90077-9journal_volume
255pub_type
杂志文章abstract：:The contractile actions of imidazoline alpha-adrenoceptor agonists were investigated in human vas deferens longitudinal and circular muscle. The effects of phenoxybenzamine were studied in comparison to dibenamine and SZL-49 (4-amino-6,7-dimethoxy-2-quinazolinyl-4-(2-bicyclo[2,2,2]octa-2,5-dienylcarbonyl-2-piperazine)...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01346-3
更新日期：2003-02-21 00:00:00
abstract：:Inhibition by antipsychotic drugs of voltage-gated L-type Ca2+ channels was characterized in rat neuronal cell line pheochromocytoma PC12 cells. Under whole-cell voltage-clamp, haloperidol and chlorpromazine (1-100 microM) inhibited Ba2+ current permeating through Ca2+ channels. Fluspirilene and pimozide the Ba2+ curr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00500-6
更新日期：1996-10-24 00:00:00
abstract：:Phenoxybenzamine greatly attenuated phenylephrine-induced contractions of dog saphenous vein in vitro, but had less effect on contractions induced by clonidine. The phenoxybenzamine-resistant responses to clonidine were not affected by prazosin or by corynanthine but were competitively antagonized by yohimbine (pA2 8....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90219-9
更新日期：1982-12-03 00:00:00
abstract：:Ketamine, a non-selective inhibitor of NMDA (N-methyl-D-aspartate) channels is used in anesthetic or sub-anesthetic doses to induce analgesia, amnesia, to suppress fear, anxiety and depression. Although the ketamine's effect on memory acquisition is known, its effects on other aspects of memory are controversial. Morr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.12.021
更新日期：2012-02-29 00:00:00
abstract：:The alpha 2-adrenoceptor antagonist, yohimbine, has been reported to protect hypoxic myocardium. Yohimbine has several other activities, including 5-HT receptor antagonism, at the concentrations at which protection was found. Therefore we designed a study to determine if yohimbine was protecting ischemic myocardium vi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90296-8
更新日期：1994-08-11 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：: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：:Vasodilation, in vitro, evoked by atrial extracts (cardionatrin) was compared with the relaxation due to acetylcholine and papaverine in rat precontracted aortae with and without endothelium. Ventricular extracts were tested as controls. Atrial extracts and papaverine caused a similar concentration-dependent relaxatio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90040-2
更新日期：1984-05-18 00:00:00
abstract：:The inhibition by various serotonin agonists and antagonists of the binding of 3 nM 3H-d-LSD, 1.7 nM 3H-serotonin and 0.22 nM 3H-spiperone to homogenates of calf hippocampus and frontal cortex was studied. The 50% inhibitory concentration (IC50) for these drugs versus 3H-d-LSD binding had similar values to and correla...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90141-7
更新日期：1980-08-29 00:00:00
abstract：:The role of prejunctional inhibitory and facilitatory muscarinic receptors was investigated in cats with tracheal hyperresponsiveness to vagal stimulation. Intrathoracic airway caliber (total lung resistance (RL) and dynamic compliance (Cdyn] and the diameter of tracheal ring 4 were measured during vagal stimulation a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90409-w
更新日期：1992-01-21 00:00:00
abstract：:Sickness behavior is a series of behavioral and psychological changes that develop in inflammatory disease, including infections and cancers. Administration of the bacterial endotoxin lipopolysaccharide (LPS) induces sickness behavior in rodents. Genipin, an aglycon derived from an iridoid glycoside geniposide extract...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.07.038
更新日期：2014-10-15 00:00:00
abstract：:Here we provide the first pharmacological exploration of the impact of acute central nervous system exposure to three recently developed ghrelin receptor (GHS-R1A) ligands on food intake and on the electrical activity of the target cells for ghrelin in the hypothalamus. Central (i.c.v) injection of GHS-R1A antagonists...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.03.066
更新日期：2009-06-10 00:00:00
abstract：:Earlier studies demonstrated that cytokine production is under the tonic control of noradrenaline. As the level and/or the duration of noradrenaline action is regulated by the noradrenaline transporter (NET), which is also a target of antidepressant treatment, we studied its role in the regulation of the cytokine resp...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01721-7
更新日期：2003-05-23 00:00:00
abstract：:The effects of GABA and diazepam on the spontaneous and potassium-evoked release of 3H-5-HT from rat hippocampal synaptosomes, preloaded by incubation with 3H-5-HT, have been investigated. Both GABA and diazepam independently increased the spontaneous release of 5-HT whereas they blocked the calcium-dependent, potassi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90054-0
更新日期：1980-11-07 00:00:00
abstract：:The failure of alpha 1-adrenoceptor antagonists, prazosin and indoramin, to cause a reflex tachycardia was investigated in the anaesthetised cat. Recordings were made of preganglionic sympathetic nerve activity from the third or fourth white ramus communicans, femoral arterial conductance, heart rate and blood pressur...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90054-2
更新日期：1984-11-27 00:00:00
abstract：:Current clinical options for the treatment of neovascular disorders of the posterior segment of the eye have several drawbacks. Photocoagulation lasers can impair peripheral and night vision. Photodynamic therapies as well as intravitreal macromolecule injections (Macugen and Lucentis) require frequent, invasive admin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.04.044
