Abstract：
:The rat vas deferens has been considered to be the tissue of choice to study alpha-adrenergic drugs. However, some of these agonists have elicited complex responses in this organ. Therefore, detailed characterization of alpha-adrenoceptor-mediated responses of the rat vas deferens was the aim of this work. Experiments were designed to study the contractile response of this tissue to phenylethanolamine (noradrenaline) and to two imidazolines (oxymetazoline and naphazoline). These responses were related to receptor occupancy and to other parameters of drug action, i.e. dissociation constants, relative efficacies, ED50 and maximal responses. A theoretical model was used to check the experimental data. There was a non-linear relationship between response and receptor occupancy with all three agonists. The dissociation constants for noradrenaline, oxymetazoline and naphazoline were 11.06, 0.15 and 0.10 microM, respectively. The rat vas deferens had 75-80% spare receptors for noradrenaline. Oxymetazoline and naphazoline were shown to be partial agonists with low relative efficacies as compared to noradrenaline (0.0063 and 0.0056 respectively). The dose-response curves generated by the model for partial agonists were similar to the curves obtained experimentally in vitro.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Díaz-Toledo A,Martí MCdoi
10.1016/0014-2999(88)90276-2subject
Has Abstractpub_date
1988-11-08 00:00:00pages
315-24issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(88)90276-2journal_volume
156pub_type
杂志文章abstract：:BAY 38-7271 [(-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate] is a novel, highly potent and selective cannabinoid CB(1)/CB(2) receptor agonist with neuroprotective properties. It was the aim of the present study to further confirm its cannabinoid CB(1) receptor agonist properties in a highly...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02697-3
更新日期：2002-12-20 00:00:00
abstract：:Prolactin blood level and apomorphine-induced yawning were studied in rats treated with the substituted benzamide amisulpride in association with bromocriptine or carmoxirole; two dopamine D(2) receptor agonists with high or low propensity to cross the brain-blood barrier, respectively. Administration of amisulpride p...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01896-4
更新日期：2002-06-28 00:00:00
abstract：:This study was designed to investigate the effect and mechanism of allicin on hyperhomocysteinemia-induced experimental vascular endothelial dysfunction in rats. Fifty male Wistar rats were randomly divided into five groups: the normal control rats (NC), the high-methionine-diet rats (Met), the high-methionine-diet ra...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.05.038
更新日期：2013-08-15 00:00:00
abstract：:Activated factor X (FXa) is an important player in the coagulation cascade responsible for thrombin generation, which is activated during atrial fibrillation. Increasing evidence suggests that FXa influences cell signalling in various cell types by activating protease-activated receptors (PARs). It is so far not known...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.09.006
更新日期：2013-10-15 00:00:00
abstract：:Since the discovery of first antidepressants in mid-1950's, the field has been intensively studied. Several new classes of compounds emerged and several hypotheses on the mechanism of their action were proposed. The novel antidepressants are either selective and reversible monoamine oxidase inhibitors, (e.g., moclobem...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(00)00565-3
更新日期：2000-09-29 00:00:00
abstract：:The cGMP response and the accumulation of inositol monophosphate (IP) induced by carbachol were compared in slices of different rat brain structures. Basal cGMP and the responses of cGMP to carbachol appeared dependent on the concentration of added Ca2+, suggesting that distinct Ca(2+)-mediated and Ca(2+)-sensitive mu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90029-h
更新日期：1991-07-12 00:00:00
abstract：:The amyloid precursor protein (APP) has been mainly studied in its role in the production of amyloid β peptides (Aβ), because Aβ deposition is a hallmark of Alzheimer's disease. Although several studies suggest APP has physiological functions, it is still controversial. We previously reported that APP increased glial ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.09.015
