Abstract：
:Choline displaced [3H]QNB binding from rat brain muscarinic receptors competitively, (Ki = 460 microM) but it was only 1/1000th as potent as ACh. Deanol was an extremely weak displacer of [3H]QNB binding while hemicholinium-3 was 50 times more potent than choline. Although brain levels of choline are well below its Ki value for muscarinic receptors, choline may directly interact with rat brain muscarinic receptors in some circumstances.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Speth RC,Yamamura HIdoi
10.1016/0014-2999(79)90012-8subject
Has Abstractpub_date
1979-09-15 00:00:00pages
197-201issue
2eissn
0014-2999issn
1879-0712pii
0014-2999(79)90012-8journal_volume
58pub_type
杂志文章abstract：:The effects of the two enantiomers of the antidepressant nomifensine on catecholamine uptake were investigated using rat brain synaptosomes. According to the results from in vitro and ex vivo/in vitro studies, the inhibitory activity on catecholamine uptake resides entirely in the (+)-form of nomifensine. Further stud...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90601-0
更新日期：1984-02-17 00:00:00
abstract：:Pyrethroid insecticides have been reported to increase transmembrane sodium influx and inhibit ion-dependent ATPases in insect, squid, and toad nerve tissues. Since changes in sarcolemmal ion fluxes and inhibition of membrane-bound ATPases can alter myocardial contractility, the effects of a potent synthetic pyrethroi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90279-6
更新日期：1984-03-02 00:00:00
abstract：:Current clinical options for the treatment of neovascular disorders of the posterior segment of the eye have several drawbacks. Photocoagulation lasers can impair peripheral and night vision. Photodynamic therapies as well as intravitreal macromolecule injections (Macugen and Lucentis) require frequent, invasive admin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.04.044
更新日期：2007-07-30 00:00:00
abstract：:To identify the site of action of opiate-induced prolactin elevation, in vitro rat hemipituitary incubations were performed in the presence of morphine, met-enkephalin, ala2-met5-enkephalinamide and dopamine (DA) and combinations of opiate with the catecholamine. No opiate stimulated prolactin release directly nor did...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90227-9
更新日期：1979-12-07 00:00:00
abstract：:Numerous studies have demonstrated the stimulatory effect of 5-HT1A receptor agonists, such as 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), on plasma corticotrophin (ACTH) levels in the rat. However, until recently the lack of a selective 5-HT1A receptor antagonist has hampered mechanistic studies in this area....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90642-4
更新日期：1994-10-13 00:00:00
abstract：:Metabotropic glutamate mGlu(1) receptors play a modulatory role in the nervous system. They enhance cell excitability, modulate synaptic neurotransmission and are involved in synaptic plasticity. During the last 10 years, several selective metabotropic glutamate mGlu(1) receptor competitive antagonists and potentiator...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.12.043
更新日期：2010-08-10 00:00:00
abstract：:Sprague-Dawley rats received oral doses of enalapril maleate (5 mg/kg), a potent, nonsulfhydryl, angiotensin converting enzyme inhibitor, or saline. Sixty min later, morphine sulfate, 5 mg/kg, or saline was injected subcutaneously. Response to a thermal stimulus was monitored before and up to 5 h ter morphine injectio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90607-1
更新日期：1984-02-17 00:00:00
abstract：:The new platinum (II) and palladium (II) complexes (2-4) with ligands 5-(2-hydroxyphenyl)-1,3-dimethyl-4-(dimethoxy)phosphonyl-1H]-pyrazole (1a) and 5-(2-hydroxyphenyl)-1,3-dimethyl-4-methoxycarbonyl-1H]-2-pyrazole (1b) were screened in a search for novel anticancer agents. Thus, alkylating activity, cytotoxicity, abi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.08.053
更新日期：2004-10-11 00:00:00
abstract：:The effect of Ca2+ on the oxytocin-induced, sustained contraction of rat uterine muscle in Ca-free medium after prolonged incubation with 3 mM EGTA (Ca-free contraction) was investigated. A micromolar concentration of Ca2+ caused phasic contraction followed by relaxation while a submicromolar concentration caused rela...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90286-x
