Abstract:
:Several lines of evidence suggest that acetylcholinesterase inhibitors (AChE) have their cognitive enhancing effects by stimulating cholinergic receptors within the medial septum. However, intraseptal administration of cholinergic enhancing drugs produce mixed results that appear to depend on both the integrity of the medial septum as well as task demands. Three experiments were conducted to determine the relationship between increased cholinergic activity within the medial septum and hippocampus and behavioral recovery in a model of diencephalic amnesia produced by pyrithiamine-induced thiamine deficiency (PTD). In Experiment 1, systemic tacrine (0.0, 0.75, 1.5mg/kg) was administered to PTD and pair-fed (PF) rats prior to a spontaneous alternation task. Without tacrine, PF rats alternated at a higher rate than PTD rats. Both doses of tacrine increased alternation in PTD rats to within the range of PF rats. In Experiment 2, three doses of intraseptal tacrine (2.5, 5.0, 12.5microg) were administered to PTD and PF rats and changes in hippocampal acetylcholine efflux were assessed. Both the 5.0 and 12.5microg doses significantly increased hippocampal acetylcholine levels, but the change was greater in the PTD rats. In Experiment 3, despite the fact that both intraseptal doses of tacrine (5.0, 12.5microg) increased hippocampal acetylcholine levels, only 5.0microg significantly improved alternation scores in PTD rats. Thus, when there is basal forebrain cholinergic cell loss in conjunction with diencephalic pathology, the therapeutic range of AChE-I in the medial septum and the effective doses do not directly map onto changes in acetylcholine efflux in the hippocampus.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Roland JJ,Levinson M,Vetreno RP,Savage LMdoi
10.1016/j.ejphar.2009.12.005subject
Has Abstractpub_date
2010-03-10 00:00:00pages
31-9issue
1-3eissn
0014-2999issn
1879-0712pii
S0014-2999(09)01126-1journal_volume
629pub_type
杂志文章abstract::Levonorgestrel (13beta-ethyl-17alpha-ethynyl-17beta-hydroxy-4-gonen-3-one), a potent contraceptive progestin stimulates growth and proliferation of cultured breast cancer cells through a receptor-mediated mechanism, even though levonorgestrel does not bind to the oestrogen receptor (ER). To assess whether the oestroge...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)01263-8
更新日期:2001-09-14 00:00:00
abstract::We tested if discontinuation of cocaine self-administration can lead to the development of depressive-like symptoms in the forced swim test expressed as changes in immobility, swimming and climbing behaviors in rats. A "yoked" procedure in which rats were run simultaneously in groups of three, with two rats received t...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.10.049
更新日期:2010-02-10 00:00:00
abstract::Histamine and serotonin levels in gastric secretion and the effects of pharmacological antagonists were studied in rats in which stomach ulceration was induced by electrical vagal stimulation. Electrical vagal stimulation (2 and 5 V) produced a graded increase in haemorrhagic glandular mucosal ulcers. NaHCO3 perfusion...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90213-4
更新日期:1985-04-02 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::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::The goals of the present study were: (1) to investigate the binding properties of (R)- and (S)-procyclidine and two achiral derivatives of muscarinic M1, M2 and M4 receptor subtypes and (2) to identify the interactions which allow these receptors to discriminate between the two stereoisomers. (R)-Procyclidine showed a...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(90)90017-r
更新日期:1990-09-18 00:00:00
abstract::This study was purposed to explore the mechanism of augmenting apoptosis-inducing effects of cisplatin on colorectal cancer SW480 cells by stable transfection of Programmed Cell Death 5 (PDCD5) gene, both in vitro and in vivo. The expression level of PDCD5 of SW480 cells stably transfected with PDCD5 (SW480/PDCD5) and...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.09.040
更新日期:2010-12-15 00:00:00
abstract::Methylxanthines increase central noradrenergic turnover by an unknown mechanism. Isobutyl methylxanthine (IBMX, 0.5-16 mg/kg i.v.) was found in this study to increase firing rats of noradrenergic neurons in the locus coeruleus, supporting increased impulse flow as one possible mechanism for increased noradrenergic tur...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90430-7
