Abstract：
:Tracazolate (ICI 136,753) 4-butylamine-1-ethyl-6-methyl-1H-pyrazolo[3,4]pyridine-5-carboxylic acid ethyl ester is a non-benzodiazepine with anxiolytic-like activity in animal models. In contrast to the benzodiazepines, it enhances [3H]flunitrazepam binding in rat synaptic membrane fragments. The enhancement is potential by chloride ion and is due to an increase in affinity of the receptor. The enhancement of benzodiazepine binding by gamma-aminobutyric acid (GABA) is additive with that of tracazolate; however, the GABA antagonist bicuculline blocks the enhancement by both compounds. Tracazolate enhances [3H]GABA binding to frozen and thawed Triton X-100-treated membrane fragments. The enhancement is due to an increase in the number of sites and potentiated by chloride. Benzodiazepines also enhanced GABA binding but the effect was due to an apparent change in affinity and not potentiated by chloride. The rank order to chlorodiazepoxide, diazepam and flunitrazepam for enhancement of GABA binding and displacement of [3H]flunitrazepam binding were the same. The enhancement of [3H]GABA binding by flunitrazepam and tracazolate were additive. Possible interactions between these various receptors are discussed.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Meiners BA,Salama AIdoi
10.1016/0014-2999(82)90033-4subject
Has Abstractpub_date
1982-03-12 00:00:00pages
315-22issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(82)90033-4journal_volume
78pub_type
杂志文章abstract：:Recent successes as a pharmacological adjunct to exposure therapy has focused attention on the therapeutic potential of the glycine(B) receptor partial agonist, D-cycloserine (DCS), in certain clinical anxiety disorders. Although widely believed to reflect a facilitation of extinction learning, previous research with ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.08.005
更新日期：2010-11-10 00:00:00
abstract：:Pregnant rats were infused with phentermine plus dexfenfluramine from days 3 through 17 of gestation. Control rats were either pair-fed or were fed ad libitum. There were no effects of prenatal drug treatment on number of offspring, their birth weights, or on their motor coordination assessed at 11 days of age. Mother...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00100-4
更新日期：1999-03-26 00:00:00
abstract：:Single myelinated nerve fibres of Rana esculenta were investigated under current and potential clamp conditions at 20 degrees C. Under 2.5 mM phenobarbital, the amplitude of the action potential was reversibly reduced to 85.5 +/- 5% (n = 6), and the threshold potential was raised by 32% of the control in Ringer soluti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90432-1
更新日期：1979-06-01 00:00:00
abstract：:The present study was to investigate the neuroprotective efficacy and mechanism of Forsythoside B. Male Sprague-Dawley rats were subjected to middle cerebral artery occlusion for 1 h followed by reperfusion for 23 h. Rats received an intravenous bolus injection of Forsythoside B at 15 min after reperfusion. The result...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.04.055
更新日期：2010-08-25 00:00:00
abstract：:Soluble amyloid β-protein (Aβ) oligomers are primary mediators of synaptic dysfunction associated with the progression of Alzheimer's disease. Such Aβ oligomers exist dependent on their rates of aggregation and metabolism. Use of selective somatostatin receptor-subtype agonists have been identified as a potential mean...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.03.020
更新日期：2012-05-15 00:00:00
abstract：:Exploring the importance of nanofibrous scaffold with traditionally important medicine as a wound dressing material prevents infection and aids in faster healing of wounds. In the present study, the Collagen (COL) from the marine fish skin was extracted and employed for coating the Poly(3-hydroxybutyric acid) (P)-Gela...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.08.003
更新日期：2017-11-05 00:00:00
abstract：:We have demonstrated that the antagonism of 5-HT2 receptors produces an enhancement of serotonergic sympathoinhibitory effect by 5-HT1D and 5-HT7 activation. The aim of this work was to determine mechanisms involved in the 5-hydroxytriptaminergic inhibitory action on the pressor responses elicited by sympathostimulati...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.02.043
更新日期：2014-05-15 00:00:00