更新日期：1987-08-21 00:00:00
abstract：:[D-Met2,Pro5]enkephalinamide (DMPEA) strongly activated cardioinhibitory vagal efferents and elicited bradycardia when perfused through the cerebroventricular system of anaesthetized dogs. These effects were concentration-dependent but plateaued at an intraventricular concentration of 200 micrograms/ml. At this maxima...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90216-x
更新日期：1985-04-02 00:00:00
abstract：:The aim of this work was to investigate the effect of P-glycoprotein modulators on human extraneuronal monoamine transporter (EMT)-mediated transport. The experiments were performed using a cell line from human embryonic kidney (HEK293 cells) stably transfected with pcDNA3hEMT (293(hEMT)), or with pcDNA3 alone (293(co...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01055-x
更新日期：2001-06-22 00:00:00
abstract：:Although cannabinoids are known to be more effective analgesics against chronic rather than acute pain, the mechanism underlying this phenomenon is still unclear. We report now that contralateral thalamic cannabinoid CB(1) receptors are upregulated after unilateral axotomy of the tibial branch of the sciatic nerve, a ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)00798-1
更新日期：2001-03-09 00:00:00
abstract：:Acute noise stress decreased [3H]5-hydroxytryptamine ([3H]5-HT) uptake in synaptosomes from rat hypothalamus, hippocampus and cerebral cortex. The decrease was due to the maximum rate of [3H]5-HT uptake, which peaked 30 min after stress and partly returned to resting values within 4 h, with no changes in affinity (Km ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90211-y
更新日期：1993-09-14 00:00:00
abstract：:H89 (N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide) is a compound characterized in vitro as a potent and selective inhibitor of protein kinase A (PKA). In this study, we found that H89 reduced the phosphorylation of the myosin regulatory light chain (MRLC) at Thr-18/Ser-19 and induced disassembly of stre...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.05.029
更新日期：2008-08-20 00:00:00
abstract：:The effect of aclarubicin on vasocontractility was investigated using aortic strips isolated from rats. The aortic strips from rats injected i.p. with aclarubicin (4 mg/kg body weight per day for 5 consecutive days) showed diminished contractile responses to KCl and phenylephrine in comparison with the controls inject...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90761-9
更新日期：1989-08-11 00:00:00
abstract：:The effect of several pyrolysate mutagens on the benzodiazepine and GABA receptors was investigated. Of amino-gamma-carbolines, Trp-P-1 antagonized the suppressive effect of diazepam on the pentylenetetrazol-induced convulsions and death, whereas Trp-P-2 by itself precipitated seizures and death in male mice. Both Trp...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90106-7
更新日期：1984-02-10 00:00:00
abstract：:The protective effect of coenzyme Q10 against testicular toxicity induced by sodium arsenite (10mg/kg/day, orally for two consecutive days) was investigated in rats. Coenzyme Q10 treatment (10mg/kg/day, i.p.) was applied for five consecutive days, starting three days before arsenite administration. Coenzyme Q10 signif...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.12.045
更新日期：2011-03-25 00:00:00
abstract：:Troxypyrrolidinium, a choline uptake inhibitor, reduced but failed to abolish responses of the rat urinary bladder to electrical stimulation at 1-100 Hz although it reduced acetylcholine output during stimulation at 10 Hz to a level similar to that of spontaneous release. Inhibition of the response to stimulation was ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90131-4
更新日期：1980-02-08 00:00:00
abstract：:Scopolamine, a non-selective muscarinic receptor antagonist has widespread central nervous system effects. Muscarinic receptors located in the central nervous system play a vital role in the modulation of impulsivity. The objective of the current study was to evaluate the effect of scopolamine on impulsivity using dif...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.10.005
更新日期：2013-11-15 00:00:00
