Abstract：
:The effects of RX 781094, a new and potent alpha 2-adrenoceptor antagonist, on locus coeruleus (LC) unit activity were examined. Low doses of RX 781094 produced suppression of spontaneous LC unit activity which could be reversed with yohimbine. The increase in LC firing produced by WB 4101 could also be reversed with a low dose of RX 781094. Thus, at low doses, RX 781094 has clonidine-like alpha 2-agonist activity. At higher doses, RX 781094 reversed the effects of clonidine and markedly shifted the dose of clonidine required to suppress LC unit activity. These data suggest that at high doses RX 781094 has alpha 2-antagonist properties. It is concluded that RX 781094 may be a partial agonist at alpha 2-adrenoceptors in the CNS.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Goldstein JM,Knobloch LC,Malick JBdoi
10.1016/0014-2999(83)90368-0subject
Has Abstractpub_date
1983-07-15 00:00:00pages
101-5issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(83)90368-0journal_volume
91pub_type
杂志文章abstract：:Our data indicate that estrogens and progesterone can regulate the number of GABA receptors (as detected by [3H]muscimol binding assay) in rat brain. Both hormones act in selected areas. The extent of the effect (up to 160% increase) and the number of areas responsive suggest that sex hormones may play a very importan...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90205-x
更新日期：1984-08-03 00:00:00
abstract：:Previous studies have shown that repeated injections of acidic saline, given into the lateral gastrocnemius muscle of rats, results in a bilateral reduction in withdrawal threshold to tactile stimulation of the hindpaws. We have now characterised this model of muscoskeletal pain pharmacologically, by evaluating the an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.01.017
更新日期：2004-03-08 00:00:00
abstract：:Severe depletion of 5-hydroxytryptamine (5-HT) by para-chlorophenylalanine (pCPA, 150 mg/kg per day x3) did not alter the hypophagic effect of d-fenfluramine (1-3 mg/kg i.p.) 1 h after food presentation in 24-h food-deprived rats, and moderately and comparably increased the hypophagic effects of its metabolite, d-norf...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90013-8
更新日期：1993-09-21 00:00:00
abstract：:Pharmacological experiments have implicated a role for serotonin (5-HT)(1A) receptors in the modulation of anxiety. More recent is the interest in corticotropin-releasing hormone (CRH) system as a potential target for the treatment of anxiety disorders. However, selective pharmacological tools for the CRH system are l...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(03)01281-0
更新日期：2003-02-28 00:00:00
abstract：:Uptake blockers and substrates are likely to recognise a common binding domain on the dopamine neuronal transporter (DAT). Among cations that form ionic gradients at the level of the cellular plasma membrane, Na+ is the only one that can stimulate their binding. The binding stimulation appears over Na+ concentrations ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2003.08.069
更新日期：2003-10-31 00:00:00
abstract：:Intracellular accumulation of calcium is thought to play an integral role in the progression of ischemic injury and cell death. We infused the calcium entry blocker, nitrendipine (1.5 micrograms/kg per min), into cats in order to investigate the importance of extracellular Ca2+ influx during hemorrhagic shock. Nitrend...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90510-7
更新日期：1984-01-13 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：:Cell-cell interaction through binding of intercellular adhesion molecule (ICAM), B7.1, B7.2 and CD40 on monocytes to their ligands on T-cells plays a number of roles in cytokine . High mobility group box 1 (HMGB1), an abundant and conserved nuclproduction and lymphocyte proliferationear protein, acts in the extracellu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.11.058
更新日期：2013-02-15 00:00:00
abstract：:Cholera toxin, stereotaxically injected into the medial septal nucleus of the rat, leads within 24 h to a dramatic decrease in body weight and an increase in septal adenylate cyclase activity. Toxin-treated rats drink one-third the water of vehicle-treated animals while excreting two-and-one half times the urine. Food...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90338-2
更新日期：1978-09-15 00:00:00
abstract：:Sibutramine is a serotonin-norepinephrine reuptake inhibitor indicated for the management of obesity in conjunction with a reduced calorie diet. Though sibutramine was originally evaluated for possible use as an antidepressant, its research development was eventually redirected to evaluate it as an anorexiant. The pha...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(02)01423-1
更新日期：2002-04-12 00:00:00
abstract：:The effects of gentamicin, an aminoglycoside antibiotic, on changes in the catecholamine levels in the rat striatum, hypothalamus, adrenal medulla and vas deferens were studied. When rats were i.v. injected with gentamicin (1.0 mg/kg), the catecholamine content of all tissues increased 2-4 h after injection. The incre...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90656-o
更新日期：1992-01-07 00:00:00
abstract：:Inhibition of the p38 mitogen-activated protein kinase (MAP Kinase) pathway reduces acute ischemic injury in vivo, suggesting a direct role for this signaling pathway in a number of neurodegenerative processes. The present study was designed to evaluate further the role of p38 MAP Kinase in acute excitotoxic neuronal ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01890-3
更新日期：2002-06-28 00:00:00
abstract：:We have recently demonstrated that hyperthermia induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and m-chlorophenylpiperazine (m-CPP) are separately mediated by selective stimulation of 5-HT2A and 5-HT2C receptors, respectively in Wistar rats. Furthermore, hyperthermia induced by either DOI or m-CPP was ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00279-t
更新日期：1995-08-25 00:00:00
