Abstract：
:In the presence of RS-15385-197 to preclude binding to alpha 2-adrenoceptors, [3H]p-aminoclonidine labelled a low affinity high capacity site, (Kd = 127.6 +/- 19.7 nM, Bmax 978 +/- 172 fmol/mg protein) whereas [3H]idazoxan labelled a high affinity low capacity site (Kd = 1.66 +/- 0.28 nM, Bmax 45.3 +/- 11.4 fmol/mg protein). Clonidine and p-aminoclonidine showed moderate affinity for the site labelled by [3H]p-aminoclonidine, but low affinity for the site labelled by [3H]idazoxan, whereas idazoxan showed high affinity for [3H]idazoxan and low affinity for [3H]p-aminoclonidine binding. Naphazoline inhibited [3H]idazoxan in a biphasic manner suggesting that [3H]idazoxan may label an heterogeneous population of imidazoline sites. GTP inhibited [3H]idazoxan but not [3H]p-aminoclonidine binding. These results suggest that [3H]idazoxan labelled imidazoline I2 binding sites, whereas [3H]p-aminoclonidine labelled a novel subtype which showed marked differences to the imidazoline I1 binding site reported in bovine and human brainstem.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
MacKinnon AC,Stewart M,Olverman HJ,Spedding M,Brown CMdoi
10.1016/0014-2999(93)90731-vsubject
Has Abstractpub_date
1993-02-23 00:00:00pages
79-87issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(93)90731-Vjournal_volume
232pub_type
杂志文章abstract：:SL 84.0418 (2-(4,5-dihydro-1H-imidazol-2-yl)-1,2,4,5-tetrahydro-2-propyl-pyrrolo[3, 2,1- hi]-indole hydrocholoride) is a novel alpha 2-adrenoceptor antagonist which possesses anti-hyperglycaemic properties in vitro study, we tested its effects on insulin release from isolated mouse islets. In the presence of 15 mM glu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90366-2
更新日期：1994-03-11 00:00:00
abstract：:A brain slice preparation was used to examine the effects of galanin on the spontaneous firing rate of locus coeruleus noradrenergic neurons. Galanin (10(-9)-10(-7) M), added to the bath, inhibited the firing of 14 out of 19 neurons in a concentration-dependent manner. The observed effect was quite variable, ranging f...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90481-0
更新日期：1989-05-19 00:00:00
abstract：:The muscarinic agonist McN-A-343 did not affect the tone or nitroprusside-induced relaxations of the rat anococcygeus, but inhibited non-adrenergic non-cholinergic (NANC) relaxations. Atropine, pirenzepine and gallamine blocked the McN-A-343 inhibition of NANC relaxations. Agonists of alpha 1-(methoxamine) or alpha 2-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90640-7
更新日期：1989-09-01 00:00:00
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：:We investigated the relationship between tension development and the cytosolic free Ca2+ level ([Ca2+]i) on exposure of the endothelium-denuded isolated rat aorta to palmitoyl-L-alpha-lysophosphatidylcholine. Lysophosphatidylcholine concentration-dependently induced a gradual increase in [Ca2+]i. Application of 10(-4)...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00458-6
更新日期：1999-08-06 00:00:00
abstract：:α1-Adrenoceptor stimulation of mouse aorta causes intracellular Ca(2+) release from sarcoplasmic reticulum Ca(2+) stores via stimulation of inositoltriphosphate (IP3) receptors. It is hypothesized that this Ca(2+) release from the contractile and IP3-sensitive Ca(2+) store is under the continuous dynamic control of ti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.04.011
更新日期：2015-08-05 00:00:00
abstract：:Kynuramine increased heart rate and blood pressure in pithed rats. Heart rate responses were blocked by beta-adrenoceptor antagonists and reserpine pretreatment. Both of these treatments reduced the pressor responses to kynuramine. Remaining pressor activity was inhibited by phentolamine. The pressor responses to kynu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90346-1
更新日期：1983-02-18 00:00:00
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：:Administration of endothelin to inactin-anesthetized rats resulted in a significant renal vasoconstriction as evidenced by a reduction in both renal plasma flow and glomerular filtration rate. Infusion of the novel nonpeptide endothelin ETA/ETB receptor antagonist, (+/-)-SB 209670, [(1RS-2SR,3RS)-3-(2-carboxymethoxy-4...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00591-9