abstract：:Hyperphosphatemia is a mineral bone-disease that increases cardiovascular complications and all-cause mortality in chronic kidney disease (CKD) patients. Oral phosphate binders absorb the dietary phosphate to prevent its high plasma levels. Moreover, they can adsorb some uremic toxins and decrease inflammation. A few ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2019.172892
更新日期：2020-02-05 00:00:00
abstract：:Farrerol, a typical natural flavanone, is the major active component of Rhododendron dauricum L. The objective of this study was to evaluate the attenuation effect of farrerol against the aortic lesions in spontaneously hypertensive rats (SHR) for the first time. Twelve-week-old male SHR were orally administered with ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.11.020
更新日期：2015-12-15 00:00:00
abstract：:The quantitative [14C]2-deoxyglucose autoradiographic technique was applied to the measurement of the cerebral metabolic effects of adenosine A1 and A2 receptor agonists and antagonists in adult rats. The adenosine A1 receptor agonist and antagonist, 2-chloro-N6-cyclopentyladenosine (CCPA) and 8-cyclopentyl-1,3-diprop...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90057-4
更新日期：1994-06-02 00:00:00
abstract：:The characteristics of the prefrontal cortex regulation of dopamine release in the rat dorsolateral striatum were investigated in focusing on the corticostriatal pathway, using dual-probe microdialysis in combination with simple behavioral procedures. Intracortical perfusion of the GABA(A) receptor antagonist bicucull...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.10.003
更新日期：2003-12-15 00:00:00
abstract：:Various in vitro models have been developed to study ischemia and/or hypoxia. In the present experiment, we examined whether hypoxia/hypoglycemia (ischemia) in rat hippocampal slices reduced the 2-deoxyglucose (2-DG) uptake and CA1 field potentials evoked by stimulation of Schaffer collaterals. Autoradiograms revealed...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90281-8
更新日期：1992-12-08 00:00:00
abstract：:Lipoprotein lipase (LPL) is the rate-controlling enzyme for the accumulation of triacylglycerol into adipocytes, which acts by digesting it into glycerol and fatty acids. In this study, we found that treatment with (+)-JQ1, an inhibitor of the bromodomain and extra-terminal (BET) family proteins, for 4 days from the e...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172492
更新日期：2019-09-05 00:00:00
abstract：:beta-Carbolines (including harmane and pinoline) stimulate insulin secretion by a mechanism that may involve interaction with imidazoline I(3)-receptors but which also appears to be mediated by actions that are additional to imidazoline receptor agonism. Using the MIN6 beta-cell line, we now show that both the imidazo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.08.018
更新日期：2004-10-06 00:00:00
abstract：:The present in vivo microdialysis study examined the role of vesicular- and carrier-mediated mechanisms underlying dopamine (DA) release, uptake and metabolism in halothane-anaesthetized rats. Omission of calcium (Ca2+) from the dialysis perfusing medium, thereby reducing the concentration of Ca2+ in the striatal micr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90067-8
更新日期：1989-07-18 00:00:00
abstract：:We examined the feasibility of coupling the 5-HT(6) receptor to a Ca(2+) signaling read-out using a chimeric G-protein, comprising of G(alphaq) with the C-terminal five amino acids from G(alphas), to facilitate assays on the fluorometric imaging plate reader (FLIPR). Using a transient transfection assay in human embry...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01855-7
更新日期：2003-07-04 00:00:00
abstract：:The anticancer drugs camptothecin (CPT) and topotecan (TPT) are known DNA topoisomerase I inhibitors which cause DNA damage and lead to cell death. In this study we provide evidence that CPT and TPT also interfere with the elements of cytoskeleton - microtubules and actin filaments which could be partly responsible fo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.07.044
更新日期：2016-10-15 00:00:00
abstract：:Acute lung injury (ALI) is a common severe clinical syndrome in intensive care unit. Inflammation has been reported to play a critical role in the development of ALI. Cordycepin, an active component isolated from Cordyceps militaris, has been reported to have anti-inflammatory effects. However, the anti-inflammatory e...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.10.029
更新日期：2018-01-05 00:00:00
