Prophylactic effect of serotonin uptake inhibitors against motion sickness in Suncus murinus.

abstract：:We have studied the pharmacological effects of (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and the enantiomers of (RS)-2-amino-3-(3-hydroxy-1,2, 5-thiadiazol-4-yl)propionic acid (TDPA) on cloned human excitatory amino acid transporter subtypes 1, 2 and 3 (EAAT1-3) expressed in Cos-7 cells. Wh...

journal_title：European journal of pharmacology

authors： Bräuner-Osborne H,Hermit MB,Nielsen B,Krogsgaard-Larsen P,Johansen TN

更新日期：2000-10-06 00:00:00

abstract：:We now describe the preparation and characterization of a novel radioligand, 2-[125I]iodo-5-methoxy-carbonylamino-N-acetyltryptamine (2-[125I]MCA-NAT), with high affinity and pharmacological selectivity for melatonin ML2 receptor sites. 2-[125I]MCA-NAT was prepared by introducing an [125I]iodine molecule on carbon 2 o...

journal_title：European journal of pharmacology

authors： Molinari EJ,North PC,Dubocovich ML

更新日期：1996-04-22 00:00:00

abstract：:Systemic or intracerebral administration of kainic acid in rodents induces neuronal death followed by a cascade of neuroplastic changes in the hippocampus. Kainic acid-induced neuroplasticity is evidenced by alterations in hippocampal neurogenesis, dispersion of the granule cell layer and re-organisation of mossy fibr...

journal_title：European journal of pharmacology

authors： Jaako K,Aonurm-Helm A,Kalda A,Anier K,Zharkovsky T,Shastin D,Zharkovsky A

更新日期：2011-09-01 00:00:00

abstract：:The effect of simultaneous topical application of adrenergic agonists was investigated on the polydipsia caused by direct carbachol (CCh) stimulation of the rat brain. In addition, fluid selection (4-choice arrangement) was studied. Noradrenaline and isoprenaline fully antagonized the CCh effect after either intracere...

journal_title：European journal of pharmacology

authors： Schmidt P,Zámbó K,Decsi L,Nagy J

更新日期：1981-10-15 00:00:00

abstract：:The effects of four fluoroquinolones (sparfloxacin, fleroxacin, ofloxacin and levofloxacin) on K(+) currents were investigated in pyramidal neurons acutely isolated from rat hippocampus, to evaluate their relative potencies for inhibiting these channels. Using patch-clamp electrophysiological techniques, we found that...

journal_title：European journal of pharmacology

authors： Zhang LR,Li MH,Cheng NN,Chen BY,Wang YM

更新日期：2003-02-21 00:00:00

abstract：:Studies were done to assess the effects of 4-aminopyridine (4AP) and streptomycin (SM) on transmitter release parameters and extracellularly recorded presynaptic action potential. The application of 5 micrometer 4AP resulted in a marked increase in the mean quantal content (m1) associated with an increase in the total...

journal_title：European journal of pharmacology

authors： Enomoto K,Maeno T

更新日期：1981-11-19 00:00:00

abstract：:The effect of idebenone on the changes in adenosine and nucleotide metabolism occurring in hippocampal slices after ischemia-like conditions (superfusion with glucose-free Krebs solution gassed with 95% N2-5% CO2) and during reperfusion with normal Krebs solution was investigated by measuring adenosine and inosine out...

journal_title：European journal of pharmacology

authors： Latini S,Pedata F,Pepeu G

更新日期：1993-11-02 00:00:00

abstract：:Ro 40-5967 [(1S,2S)-2-[2[3-(2-benzamidopropyl]- methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphthyl- methoxyacetate] is a new Ca2+ channel antagonist active at L-type channels. Radioligand binding studies in cardiac tissue show that Ro 40-5967 does not inhibit 1,4-dihydropyridine binding, but does in...

journal_title：European journal of pharmacology

authors： Rutledge A,Triggle DJ

更新日期：1995-07-04 00:00:00

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 ...

journal_title：European journal of pharmacology

authors： Goldstein JM,Knobloch LC,Malick JB

更新日期：1983-07-15 00:00:00

abstract：:Corticotropin-releasing factor (CRF) is a neurohormone that mediates stress, anxiety, and affects serotonergic activity. Studies have shown that CRF has dose-dependent opposing effects on serotonergic activity. This effect has been hypothesized to be differentially mediated by CRF(1) and CRF(2) receptors in the dorsal...

journal_title：European journal of pharmacology

authors： Lukkes JL,Forster GL,Renner KJ,Summers CH

更新日期：2008-01-14 00:00:00

abstract：:In isolated guinea pig bronchi, the influence of ruthenium red, capsazepine and extracellular Ca2+ on capsaicin-induced desensitization was examined to investigate whether this desensitization was mediated via a specific receptor coupled with an ion channel. Pre-exposure of tissues to capsaicin (1, 3 or 10 microM) cau...