更新日期：1995-12-29 00:00:00
abstract：:The relationship between isometric tension and the increase in cyclic GMP level associated with the initial phase of drug-induced contraction of taenia coli was studied. Maximal contraction induced by 100 micrometers carbachol or 124 mM KCl occurred in 30 sec and was associated with an increase in cyclic GMP levels of...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90209-0
更新日期：1981-03-12 00:00:00
abstract：:The responsiveness of the rat striatal dopamine (DA) receptor system to apomorphine (APO) was assessed after 10 days of antidepressant administration. Desipramine (DMI), dothiepin (DOTH), iprindole (IPR) and nomifensine (NOM) were administered intra-peritoneally, twice daily, to rats for 10 days and 42 h after the las...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90617-4
更新日期：1984-10-15 00:00:00
abstract：:C-type natriuretic peptide (CNP) is the major natriuretic peptide in the brain and its mRNA has been reported in the central nervous system, which supports local synthesis and its role as a neuromodulator. The aim of the present work was to study the effect of centrally applied CNP on pancreatic secretion. Rats were f...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.09.015
更新日期：2005-11-07 00:00:00
abstract：:Our goal was to determine if venlafaxine has a negative effect on bone metabolism. Rats were divided into three groups. The sham-operated control group (SHAM), the control group after orchidectomy (ORX), and the experimental group after orchidectomy received venlafaxine (VEN ORX) in standard laboratory diet (SLD) for ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.04.029
更新日期：2015-08-15 00:00:00
abstract：:There is no established pharmacological therapy for skin keloids, a wound healing disorder. In this study, we investigated the effect of N-benzoyl staurosporine (PKC412), a protein kinase C inhibitor, on human keloid-derived fibroblasts to examine whether this agent is applicable for the treatment of keloid formation....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.06.050
更新日期：2004-08-23 00:00:00
abstract：:Pain is a global health challenge. For decades, we have been primarily relying upon opioids and nonsteroidal anti-inflammatory drugs (NSAIDs) for pain management. However, adverse effects related to opioid and NSAID use are severe and often lead to forced drug discontinuation and inadequate pain relief. Despite decade...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2012.01.017
更新日期：2012-04-15 00:00:00
abstract：:The breakdown of the relaxation-inducing second messengers cAMP and cGMP is mediated by phosphodiesterases. Inhibitors of functionally present phosphodiesterases can be expected to induce relaxation by increasing the basic amount of cAMP and/or cGMP. In the cat gastric fundus, vinpocetine, which has some selectivity f...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00009-a
更新日期：1995-03-24 00:00:00
abstract：:The aim of the present research was to characterize the pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel quinazolinone-based dipeptidyl peptidase-4 (DPP-4) inhibitor. Alogliptin potently inhibited human DPP-4 in vitro (mean IC(50), ~ 6.9 nM) and exhibited > 10,000-fold selectivity for DPP...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.04.047
更新日期：2008-07-28 00:00:00
abstract：:Dextromethorphan which is an active ingredient in many cough medicines has been previously shown to potentiate amnesic effect of morphine in rats. However, the effect of dextromethorphan, that is also a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist, in combination with morphine on hippocampus-based lo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.11.025
更新日期：2017-01-05 00:00:00
abstract：:In the present study, the development of tolerance to the motor impairing effects of gamma-hydroxybutyric acid (GHBA) and ethanol was compared (Experiment 1). Rats were required to perform a motor coordination task daily shortly after ethanol (3.5 g/kg) and GHBA (1.0 g/kg) administration for 9 consecutive days. Tolera...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)00687-3