更新日期：2011-01-10 00:00:00
abstract：:Heme oxygenase is the rate-limiting enzyme in the catabolism of heme to carbon monoxide, bilirubin and free iron. Many cell types express heme oxygenase-2 constitutively while heme oxygenase-1 is induced at sites of inflammation and oxidative stress. In systemic blood vessels, carbon monoxide may have an important hom...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)02001-6
更新日期：2003-07-25 00:00:00
abstract：:A series of oximes and related compounds were assessed for their ability to restore soman-induced neuromuscular block in the isolated diaphragm preparation of the rat, guinea-pig and marmoset. In the rat the bispyridinium oximes HS6, HI6 and HS14 were superior to P2S and all other compounds tested. Conversely, in the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90164-4
更新日期：1983-08-05 00:00:00
abstract：:In male Swiss mice, muscimol produced myoclonic jerks. A 3 mg/kg (i.p.) dose induced this response in all of the mice tested and the peak response of 73 jerks per min was observed between 27 and 45 min. Increasing the brain serotonin levels by the administration of 5-hydroxytryptophan (80-160 mg/kg) in combination wit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90087-x
更新日期：1981-07-17 00:00:00
abstract：:Lemnalol (8-isopropyl-5-methyl-4-methylene-decahydro-1,5-cyclo-naphthalen-3-ol) is a natural compound isolated from the marine soft coral Lemnalia cervicorni. In the present study, the anti-inflammatory and anti-nociceptive properties of lemnalol were investigated in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.08.048
更新日期：2008-01-14 00:00:00
abstract：:The novel antiepileptic and neuroprotective drug felbamate (1 mM) caused a marked inhibition of voltage-dependent Na+ currents expressed in Xenopus oocytes upon injection of the cRNA encoding alpha-subunits from rat and human brain. This inhibition was present only if felbamate was perfused on the intracellular side o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00802-3
更新日期：1996-12-05 00:00:00
abstract：:Apomorphine (50 micrograms/kg) induced repeated episodes of yawning, penile erection and genital grooming in rats. A dose of cycloheximide, which inhibited brain protein synthesis by 50% totally prevented apomorphine-induced yawning and reduced by approximately 50% the occurrence of episodes of penile erection and gen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90327-2
更新日期：1982-12-24 00:00:00
abstract：:SQ 20009 and SQ 65396, two new pyrazolopyridines with anxiolytic properties in animals, reversibly increased Na+-independent 3H-GABA binding to rat cerabral cortex membranes in vitro. This modulation was partially chloride dependent and sensitive to Triton-X 100. Kinetic analysis of 3H-muscimol binding revealed an inc...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90281-2
更新日期：1980-03-21 00:00:00
abstract：:Cerebral ischemia/reperfusion (I/R) is a lethal and disabling disease. Studies have suggested that hyperglycemia is a risk factor for cerebral I/R. Baicalin is a natural bioactive flavonoid extracted from Scutellaria baicalensis Georgi with neuroprotective activity. In the present study, we investigated the effects of...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.07.041
更新日期：2017-11-15 00:00:00
abstract：:Although accumulated data suggest that calcitonin gene-related peptide (CGRP) produces anabolic effects in skeletal tissue by directly acting on osteogenic cells, neither the distribution of CGRP receptor subtypes nor the associated cellular signaling pathways are well understood. In this study, we have pharmacologica...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01763-1
更新日期：2003-06-06 00:00:00
abstract：:A series of neurochemical studies evaluated the selectivity of the depletions of norepinephrine produced by intraventricular injections of xylamine. Brain monoamines were assayed by liquid chromatography with electrochemical detection. With ether anesthesia, bilateral injections of 50 or 100 micrograms xylamine reduce...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90228-0
更新日期：1984-04-20 00:00:00
abstract：:Agomelatine is an antidepressant with a novel mechanism of action. It is a melatonergic agonist for MT1 and MT2 receptors and a serotonin (5-HT2C) receptor antagonist. Agomelatine has been suggested not to have adverse effects on sexual functions. However, the effects of chronic agomelatine administration on reproduct...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.11.054