journal_title：European journal of pharmacology

authors： Jung YS,Cho TS,Moon CH,Shin HS

更新日期：1998-12-04 00:00:00

abstract：:Opiates impair neutrophil-mediated host defense, but the involvement of kappa-opioid receptors in this action has not been defined. The selective kappa-opioid receptor agonist [trans-(+)3,4-dichloro-N-methyl-N[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide methanesulfonate inhibited macrophage inflammatory protein-2-i...

journal_title：European journal of pharmacology

authors： Kulkarni-Narla A,Walcheck B,Brown DR

更新日期：2001-03-02 00:00:00

abstract：:The activity of a selective tachykinin NK1 receptor antagonist, PD 154075 ([(2-benzofuran)-CH2OCO]-(R)-alpha-MeTrp-(S)-NHCH(CH3) Ph), was examined in radioligand binding studies, in a [Sar9,Met(O2)11]substance P-induced foot-tapping model in the gerbil, and in cisplatin-induced acute and delayed emesis in the ferret. ...

journal_title：European journal of pharmacology

authors： Singh L,Field MJ,Hughes J,Kuo BS,Suman-Chauhan N,Tuladhar BR,Wright DS,Naylor RJ

更新日期：1997-02-26 00:00:00

abstract：:Diabetic cardiomyopathy (DCM) is one of the major cardiac complications in diabetic patients and a major reason for the death of diabetic patients. Obeticholic acid (OCA) is a semi-synthetic bile acid analogue. The objective of the present study was to investigate the possible cardio-protective effect of OCA against D...

journal_title：European journal of pharmacology

authors： Wu H,Liu G,He Y,Da J,Xie B

更新日期：2019-09-05 00:00:00

abstract：:The inflammation and proliferation of vascular smooth muscle cells (VSMCs) are the basic pathological feature of proliferative vascular diseases. Tanshinone ⅡA (Tan ⅡA), which is the most abundant fat-soluble element extracted from Salvia miltiorrhiza, has potent protective effects on the cardiovascular system. Howeve...

journal_title：European journal of pharmacology

authors： Qin Y,Zheng B,Yang GS,Zhou J,Yang HJ,Nie ZY,Wang TR,Zhang XH,Zhao HY,Shi JH,Wen JK

更新日期：2020-08-05 00:00:00

abstract：:Platelet serotonin (5HT) uptake was measured in 18 subjects administered physostigmine salicylate in a double-blind, placebo crossover design. In comparison to placebo, the drug caused a significant transient depression in mood, as measured by self- and observer-rated depression scores. In addition, physostigmine sign...

journal_title：European journal of pharmacology

authors： Rausch JL,Janowsky DS,Risch SC,Huey LY

更新日期：1985-02-12 00:00:00

abstract：:The effect of potassium on the binding of digoxin or digoxigenin to isolated Na+, K+-ATPase was compared with that of potassium on the positive inotropic action of the agents in guinea-pig hearts. The binding of digoxigenin to the enzyme in vitro was reduced to a greater extent by potassium than was the binding of dig...

journal_title：European journal of pharmacology

authors： Akera T,Wiest SA,Brody TM

更新日期：1979-08-15 00:00:00

abstract：:Unlike classical antipsychotic drugs, clozapine activates the hypothalamo-pituitary-adrenal axis and induces a specific regional pattern of Fos-protein expression in the rat forebrain. Whether corticosterone plays a role in the clozapine-induced Fos response is the subject of this study. Some rats were adrenalectomize...

journal_title：European journal of pharmacology

authors： Sebens JB,Middelveld RJ,Koch T,Ter Horst GJ,Korf J

更新日期：2001-04-06 00:00:00

abstract：:The aim of the present study was to examine the influence of ifenprodil (a non-competitive NMDA receptor antagonist which also blocks 5-HT3 receptors and alpha1-adrenoceptors) on the effects of ethanol in the mouse in vivo and to elucidate the role of various receptors in these actions. The ethanol (4 g/kg i.p.)-induc...

journal_title：European journal of pharmacology

authors： Malinowska B,Napiórkowska-Pawlak D,Pawlak R,Buczko W,Göthert M

更新日期：1999-07-14 00:00:00

abstract：:Malfunction of the serotonergic system and dysregulation of the hypothalamo-pituitary-adrenocortical axis have been implicated in the pathophysiology of depression. Several studies provide evidence for reciprocal influences between glucocorticoids and 5-HT receptors. The effect of repeated treatment with a high dose o...