更新日期：2007-07-30 00:00:00
abstract：:Insulin resistance is a causative factor for type 2 diabetes, whereas the development of insulin resistance is closely related to chronic inflammation induced by factors such as tumor necrosis factor-α (TNF-α). Momordica charantia, also known as bitter melon, has been used as an herbal medicine and reported to amelior...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.05.033
更新日期：2012-08-15 00:00:00
abstract：:A sensitive high pressure liquid chromatography (HPLC) method was used to measure acetylcholine release from canine bronchial tissue in response to electrical stimulation. Indomethacin enhanced the efflux of acetylcholine, an effect that was reversed by the addition of prostaglandin E2 (PGE2). Prostaglandin D2 (PGD2) ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90451-2
更新日期：1989-08-29 00:00:00
abstract：:MK-801, phenobarbital and clonazepam blocked convulsions elicited in mice by bicuculline. Treatment with Ro 15-1788 antagonized the anticonvulsant action of clonazepam, but not MK-801 or phenobarbital. The anticonflict effect in the rat of chlordiazepoxide, but not MK-801, was antagonized by Ro 15-1788. Despite having...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90167-4
更新日期：1982-10-15 00:00:00
abstract：:The intravenous infusion of catecholamines to rats induced a dose dependent increase of immunoreactive beta-endorphin (beta-Endi) in plasma. The ED50 values of 1-epinephrine and 1-isoproterenol were 110 and 100 ng/kg X min respectively. 1-Propranolol, but not d-propranolol prevented the effect of 1-epinephrine. Infusi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90303-4
更新日期：1981-06-10 00:00:00
abstract：:The effects of inhibitors of Ca(2+)-dependent endopeptidases (antipain and leupeptin) on morphine analgesia, reinforcing properties of morphine and on the development of opiate physical dependence were studied. Male Wistar rats were used. The analgesic action of morphine in the tail-immersion test was increased signif...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00092-1
更新日期：1996-05-23 00:00:00
abstract：:Little research has been conducted investigating the long-term impact of opioid exposure during adolescence. These experiments were conducted to determine the behavioral effects of morphine exposure during periadolescence (postnatal days 30-32) versus young adulthood (postnatal days 65-67) on subsequent sensitivity to...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.10.026
更新日期：2005-12-28 00:00:00
abstract：:Chemopreventive non-steroidal anti-inflammatory drugs (NSAIDs) exhibit diverse pharmacological and biological activities mainly through their inhibitory effect on cyclooxygenase (COX). However, COX-independent mechanisms involving kinase inhibition have been proposed to explain certain therapeutic effects of NSAIDs. H...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.04.012
更新日期：2010-07-25 00:00:00
abstract：:Bronchoconstrictor responses were measured in lungs isolated from spontaneously hypertensive (SHR) and normotensive rats, perfused via the airways. Lungs from SHRs were more responsive than lungs from normotensive rats to methacholine, 5-hydroxytryptamine (5-HT), arachidonic acid or prostaglandin H(2). The responses o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.02.005
更新日期：2004-03-19 00:00:00
abstract：:Direct instillation of a recombinant human form of MMP-12 (rhMMP-12) in mice airways elicited an early inflammatory response characterized by neutrophil influx, cytokine release and gelatinase activation followed by a delayed response, mainly characterized by macrophage recruitment. As this experimental model of lung ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.11.070
更新日期：2007-03-15 00:00:00
abstract：:SR 95103 has recently been described as a selective GABAA antagonist. In this study, the electroencephalographic (EEG) effects of SR 95103 were investigated as well as its central interaction with inhibitory amino acids and muscimol. Slow intravenous infusions of SR 95103 in rats induced epileptiform EEG activities wh...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90630-2
更新日期：1985-08-15 00:00:00
abstract：:Selective serotonin reuptake inhibitors (SSRIs) are known to cause sexual dysfunction, such as decreased sexual motivation, desire, arousal, and orgasm difficulties. These SSRI-induced sexual complaints have a high prevalence rate, while there is no approved pharmacological treatment for SSRI-induced sexual dysfunctio...
journal_title：European journal of pharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.ejphar.2014.10.061
更新日期：2015-04-15 00:00:00
abstract：:Therapeutic angiogenesis is a promising strategy for treating ischemia. The lysophospholipid mediator sphingosine-1-phosphate (S1P) acts on vascular endothelial cells to stimulate migration and tube formation, and plays the critical role in developmental angiogenesis. We developed poly(lactic-co-glycolic-acid) (PLGA)-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.02.038
更新日期：2010-05-25 00:00:00
abstract：:Many studies have shown that anti-inflammatory agents are effective in the treatment of endometriosis. β-Caryophyllene exerted a potent anti-inflammatory effect in vivo. However, its effect on endometriosis has not been investigated. This study aims at investigating the effect of β-caryophyllene on endometriosis and o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.01.011
更新日期：2013-02-28 00:00:00
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