更新日期:1982-11-05 00:00:00
abstract::Corticotropin-releasing factor (CRF) regulates the hypothalamic-pituitary-adrenal axis, coordinates the mammalian stress response, and acting primarily via the CRF(1) receptor, has been strongly implicated in the pathophysiology of depression and anxiety. Furthermore, the behavioral and autonomic activation that occur...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.05.041
更新日期:2007-09-24 00:00:00
abstract::The overactivation of glutamate receptors is a major cause of Ca(2+) overload in cells, potentially leading to cell damage and death. There is an abundance of agents and mechanisms by which glutamate receptor activation can be prevented or modulated in order to control these effects. They include the well-established,...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/s0014-2999(02)01851-4
更新日期:2002-07-05 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::Beta2-adrenoceptor agonists are the first-line treatment of asthma and chronic obstructive pulmonary disease (COPD), in which a short-acting beta2-adrenoceptor agonist is used as required for relief of bronchoconstriction. A long-acting beta2-adrenoceptor agonist may be added to an inhaled corticosteroid as step 3 in ...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2005.12.060
更新日期:2006-03-08 00:00:00
abstract::In the present study, the mechanism of relaxant response of nitric oxide precursor, L-arginine, was investigated in goat isolated coronary artery. L-arginine (1 mM) reversed the U-46619 (1 microM)-induced contraction both in endothelium-intact and endothelium-denuded arterial ring preparations. L-arginine analogues, L...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.03.031
更新日期:2009-05-01 00:00:00
abstract::Continuous monitoring of the foetal electrocorticogram, eye movements and heart rate in ewes during the last month of gestation showed rapid placental transfer from the mother to the foetus of phenothiazine derivatives (acepromazine maleate), short-acting barbiturates (thiopental sodium) and narcotic analgesics (meper...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(76)90022-4
更新日期:1976-05-01 00:00:00
abstract::The novel substituted benzamide eticlopride, (S)-(-)-5-chloro-3-ethyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxy salicylamide hydrochloride (A38503; FLB 131), was radiolabelled to high specific activity and used for in vivo receptor binding studies in the rat brain. Intravenous injections of [3H]eticlopride resulted...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90543-1
更新日期:1986-01-21 00:00:00
abstract::The present study was conducted to evaluate the effect of L-3, 4-dihydroxyphenylalanine (L-DOPA) on the daily rhythms of temperature, heart rate and locomotor activity in rats that received a 7-day continuous infusion. Our results indicate that L-DOPA does not induce a loss of the daily rhythmicity of temperature, hea...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00422-2
更新日期:2000-07-28 00:00:00
abstract::Astragaloside IV (AS-IV) is one of the main active ingredients of Astragalus membranaceus. This study is aimed to investigate AS-IV׳s effects on Ca(2+) channel activity of single cardiomyocytes and single Ca(2+) channels. Whole-cell Ca(2+) currents in freshly dissociated cardiomyocytes were measured using the whole-ce...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2015.03.082
更新日期:2015-08-05 00:00:00
abstract::Disturbances in oxidative metabolism are involved in many acute and chronic diseases, as well as in several other conditions. The objective of the present study was to examine the relationship between the level of intracellular reactive oxygen species in the peripheral blood granulocytes of mice, as evaluated by 2',7'...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.11.001
更新日期:2010-02-10 00:00:00
abstract::Angiotensin AT1 receptor antagonists are divided into two types, surmountable and insurmountable, based on the way they inhibit angiotensin II-induced vasoconstriction. To elucidate what causes the difference, we studied how antagonists associate with and dissociate from AT1 receptor sites in rat liver membranes. Thre...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(95)90103-5
更新日期:1995-04-28 00:00:00