journal_title：European journal of pharmacology

authors： Berendsen HH,Kester RC,Peeters BW,Broekkamp CL

更新日期：1996-07-18 00:00:00

abstract：:Evidence suggests that insulin has direct, potent and physiologically relevant vasodilatory effects. This has led to the hypothesis that in states of insulin resistance, insulin's vasodilatory effects may be blunted leading to an increase in vascular tone and blood pressure. To examine this proposition we studied the ...

journal_title：European journal of pharmacology

authors： Verma S,Bhanot S,Yao L,McNeill JH

更新日期：1997-03-19 00:00:00

abstract：:Chronic administration of amphetamine to cats (twice daily, in doses increasing from 5 to 15 mg/kg over a 10-day period) elicited a number of behaviors e.g., limb flicking, abortive grooming, and excessive head shaking, which were originally proposed as an animal behavioral model for studying the actions of hallucinog...

journal_title：European journal of pharmacology

authors： Trulson ME,Crisp T

更新日期：1984-04-06 00:00:00

abstract：:The alpha1-adrenoceptor subtypes of rat prostate were characterized in binding and functional experiments. In binding experiments, [3H]tamsulosin bound to a single class of binding sites with an affinity (pKD) of 10.79+/-0.04 and Bmax of 87+/-2 fmol mg(-1) protein. This binding was inhibited by prazosin, 2-(2,6-dimeth...

journal_title：European journal of pharmacology

authors： Hiraoka Y,Ohmura T,Oshita M,Watanabe Y,Morikawa K,Nagata O,Kato H,Taniguchi T,Muramatsu I

更新日期：1999-01-29 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

authors： Budzisz E,Krajewska U,Rozalski M,Szulawska A,Czyz M,Nawrot B

更新日期：2004-10-11 00:00:00

abstract：:Compared with sham-operated guinea pigs, chronic heart failure produced by aortic constriction resulted in a 79% increase in alpha 1-adrenoceptor density as measured by [3H]prazosin binding (73 +/- 15 vs. 131 +/- 20 fmol/mg protein, P < 0.05); beta-adrenoceptor number, measured by (-)-[3H]dihydroalprenolol binding, in...

journal_title：European journal of pharmacology

authors： Karliner JS,Barnes P,Brown M,Dollery C

更新日期：1980-10-03 00:00:00

abstract：:We investigated the mechanism of antithrombin III-induced vascular release of endothelins in rat isolated lung. The antithrombin III-stimulated release of big endothelin-1 and endothelin-1 (1.7-fold and 1.3-fold over baseline) was abolished by nicardipine (L-type Ca2+ channel blocker), heparin, and N-acetyl heparin (a...

journal_title：European journal of pharmacology

authors： Stangl K,Dschietzig T,Alexiou K,Brunner F

更新日期：1999-04-01 00:00:00

abstract：:A series of 26 drugs was tested for in vitro binding to opiate receptors in the presence and absence of 0.1 M NaCl. The results were correlated with assays for in vivo pharmacological potency. Highly significant correlation was found between binding in the presence and absence of sodium ions and analgesic potency. For...

journal_title：European journal of pharmacology

authors： Stahl KD,van Bever W,Janssen P,Simon EJ

更新日期：1977-12-01 00:00:00

abstract：:We investigated the influence of inhibition of nitric oxide (NO) synthase, using NG-nitro-L-arginine (L-NNA) or NG-mono-methyl-L-arginine (L-NMMA), and the effects of exogenous donor of NO, such as glyceryl trinitrate (GTN), on the healing of chronic gastric ulcers induced by acetic acid, on gastric blood flow around ...

journal_title：European journal of pharmacology

authors： Konturek SJ,Brzozowski T,Majka J,Pytko-Polonczyk J,Stachura J

更新日期：1993-08-03 00:00:00

abstract：:In recent years, the pilocarpine model of temporal lobe epilepsy has become the most popular and widely used rodent model of this common and difficult-to-treat type of epilepsy. In this model, the cholinomimetic convulsant pilocarpine is used to induce a status epilepticus, which is followed by hippocampal damage and ...

journal_title：European journal of pharmacology

authors： Müller CJ,Bankstahl M,Gröticke I,Löscher W

更新日期：2009-10-01 00:00:00

abstract：:The cerebrovascular actions of bosentan, a novel endothelin antagonist with effects at endothelin ETA and ETB receptors, have been examined in individual pial arterioles on the cortical surface of chloralose-anaesthetised cats. Subarachnoid perivascular microapplication of bosentan (0.3-300 microM) had minimal effect ...

journal_title：European journal of pharmacology

authors： Patel TR,McAuley MA,McCulloch J

更新日期：1994-07-21 00:00:00