更新日期：2016-01-05 00:00:00
abstract：:The effects of Bay K 8644 [methyl-1,4-dihydro-2,6-dimethyl-3-nitro-4-(2-trifluoromethylphenyl) -pyridine-5-carboxylate], a calcium channel agonist, on renin release in rat kidney cortical slices were examined. Bay K 8644 produced a dose-related inhibition of renin release in the presence of 15 mM potassium. The inhibi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90011-1
更新日期：1985-11-19 00:00:00
abstract：:Little information is available on the influence of sex in combination with smoking habits and combined oral contraceptives (COC) use on cellular inflammatory indexes such as neutrophil/lymphocyte ratio (NLR), derived NRL (dNLR), platelet/lymphocyte ratio (PLR), monocyte/lymphocyte ratio (MLR), mean platelet volume/pl...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173762
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abstract：:In superfusion experiments with a crude synaptosomal fraction from the nucleus accumbens of rats, lysergic acid diethylamide, mescaline and N,N-dimethyltryptamine (representing different chemical classes of psychotomimetics) produced a concentration-related inhibition of K+-evoked [3H]dopamine release whereas spontane...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90140-1
更新日期：1983-09-30 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：:We previously reported the synthesis of three new opioid agonists as well as their in vitro and in vivo activity [Girón, R., Abalo, R., Goicoechea, C., Martín, M.I., Callado, L.F., Cano, C., Goya, P., Jagerovic, N. 2002. Synthesis and opioid activity of new fentanyl analogs. Life Sci. 71, 1023-1034]. One of them, N-[1...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.07.052
更新日期：2008-10-24 00:00:00
abstract：:3H-Mepyramine (3H-MEP) binds to slide-mounted tissue sections with characteristics indicating the labelling of a H1-histamine receptor. It is saturable (Bmax 12 pg/g tissue), of a high affinity (KD 0.5 mM) and possesses a drug specificity similar to that observed for H1 receptors in a variety of systems. In agreement ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90478-3
更新日期：1979-10-01 00:00:00
abstract：:The effects of rat calcitonin gene-related peptide (CGRP) on superfused rat aortic smooth muscle cells in cell culture were investigated. Exposure of the cells for 10 min to CGRP (10(-7) M), with or without pretreatment with pertussis toxin, stimulated the release of cyclic AMP but not of prostacyclin, as judged by ra...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90062-9
更新日期：1989-07-18 00:00:00
abstract：:Impairment of nitric oxide (NO) - cyclic GMP signaling pathway is likely to contribute to human begnin prostate hyperplasia (BPH). In the present study we have used a model of chronic NO synthesis inhibition to evaluate the functional alterations of prostate smooth muscle (PSM) machinery, and involvement of Rho-kinase...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.03.057
更新日期：2015-07-05 00:00:00
abstract：:Multiple myeloma cells can be characterized immunophenotypically as the expression levels of several membrane antigens differ from those of normal plasma cells. These antigens are important for making a diagnostic of multiple myeloma; they have a significant role in survival and proliferation of multiple myeloma cells...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.02.002
更新日期：2013-04-15 00:00:00
abstract：:Adult rats submitted to perinatal protein deprivation (from day 14 of fetal life till 50 days of age) followed by a longer phase of nutritional recovery on balanced laboratory chow, showed a significant decrease of the pressor response elicited by noradrenaline and adrenaline, an effect that persisted after ganglionic...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90055-9
更新日期：1983-01-28 00:00:00
abstract：:The influence of ethanol (0.5, 1.0 and 2.0 g/kg i.p.) on the Bezold-Jarisch reflex in urethane-anaesthetized rats was studied. 5-Hydroxytryptamine (serotonin; 5-HT; 1, 3, 10 and 30 micrograms/kg i.v.) and capsaicin (1, 3 and 10 micrograms/kg i.v.) reflexly decreased heart rate in a dose-dependent manner. The 5-HT3 rec...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(95)90020-9
更新日期：1995-05-26 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