abstract：:Rat hearts were perfused at 37 degrees C with three clearly-defined protocols: the Ca2+ paradox, the O2 paradox and with 20 mM caffeine. Each protocol involved an initial priming (stage 1) and a subsequent full activation (stage 2) of the damage system of the sarcolemma. Raising [K+]o from 5.4 to 6.5 mM in the Ca2+ pa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00676-0
更新日期：1996-12-05 00:00:00
abstract：:Several anticancer drugs are ineffective against brain tumor and do not impact patient survival because they fail to cross the blood-brain tumor barrier (BTB) effective levels. One such agent temozolomide is commonly used in brain tumor patients, which works better when combined with radiation or other anticancer agen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.10.056
更新日期：2009-01-14 00:00:00
abstract：:Dantrolene sodium (3 X 10(-4) M) exerted a biphasic effect on the mechanical and electrical activity of the isolated guinea pig left atrium. In the first phase, the drug increased the contractile force by about 200%, and prolonged the action potential duration. This transient positive inotropic effect was antagonized ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90529-x
更新日期：1981-09-11 00:00:00
abstract：:Selegiline, a therapeutic agent of Parkinson's disease, and its metabolite, desmethylselegiline, were explored for their neuroprotective effects against N-methyl-D-aspartate (NMDA)-induced cell death in rat retina. Morphometric analysis of the retina revealed that an intravitreal injection of NMDA induced a significan...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02729-2
更新日期：2003-01-01 00:00:00
abstract：:The purpose of this study was to investigate whether the selective angiotensin AT2 receptor ligands, CGP 42112B (Nic-Tyr-(N alpha-benzoyloxycarbonyl-Arg)Lys-His-Pro-Ile-OH) and PD 123319 ((s)-1-[[4-(dimethylamino)-3-methyl-phenyl]methyl]-5-(diphenylacetyl+ ++)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]-pyridine-6-carboxylic...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90153-8
更新日期：1994-06-23 00:00:00
abstract：:(25R)-spirost-5-en-3β-ol, also known as diosgenin (DSG), exerts antiproliferative activity on diverse cell lines, induces apoptosis, and acts as a chemopreventative agent. However, the relationship between DSG glycosides and apoptotic, necrotic, and antiproliferative activity remains unclear. It is in this regard that...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.172942
更新日期：2020-03-15 00:00:00
abstract：:The purpose of this study was to investigate whether high conductance Ca2+-activated K+ channels (BK(Ca)) are mediating the vasodilator action of hydralazine. In isolated porcine coronary arteries, hydralazine (1-300 microM), like the K+ channel opener levcromakalim, preferentially relaxed contractions induced by K+ (...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00701-8
更新日期：1998-11-13 00:00:00
abstract：:In vitro effects of d,l-methadone and morphine on [3H]serotonin (3H-5-HT) uptake in rat periaqueductal gray (PAG) slices were investigated. Only methadone had a significant inhibitory effect on 3H-5-HT uptake which was significantly enhanced by naloxone. The systemic administration of methadone did not affect 3H-5-HT ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90030-x
更新日期：1979-10-26 00:00:00
abstract：:The effects of endothelin, a potent endogenous vasoconstrictor peptide, were examined in a range of vascular and non-vascular tissues. At concentrations that cause vasoconstriction in portal vein and aorta, the peptide strongly contracted rat uterus, trachea and vas deferens, but not guinea pig ileum. Nifedipine, a di...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90716-4
更新日期：1989-06-20 00:00:00
abstract：:After chronic exposure to neurokinin A, a time-dependent and recoverable desensitization of inositol monophosphate accumulation occurred in B82 fibroblasts transfected with cDNAs encoding for the bovine stomach NK2 receptor. Desensitized cells also showed decreased Ca2+ mobilization. While NK2 receptor antagonists had...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(93)90172-6
更新日期：1993-03-15 00:00:00
abstract：:The influence of inflammatory cells on airway reactivity was investigated on arachidonic acid-induced relaxations of guinea-pig trachea and on arachidonic acid metabolism in guinea-pig tracheal epithelial cells. The presence of either eosinophils or neutrophils (1.0 x 10(7) cells/ml), from bronchoalveolar lavage, decr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00736-4
更新日期：1996-12-19 00:00:00