abstract：:Thaliporphine (0.1-100 microM) produced sustained, concentration-dependent contraction in isolated rings of rat aorta. Thaliporphine (ED50 = 1.5 +/- 0.5 microM) was less potent than endothelin (ED50 = 3.9 +/- 0.4 nM), but was more potent than Bay K 8644 (ED50 = 5.5 +/- 0.6 microM). Thaliporphine also contracted guinea...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90342-f
更新日期：1993-03-16 00:00:00
abstract：:Immunohistofluorescent neurotensin (NT) is found in the ventral tegmental area (VTA), and bilateral injection of NT into the VTA produces an increase in exploratory behaviors. The VTA also contains dopaminergic cell bodies with axonal projections to the nucleus accumbens. In this study it was shown that bilateral micr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90491-5
更新日期：1982-03-26 00:00:00
abstract：:We have investigated the effects of four fluoroquinolones on the human ether-à-go-go-related gene (HERG) mediated K(+) currents to evaluate their potential to induce QT-prolongation. HERG currents were measured from stably transfected Chinese hamster ovary (CHO) cells by means of the patch-clamp technique. Bath applic...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00693-2
更新日期：2000-10-20 00:00:00
abstract：:Carbocyclic thromboxane A2 (CTA2) constricted rabbit basilar and saphenous arteries. The contractions of the basilar artery, but not those of the saphenous artery, were potently inhibited by the calcium antagonist nimodipine. Selective inhibition of thromboxane-induced vasoconstriction of cerebral vessels may contribu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90417-9
更新日期：1981-01-16 00:00:00
abstract：:β-Methoxyacrylate antibiotics are well known to inhibit the fungal and yeast mitochondrial respiratory chain. In addition, β-methoxyacrylates are reported to suppress the proliferation of mammalian cancer cells. Differentiation and cell-cycle arrest are closely related. The cell cycle of proliferating cells is suppres...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.08.018
更新日期：2012-11-05 00:00:00
abstract：:Intracerebroventricular (i.c.v.) or intravenous (i.v.) administration of morphine (10 micrograms or 25 mg/kg, respectively) increased the mortality rate in experimental anaphylaxis in mice. This effect was blocked by the opiate antagonist naltrexone administered systemically (5 mg/kg) or i.c.v. (10 micrograms). Moreov...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90274-1
更新日期：1983-11-11 00:00:00
abstract：:Trans-dehydrocrotonin has antiulcerogenic and antitumor activities. A complex of beta-cyclodextrin with dehydrocrotonin was developed to improve the delivery of dehydrocrotonin. Complex in solid state was evaluated using X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermal gravimetric analysis (TG...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.01.016
更新日期：2005-03-07 00:00:00
abstract：:The effects of lorcainide and its metabolite norlorcainide on the maximal rate of depolarization (Vmax) were compared at different rates of stimulation and at various membrane potentials in ventricular muscle preparations of guinea-pig heart. A standard microelectrode technique was used. The results show that lorcaini...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90202-0
更新日期：1987-01-06 00:00:00
abstract：:Non-peptide antagonists of the NK1 and NK2 receptors were tested as inhibitors of the reaction time in the rat tail-flick and on the decrease of reaction time induced by the intrathecal injection of the NK1 receptor selective agonist [Sar9,Met(O2)11]SP or of the NK2 selective agonist NKA-(4-10). The decrease in reacti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90782-d
更新日期：1993-03-02 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：:The effects of acute treatment with (S)-2-[[(7-fluoroindan-4-yl)oxy]methyl]morpholine monohydrochloride (YM992), venlafaxine, fluoxetine and citalopram on extracellular norepinephrine levels were examined in the rat frontal cortex by in vivo microdialysis. YM992 (3, 10, 30 mg/kg, i.p.) dose-dependently increased extra...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00173-4
更新日期：2000-04-21 00:00:00
abstract：:We assessed the effects of active site-directed, fibrinogen recognition exosite (FRE)-directed and bifunctional thrombin inhibitors, on shear-induced platelet reactivity (adhesion/aggregation) and dynamic coagulation (coagulation of flowing blood). An in vitro test for shear-induced haemostatic plug formation and dyna...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00655-5
更新日期：2000-10-13 00:00:00
