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Showing papers in "European Journal of Pharmacology in 1994"


Journal ArticleDOI
TL;DR: Rat liver and kidney were investigated for the presence of sigma (σ) receptor subtypes by radioligand binding with three highly selective σ probes and by photoaffinity labeling using [H]azido-di-o-tolyguanidine ([3H]AZido-DTG and [3H](+)-3-PPP + dextrallorphan, suggesting that liver and kidneys contain both subtypes of σ receptor.

401 citations


Journal ArticleDOI
TL;DR: The ligand preferences of recombinant NR1 homomeric and NR1-NR2 heteromeric NMDA receptors were examined by homogenate binding assay as discussed by the authors, and the binding affinities for most ligands were similar to those reported for native NMDA receptor.

372 citations


Journal ArticleDOI
TL;DR: BIBP3226 displayed potent antagonistic properties both in in vitro and in vivo models and thus represents the first selective non-peptide neuropeptides Y Y1 receptor antagonist.

365 citations


Journal ArticleDOI
TL;DR: There is no firm scientific evidence at present to recommend drastic reductions beyond the average levels of nitrate encountered in vegetables grown in keeping with good agricultural practice, and recommendations are made for further animal and human studies to elucidate the potential risks to man from ingested nitrate.

342 citations


Journal ArticleDOI
TL;DR: In this article, the potency of four different lipophilic GABA transporters, namely GAT1, GAT-2, BGT-1, and GAT3, has been determined.

324 citations


Journal ArticleDOI
TL;DR: NS 1619 is a selective and new type of K+ channel activator, which may significantly modulate cell excitability, which was antagonized by charybdotoxin as well as by tetraethylammonium ions and hyperpolarized the smooth muscle cells.

307 citations


Journal ArticleDOI
TL;DR: The data indicate that stimulation of adenosine A3 receptors may play an important role in the development of ischemic damage, and that adenosines A2 receptors may offer a new target for therapeutic interventions.

268 citations


Journal ArticleDOI
TL;DR: It is found that the stress-induced deficit in sucrose intake was gradually reversed by chronic (4-5 weeks) treatment with MK-801 and CGP, suggesting that antagonists of NMDA receptors may have antidepressant properties.

266 citations


Journal ArticleDOI
TL;DR: The study of the baculovirus-eukaryotic cell expression system provides the first evidence that the human dopamine D1 receptor undergoes agonist-dependent desensitization, phosphorylation and palmitoylation.

186 citations


Journal ArticleDOI
TL;DR: Findings indicate that adrenomedullin is a potent renal vasodilatory peptide with a diuretic action, close to its physiological concentration in human plasma, and may play an important role in the regulation of renal function.

184 citations


Journal ArticleDOI
TL;DR: It is indicated that acute cycloserine administration can enhance consolidation and retrieval of memory but that desensitization may occur with chronic exposure to the drug.

Journal ArticleDOI
TL;DR: Diclofenac has a direct effect on ongoing hyperalgesia in addition to its ability to block cyclo-oxygenase, thus indicating that the analgesic effect of the latter is independent of a central or peripheral opioid effect.

Journal ArticleDOI
TL;DR: The data suggest an involvement of the mineralocorticoid receptor in the regulation of the 5-HT1A receptor mRNA and a possible synergistic effect of additional glucocortioid receptor activation.

Journal ArticleDOI
TL;DR: It is suggested that the addition of a nitroxybutyl moiety to diclofenac markedly reduces the ulcerogenic properties of this compound without interfering with its ability to inhibit cyclo-oxygenase activity or to reduce acute inflammation.

Journal ArticleDOI
TL;DR: Clozapine was studied in functional assays at human muscarinic M1-M5 receptors expressed in Chinese hamster ovary cells, producing inhibition of forskolin-stimulated cAMP accumulation and potentially contributing to its atypical antipsychotic efficacy.

Journal ArticleDOI
TL;DR: The data obtained suggest that (Rp)-8-pCPT-cGMPS may be a useful tool for studying the role of cGMP in vitro and in intact cells.

Journal ArticleDOI
TL;DR: It is concluded that the neuropharmacological effects of metalloporphyrins may result from their direct inhibition of soluble guanylyl cyclase, rather than from an effect on carbon monoxide synthesis.

Journal ArticleDOI
TL;DR: Using membranes from whole rat brain yields data suggesting that all three Nicotinic ligands bind to the same nicotinic acetylcholine receptor subtype, and are unable to distinguish subtypes of neuronal nicotinIC acetyl choline receptor at the level examined.

Journal ArticleDOI
TL;DR: It is demonstrated that 5-HT1A somatodendritic autoreceptors and post-synaptic receptors mediate anxiolytic and anxiogenic effects, respectively, in the social interaction test of anxiety.

Journal ArticleDOI
TL;DR: It is demonstrated that phenylglycine analogs possess differential functional activities at subtypes of the mGluR family.

Journal ArticleDOI
TL;DR: The hypothesis that the functional dopamine D3 receptor is a postsynaptic receptor inhibitory on rat locomotion is supported and the present data support the hypothesis.

Journal ArticleDOI
TL;DR: The results suggested that KF17837 is a centrally active adenosine A2A receptor antagonist and that the dopaminergic function of the nigrostriatal pathway is potentiated by adenosines A1A receptor antagonists, and may be a useful drug in the treatment of parkinsonism.

Journal ArticleDOI
TL;DR: It is concluded that activation of 5- HT2 receptors is an important determinant of the acute increase in extracellular dopamine and, consequently, the long-term depletion of brain 5-HT produced by MDMA.

Journal ArticleDOI
TL;DR: The results demonstrate that rod bipolar cells possess two populations of pharmacologically distinct GABA receptors, GABAA and novel-type GABAC receptors, which might subserve different physiological functions in controlling visual transduction in the retina.

Journal ArticleDOI
TL;DR: Treatment with SR-3 for a period of 3 weeks prior to challenge was found effective in each of these experimental models of epileptic seizures and caused up to a 22-fold increase in latency to major motor seizures.

Journal ArticleDOI
TL;DR: It is suggested that somatodendritic 5- HT1A receptors are desensitized after chronic treatment with citalopram and this results in facilitation of its effect on cortical dialysate 5-HT.

Journal ArticleDOI
TL;DR: It is suggested that opiate abstinence develops within the first 24 h and follows the time course of the development of tolerance, dependence and abstinence following subcutaneous pellet implantation.

Journal ArticleDOI
TL;DR: It is demonstrated that 5- HT2A receptors mediate the discriminative stimulus effects of DOI and support the hypothesis that an antagonistic action at 5-HT2a receptors contributes to the in vivo actions of 'atypical' antipsychotics.

Journal ArticleDOI
TL;DR: The ligand-selective cAMP accumulation, its independence from Ca2+ and the carbachol-activated adenylyl cyclase in membranes suggest that it represents an independent m1AChR-mediated signal, unrelated to phosphoinositide hydrolysis.

Journal ArticleDOI
TL;DR: Results demonstrate that activation of protein kinase C alters dopamine transporter functions in both ligand recognition and substrate translocation and suggest the possibility that phosphorylation could modulate the activity of this important dopaminergic synaptic regulator under physiological conditions.