abstract::The analgesic effect of cyclazocine microinjected into the diencephalon of rats was studied by using the bradykinin-induced flexor reflex test. The dorsal portion of the medial hypothalamic area was sensitive to cyclazocine with respect to the production of analgesia (ED50 2.6 micrograms/rat). Microinjections of morph...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90119-0
更新日期:1985-04-23 00:00:00
abstract::Experiments were performed to provide a quantitative description of the barbiturate withdrawal syndrome. Physical dependence was produced in 63 cats by 'maximally tolerable' dosing with sodium pentobarbital. After 5 weeks of chronic treatment each animal was placed in an activity monitoring cage and observed closely f...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(76)90360-5
更新日期:1976-11-01 00:00:00
abstract::Electrical stimulation (ES) contracted superfused mouse bladder, and 10(-7) M tetrodotoxin (TTX) abolished the twitches without impairing responses to acetylcholine (ACh) or beta,gamma-methylene ATP. ES acted largely through nerves which were not cholinergic, adrenergic or histaminergic. They may be purinergic because...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90190-6
更新日期:1985-10-08 00:00:00
abstract::This study compared the peripheral analgesic effects of a novel opioid agonist 14-O-methylmorphine-6-O-sulfate (14-O-MeM6SU), to that of non-peptide (morphine, fentanyl) and peptide opioid agonists (Met-enkephalin; met-ENK and β-endorphin; β-END) in a model of localized inflammatory pain evoked by intraplantar (i.pl.)...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.04.043
更新日期:2013-08-05 00:00:00
abstract::Endogenous polyamines mediate acute metabolic effects and cardiac hypertrophy associated to beta-adrenoceptor stimulation. The aim of this study is to characterize the role of polyamines on beta-adrenoceptor system mediated responses. To this end, the functional interaction of polyamine modifying drugs on isoprotereno...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.07.069
更新日期:2008-11-19 00:00:00
abstract::The occurrence and characteristics of binding sites specific for gamma-aminobutyric acid (GABA) and muscimol in the rat stomach were examined by biochemical and autoradiographic techniques, and the effects of GABAergic model compounds on gastric ulceration induced by chemical irritation was studied in intact and unila...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90772-3
更新日期:1989-06-08 00:00:00
abstract::The present study addresses the causal relationship between induction of endo/sarcoplasmic reticulum stress and dysregulation of calcium transport, while examining whether the most widely-used experimental endo/sarcoplasmic reticulum stressors can be considered appropriate for elucidating underlying cellular mechanism...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2015.07.026
更新日期:2015-10-05 00:00:00
abstract::We have eliminated putative palmitoylation sites in the carboxyl tail of the human dopamine D1 receptor by replacing the two cysteine residues with alanines either separately or together. The wild type and the three mutated dopamine D1 receptors were stably expressed in baby hamster kidney cells and characterized to d...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)00059-9
更新日期:1997-04-11 00:00:00
abstract::In this study, the anti-inflammatory effects of flavonoids isolated from the roots of Glycyrrhiza uralensis (Leguminosae), namely, isoliquiritin (the glycoside of isoliquirigenin) and isoliquiritigenin (the aglycone of isoliquiritin) were evaluated on lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. Isoliquirit...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.01.032
更新日期:2008-04-14 00:00:00
abstract::The pharmacological profile of DSP-6952, a novel 5-HT4 receptor partial agonist, was investigated to evaluate the potential use for GI disorders, and to compare its effects in some GI dysfunction models with those of clinically efficacious prokinetic agents. DSP-6952 enhanced gastric motility and caused colonic giant ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2018.02.005
更新日期:2018-05-05 00:00:00
abstract::Ca2+-handling disturbances play an important role in the genesis of myocardial ischemia/reperfusion (I/R) injury. Ischemic preconditioning (IPC) is a powerful strategy to induce tolerance against subsequent ischemic episodes. IPC signaling pathways may be triggered by Ca2+ ion. Since Na+/Ca2+ exchanger 1 (NCX1) partic...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2016.11.045
更新日期:2017-01-05 00:00:00