abstract：:Galectins are carbohydrate-binding proteins and these have very high affinity for β-galactoside containing glycoproteins and glycolipids. Amongst sixteen types of galectin, the role of galectin 1, 3, 9 and 12 is defined in the development and progression of different types of leukemia including acute myeloid leukemia,...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2018.11.019
更新日期：2019-02-05 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 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：:In isolated rabbit aortae, imidazole (10(-4)M) caused a unique nonspecific potentiation of the contractile responses to prostaglandins, norepinephrine, 5-hydroxytryptamine, histamine and potassium only at low concentrations. Imidazole had no effect on the dose-response relationship for Ca2+ in the presence of potassiu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90255-2
更新日期：1982-09-24 00:00:00
abstract：:The production of reactive oxygen species plays roles during the development of endothelial dysfunction and it represents a significant prognostic factor for evaluating the risk of cardiovascular disease. Although statins target cholesterol biosynthesis, the beneficial effects on cardiovascular disease remain to be fu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.12.037
更新日期：2010-03-25 00:00:00
abstract：:The effects of selective phosphodiesterase inhibitors, cyclic AMP (cAMP) elevating agents and stable analogues of cyclic nucleotides, on the release of arachidonate induced by N-formyl-Met-Leu-Phe (fMLP) were investigated on human peripheral blood mononuclear cells. The selective phosphodiesterase IV inhibitors, rolip...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(95)90129-9
更新日期：1995-10-15 00:00:00
abstract：:The aim of the present study was to investigate the effects of chronic administration of morphine on the expression of an endogenous opioid peptide in the spinal dorsal horn. Bovine adrenal medulla 22-like immunoreactivity (BAM22-IR) was found in the superficial layers of the spinal cord. Intrathecal (i.t.) administra...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.06.023
更新日期：2008-07-28 00:00:00
abstract：:Incubated tissue slices from different regions of the rat brain contained cyclic guanosine 3',5'-monophosphate (cyclic GMP) in the following descending order of content: cerebellum greater than hypothalamus greater than striatum greater than thalamusmidbrain greater than brain stem greater that hippocampus greater tha...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90308-8
更新日期：1975-06-01 00:00:00
abstract：:Clomipramine is a tricyclic antidepressant for psychiatric disorders that can induce QT prolongation, which may lead to torsades de pointes. Since blockade of cardiac human ether-a-go-go-related gene (hERG) channels is an important cause of acquired long QT syndrome, we investigated the acute effects of clomipramine o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.06.094
更新日期：2008-09-11 00:00:00
abstract：:Increased O-Linked β-N-acetylglucosamine (O-GlcNAc) is observed in several pathologies, and unbalanced O-GlcNAcylation levels favor endothelial dysfunction. Whether augmented O-GlcNAc impacts the uterine artery (UA) function and how it affects the UA during pregnancy remains to be elucidated. We hypothesized that gluc...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173133
更新日期：2020-08-05 00:00:00
abstract：:We have investigated the role of tyrosine kinase in the antiarrhythmic effects of peroxynitrite preconditioning in rat isolated heart by using a tyrosine phosphatase inhibitor, sodium orthovanadate, and tyrosine kinase inhibitors, genistein and tyrphostin. Rat hearts were preconditioned by peroxynitrite administration...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01377-3
更新日期：2003-03-19 00:00:00
abstract：:The involvement of delta opioid receptors in supraspinal analgesia was investigated. With this aim, opioids that produced analgesia in the tail immersion test were administered i.c.v. to mice a few minutes before the irreversible antagonist, beta-funaltrexamine (beta-FNA). Protection of the respective analgesic effect...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90038-1
更新日期：1989-01-02 00:00:00
abstract：:The opioid properties of endomorphin derivatives containing a C-terminal alcoholic(-ol) function were compared to the parent amidated compounds in isolated organs (longitudinal muscle strip of guinea-pig ileum and mouse vas deferens). Similar data were also generated for the mu-opioid receptor selective agonist synthe...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01014-7
更新日期：2001-06-01 00:00:00
abstract：:We sought to examine the involvement of central cannabinoid CB2 receptor activation in modulating mechanical allodynia in a mouse model of neuropathic pain. JWH133 was demonstrated to be a selective cannabinoid CB2 receptor agonist in mice, reducing forskolin-stimulated cAMP production in CHO cells expressing mouse ca...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.01.010
更新日期：2008-03-31 00:00:00
abstract：:In this study, we synthesized a novel carbazole derivative, MHY407, as a sensitizer of cancer cells to increase DNA damage. We then evaluated the anticancer effects of MHY407 and identified the molecular mechanism for the sensitization of breast cancer cell lines. MHY407 significantly increased DNA damage as determine...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.10.001
更新日期：2012-12-15 00:00:00
abstract：:The potencies of histamine and methacholine were significantly increased by approximately 2- and 5-fold respectively in human non-diseased isolated bronchi on removal of the epithelium. In contrast, no increases in spasmogen potency were observed following epithelium removal in bronchi obtained from a sample of asthma...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90360-i
更新日期：1990-10-23 00:00:00
abstract：:The effect of systemic administration of the nonselective dopamine receptor agonist apomorphine on efflux of serotonin (5-hydroxytryptamine, 5-HT) in striatum and hippocampus of freely moving rats was examined using in vivo microdialysis. 5-HT efflux was increased by a moderate dose of apomorphine sufficient for a pos...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00321-5
更新日期：1998-06-26 00:00:00