更新日期：1995-02-06 00:00:00
abstract：:Organ culture is an in vitro method for investigating cellular mechanisms involved in upregulation of vasocontractile G-protein coupled receptors. We hypothesize that mitogen-activated-protein kinase (MEK) and/or extracellular-signal-regulated kinase (ERK) specific inhibitors will attenuate the G-protein coupled recep...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.06.053
更新日期：2010-10-10 00:00:00
abstract：:Hypoglycemia developed in fasted rats during forced swimming. This hypoglycemia was mostly abolished by phentolamine, an alpha-adrenolytic agent, or by hexamethonium; was potentiated by propranolol, a beta-adrenolytic agent, of by 5-methoxyindole-2-carboxylic acid, a gluconeogenic inhibitor; and was not affected by an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90184-4
更新日期：1977-03-07 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：:The binding of [3H]N-(1-[2-thienyl]cyclohexyl)piperidine (TCP) to N-methyl-D-aspartate (NMDA) receptor sites in synaptic membranes prepared from the dorsal hippocampus of the ischaemic gerbil, has been studied. Forebrain ischaemia was induced by 10 min bilateral carotid occlusion and receptor binding determined in the...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90855-2
更新日期：1988-07-26 00:00:00
abstract：:We studied beta-adrenoceptors by quantitative autoradiography in the cardiac vagus ganglia of the rat, after incubation of tissue sections with [125I]iodocyanopindolol. The cardiac vagus ganglia presented a high concentration of a single population of high affinity binding sites (Bmax 109 +/- 10 fmol/mg protein; Kd 64...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90617-6
更新日期：1988-08-24 00:00:00
abstract：:WEB 2086, a novel specific platelet activating factor (PAF) antagonist derived from triazolodiazepines, inhibited in a dose-related manner the hypotensive and lethal effect of PAF as well as of E. coli endotoxin in the rat. The hypotension induced by endotoxin (15 mg/kg i.v.) or PAF (30 ng/(kg X min) i.v.) in anaesthe...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90602-9
更新日期：1987-03-17 00:00:00
abstract：:This study investigated the characteristics of atrial natriuretic peptide (ANP) release from superfused sliced atria and ventricles of rats. Right atria spontaneously released more immunoreactive ANP (Ir-ANP: pg/min per mg tissue) (32 +/- 3) than did left atria (11 +/- 2) or right ventricles (1.5 +/- 0.5). Addition of...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90009-f
更新日期：1991-12-10 00:00:00
abstract：:It has been well documented that nordihydroguaiaretic acid (NDGA), a phenolic lignan isolated from the creosote bush, Larrea tridentate, has anti-cancer activity in vitro and in vivo. Several mechanisms have been identified that could contribute to these actions, as NDGA directly inhibits metabolic enzymes and recepto...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.06.012
更新日期：2009-08-15 00:00:00
abstract：:We investigated intracellular Ca2+ regulation in pancreatic acinar cells from rats with diabetes induced by a single injection of streptozotocin (80 mg/kg). Experiments were performed 2 days and 7 days after the injection of streptozotocin. The density of muscarinic receptors, measured by [3H]N-methyl scopolamine bind...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00796-2
更新日期：1996-03-18 00:00:00
abstract：:The present study was performed to examine the sedative effects of second-generation histamine H(1) receptor antagonist using power spectrum analysis in the rat. Similar to ketotifen, olopatadine caused a decrease in sleep latency at a dose of 50 mg/kg, while epinastine and cetirizine showed no significant effect even...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.05.010
更新日期：2004-06-28 00:00:00
abstract：:Pramipexole (SND 919; 2-amino-4,5,6,7-tetrahydro-6-propyl-amino-benzthiazole-dihydroc hlo ride) is a novel dopamine D2 family receptor agonist with a predominant action on D2 autoreceptors and with some D3 vs. D2 receptor preference. The central behavioural effects of pramipexole given subcutaneously to rats (male Wis...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)00066-6
更新日期：1997-04-11 00:00:00
